THE NAUTA PHARMACOCHEMISTRY AWARD FOR MEDICINAL CHEMISTRY AND CHEMICAL BIOLOGY Award Lecture
Prof. Ad P. IJZERMAN
LEIDEN UNIVERSITY, Leiden, The Netherlands Read more
Prof. Ad P. IJZERMAN
Ad P. IJzerman, professor of medicinal chemistry at the Leiden Academic Centre for Drug Research, Leiden University, the Netherlands.
Ad IJzerman is an expert on G protein-coupled receptors (GPCRs), an important class of drug targets. Over the years he has blended his medicinal chemistry background with computational and pharmacological approaches to unravel novel concepts in GPCR drug discovery. Gradually he developed the notion that GPCRs are "allosteric machines", which are activated and inhibited in many different ways. Principles studied by him such as intrinsic efficacy, insurmountable antagonism and residence time scratch the surface of what is known about this protein superfamily. His contributions to collaborative efforts in the structural biology of GPCRs, long thought out of reach, elucidated and visualized among others i) the unexpected binding orientation of an antagonist, ii) the sodium ion binding site on many GPCRs, and iii) the textbook-changing presence of two antagonists at the same time.
Ad was trained as a pharmacist at Utrecht University, and obtained his PhD degree in medicinal chemistry at the Vrije Universiteit Amsterdam under the supervision of Henk Timmerman. Thereafter he moved to Leiden University, where he has been a professor since 2001.
THE UCB-EHRLICH AWARD FOR EXCELLENCE IN MEDICINAL CHEMISTRY Award Lecture
Dr. Malin Lemurell is the Head of Head of Medicinal Chemistry in Cardiovascular, Renal and Metabolism at AstraZeneca Gothenburg, Sweden. Since 2013 she has been leading the department with 60+ Medicinal Chemists supporting the portfolio across multiple chemical modalities. Malin received her PhD at the Gothenburg University in 1999 in organic chemistry. After post-doctoral studies on metal catalyzed asymmetric oxidation at The Scripps Research Institute in California with Prof. Barry Sharpless, she joined AstraZeneca as a scientist and has subsequently held various leadership roles. Dr. Lemurell is an author of multiple publications and patents, including patents related to eg. Odevixibat and AZD5718 (Phase II). Her current interests include drug design across small molecules and New Modalities, targeted drug delivery, drugging RNA structure using small molecules and to develop drug hunters of the future.
Dr. John Macor earned his B.S. degree from the University of Notre Dame in 1982 doing undergraduate research with Professor Marvin Miller, and earned his Ph.D. degree in organic chemistry at Princeton University with Professor E. C. Taylor in 1986. Dr. Macor’s professional career has spanned five different decades and four different pharmaceutical companies with significant contributions at each of them. He began his career at Pfizer (Groton, CT) in 1986, and he moved to Astra Arcus (Rochester, NY) in 1994. In 1997 he joined Bristol-Myers Squibb (Princeton, NJ), and in 2016, he accepted the role as Global Head of Integrated Drug Discovery for Sanofi with groups in Paris, Frankfurt and Waltham, MA. Dr. Macor is a co-inventor of Relpax® (eletriptan) and Nurtec® (rimegepant), both for the treatment of migraine with different mechanisms of action. Dr. Macor is also a co-inventor of rizegepant (migraine, Ph 2/3), sparsentan (focal segmental glomerulosclerosis, Ph 3) and LX-9211 (neuropathic pain, Ph 1b). A full biography for Dr. Macor can be found at https://www.acsmedchem.org/?nd=Macor.
THE PROUS INSTITUTE-OVERTON AND MEYER AWARD FOR NEW TECHNOLOGIES IN DRUG DISCOVERY Award Lecture
Prof. Gisbert SCHNEIDER
ETH ZÜRICH, Zürich, Switzerland
THE KLAUS GROHE AWARD Award Lecture
Prof. Stephan A. SIEBER
TECHNICAL UNIVERSITY MUNICH, Garching, Germany Read more
Phil Baran was born in 1977 in Denville, New Jersey. He received his B.S. in chemistry from NYU in 1997, his Ph.D. at The Scripps Research Institute in 2001, and from 2001-2003 he was an NIH-postdoctoral fellow at Harvard. His independent career began at Scripps in the summer of 2003. He currently holds the Darlene Shiley Chair in Chemistry. Phil has published over 180 scientific articles and has been the recipient of several ACS awards such as the Corey (2015), Pure Chemistry (2010), Fresenius (2006), and Nobel Laureate Signature (2003), and several international distinctions such as the Hirata Gold Medal and Mukaiyama Prize (Japan), the RSC award in Synthesis (UK), and the Sackler Prize (Israel). In 2013 he was named a MacArthur Foundation Fellow, in 2015 he was elected to the American Academy of Arts and Sciences, in 2016 he was awarded the Blavatnik National Award, and most recently, in 2017, he was elected to the National Academy of Sciences, USA. He has delivered hundreds of lectures around the world and consults for numerous companies such as Bristol-Myers Squibb (since late 2005), Boehringer-Ingelheim, AstraZeneca, DuPont and TEVA, and is a scientific advisory board member for Eisai, Abide, and AsymChem. In 2016 he was appointed as an Associate Editor for the Journal of the American Chemical Society. He co-founded Sirenas Marine Discovery (2012) and Vividion Therapeutics (2016) and in 2013 he co-authored The Portable Chemist’s Consultant, an interactive book published on the iBooks store along with his graduate class in Heterocyclic Chemistry (viewable for free by anyone on iTunes University). Outside of the lab, Phil enjoys spending time with his wife Ana and three young children (Lucia, Leah, and Manuel).
Title of talk be announced
Dr Karin BRINER
NOVARTIS, Cambridge, United States
Medicinal Chemistry: More than Ever
Dr Jean-Paul CLOZEL
IDORSIA PHARMACEUTICALS LTD, Allschwil, Switzerland Read more
Dr Jean-Paul CLOZEL
Jean-Paul Clozel is a cardiologist educated in France, with further training in pharmacology and physiology at the University of Montreal, Canada, and the University of California, San Francisco. After eleven years as a clinician, he decided to move to applied research. During his 12 years at F. Hoffmann-La Roche Ltd, he was responsible for the selection of the first T-channel blocker. He also participated in the characterization of renin inhibitors as well as several endothelin receptor antagonists such as bosentan and clazosentan. Overall, the group he was heading discovered seven compounds that entered clinical trials.
During his 25-year-career in cardiology, he has published widely in peer-reviewed medical and scientific journals. At the same time, his passion has remained unchanged: being involved as closely as possible in bringing innovative medicine to "his" patients. He has developed various, novel experimental models allowing the differentiation of these drugs, work honored with the 1997 Hoffmann-La Roche Research Prize. In 2007 he was nominated professor at the Collège de France in Paris, France (Chair of Technical Innovation).
At the end of 1997, Jean-Paul founded Actelion, together with his wife, Martine, and work colleagues and friends Walter Fischli, Thomas Widmann and André J. Mueller. First mainly focusing on Research and Development, he became CEO of the company to bring Actelion to the public in April 2000.
With the sale of Actelion to Johnson & Johnson in June 2017, the drug discovery and early clinical pipeline business was demerged and Idorsia was established. Idorsia, a new biopharmaceutical company, is specialized in the discovery and development of small molecules to provide innovative therapeutic options. Jean-Paul retains his role as CEO.
Targeting Protein Scaffolding Function in Kinases
Prof. Stefan KNAPP
GOETHE UNIVERSITY FRANKFURT, Frankfurt am Main, Germany Read more
Prof. Stefan KNAPP
Prof Stefan Knapp studied Chemistry at the University of Marburg (Germany) and at the University of Illinois. He did his PhD in protein crystallography at the Karolinska Institute in Stockholm. In 1999, he joined the Pharmacia and left the company in 2004 to set up a group at the Structural Genomics Consortium at Oxford University. From 2008 to 2015 he was a Professor of Structural Biology at Oxford University (UK) and director for Chemical Biology at the Target Discovery Institute. He joined Frankfurt University in 2015 as a Professor of Pharmaceutical Chemistry. Since 2017 he is the CSO of the SGC node at the Goethe-University Frankfurt. His research interests are the rational design of selective kinase inhibitors and inhibitors of protein interactions modules that function as reader domains of the epigenetic code.
The Design, Synthesis and Optimization of αvβ6 Antagonists as Potential Idiopathic Pulmonary Fibrosis Agents
Dr Niall ANDERSON
GLAXOSMITHKLINE, Hertfordshire, United Kingdom Read more
Dr Niall ANDERSON
Niall received his masters degree in medicinal chemistry from the University of Strathclyde, Glasgow, Scotland and subsequently joined GlaxoSmithKline’s Discovery Chemistry group in Stevenage, England in 2006. From there, Niall gained experience across multiple phases of drug discovery throughout GSK from hit identification to late stage lead optimisation and targetted protein degradation. In 2014 Niall gained his PhD in a collaborative programme between GSK and the University of Strathclyde on a project entitled “The design, synthesis and optimisation αvβ6 antagonists as potential idiopathic pulmonary fibrosis agents”, a project that led to the identification of clinical candidate GSK3008348A. Niall is a named inventor on 11 patent applications and has authored 11 scientific publications.
Innovative DNA-based Asymmetric Catalysis
Dr Stellios ARSENIYADIS
QUEEN MARY UNIVERSITY OF LONDON, London, United Kingdom Read more
Dr Stellios ARSENIYADIS
Stellios Arseniyadis did his PhD under the guidance of Dr Charles Mioskowski at the University of Strasbourg (France). In 2001, he joined Rhodia Chirex Inc. in Boston (USA) where he worked on various palladium- and copper-catalyzed aryl bond forming processes in collaboration with Pr Stephen L. Buchwald from MIT. After a first postdoc with Pr. Alan C. Spivey at Imperial College London (UK) working in the field of asymmetric organocatalysis, he joined Pr. K. C. Nicolaou's group at The Scripps Research Institute in La Jolla (USA) where he was involved in the synthesis of new epothilone B analogues and on the total synthesis of vannusal A. In 2005, he was appointed a permanent CNRS researcher position back in France and was promoted to Director in 2015. The same year, he accepted a Reader position at Queen Mary University of London (UK). His group is mainly interested in developing new synthetic tools and applying them to the synthesis of biologically active frameworks - https://arseniyadislab.sbcs.qmul.ac.uk
Chemical Biology of Antibody Conjugates and Natural Products
Prof. Gonçalo BERNARDES
UNIVERSITY OF CAMBRIDGE, Cambridge, United Kingdom Read more
After completing his D.Phil. in 2008 at the University of Oxford, U.K., he undertook postdoctoral work at the Max-Planck Institute of Colloids and Interfaces, Germany, and the ETH Zürich, Switzerland, and worked as a Group Leader at Alfama Lda in Portugal. He started his independent research career in 2013 at the University of Cambridge as a Royal Society University Research Fellow. In 2018 he was appointed University Lecturer (Tenured) and recently has been promoted to Reader (Associate Professor). Gonçalo is the recipient of two European Research Council grants; a starting grant and a proof-of-concept grant, and was awarded the Harrison–Meldola Memorial Prize in 2016 and the MedChemComm Emerging Investigator Lectureship in 2018, both from the Royal Society of Chemistry. His research group interests focus on the use of chemistry principles to tackle challenging biological problems for understanding and fight cancer.
Omics-Based Development of Nanomedicines for Safe and Effective Drug Delivery in Cancer
Erem Bilensoy is a full Professor of Pharmaceutical Technology at Hacettepe University Faculty of Pharmacy in Ankara. She has completed her double PhD in Universite Paris-Sud and Hacettepe University in 2002. She served as EUFEPS President between 2015-2019 and is member of FIP Board of Pharmaceutical Sciences and Vice Chair of FIP SIG on Drug Delivery and Manufacturing. Her current research interests include targeted nanoparticles in cancer therapy, cholesterol-targeted nanoparticles to overcome multidrug drug resistance and enhance cellular delivery, applications of proteomics, metabolomics and lipidomics to develop nanomedicines, cationic nanoparticles and their mucosal/oral applications, cyclodextrin-based drug delivery, inkjet and 3D printed drug delivery systems.
Drugging RNA Modifying Enzymes
Dr Wesley BLACKABY
STORM THERAPEUTICS, Cambridge, United Kingdom Read more
Dr Wesley BLACKABY
Wesley joined Storm Therapeutics as VP of Chemistry in March 2017 and is responsible for all chemistry-related activities. Wesley began his industrial career within process chemistry at Glaxo-Wellcome in Dartford before moving to Merck Sharpe and Dohme (MSD) in 1996. At MSD, Wesley worked on several programmes which reached clinical trials for schizophrenia and anxiety disorders. On leaving MSD in 2006 he joined BioFocus, part of the Galapagos group, advancing in project leadership roles culminating as Senior Director in Medicinal Chemistry, and was responsible for maintaining large multidisciplinary collaborations, overseeing the delivery of multiple drug discovery projects and pre-clinical candidates. Wesley has extensive experience across a wide range of therapeutic areas and drug target classes in lead identification, lead optimisation and candidate nomination. Wesley completed his PhD studies under the joint supervision of Prof. Chris McGuigan (University College Cardiff) and Prof. George Attard (University of Southampton).
Utilization of Fe/α-Ketoglutarate-Dependent Enzymes for C-H Functionalization
Prof. Rebecca BULLER
ZHAW SCHOOL OF LIFE SCIENCES AND FACILITY MANAGEMENT, Wädenswil, Switzerland Read more
Prof. Rebecca BULLER
Rebecca Buller is Professor for Chemical and Biotechnological Methods, Systems and Processes at the Zurich University of Applied Sciences (ZHAW) and leads the Swiss Competence Center for Biocatalysis (CCBIO). Prior to joining the ZHAW in 2015, she developed several industrial biocatalytic processes in her function as laboratory head and project manager at Firmenich SA, a flavor and fragrance company. Rebecca studied chemistry at the Westfälische Wilhems-Universität Münster and at UC Santa Barbara and holds a PhD degree from the Institute of Chemistry and Applied Biosciences at ETH Zurich. Her research interests include the expansion of the biocatalytic toolbox by sourcing and engineering enzymes for synthetic applications.
Recent Developments in Strategies and Tactics Towards Complex Secondary Metabolites
Prof. Erick M. Carreira obtained a B.S. degree in 1984 from the University of Illinois at Urbana- Champaign under the supervision of Scott E. Denmark and a Ph.D. degree in 1990 from Harvard University under the supervision of David A. Evans. After carrying out postdoctoral work with Peter Dervan at the California Institute of Technology through late 1992, he joined the faculty at the same institution as an assistant professor of chemistry and subsequently was promoted to the rank of associate professor of chemistry in the Spring of 1996, and full professor in Spring 1997. Since September 1998, he has been professor of chemistry at the ETH Zürich in the Institute of Organic Chemistry. Since 2011, he has been also been a Member of the Competence Center for Systems Physiology and Metabolic Diseases at ETH-Zürich.
Carreira has authored over 340 publications and 36 patents. He has mentored in his laboratory 140 undergraduates, 100 doctoral students, and 79 post-doctoral associates. He has been associate editor with Organic Letters, Thieme Verlag (Synfacts and Synthesis), and Organic Synthesis. As of January 2019 he was assigned the role of Editor-in-Chief for Organic Letters. Together with colleagues at ETH Zurich he has co-founded three companies: Lipideon, SpiroChem, and Glycemicon. He is a consultant for companies in North America, Europe, Switzerland, the United Kingdom, Asia, and Africa.
Title of talk to be confirmed
Dr Paola CASTALDI
LIFEMINE THERAPEUTICS, Cambridge, United States Read more
Dr Paola CASTALDI
Paola Castaldi is the global Head of Chemical Biology & Proteomics at AstraZeneca. Her team is focused on supporting drug discovery programs across all therapeutics areas using state of the art technologies with emphasis on target ID, MOA, and off-target determination. Paola played a critical role to the establishment of the Mass Spectrometry Boston Hub, the therapeutic protein degradation platform, and the multi-omics initiative. Before AstraZeneca, Paola was a key contributor of the Chemical Genetics group at Sanofi Oncology, Cambridge, MA with a focus on phenotypic drug discovery projects for the Wnt and KRAS oncogenic pathways. Prior to Sanofi Paola was at Makoto Life Sciences, where she was responsible for the chemistry strategies towards the identification of the PRPK/TPRKB complex as validated multiple myeloma targets of IMiDs. Paola Castaldi completed graduate research studies at Imperial College London, UK and postdoctoral studies at UCSD and Boston University.
Bernd Clement was Professor of Pharmaceutical (Medicinal) Chemistry (C4 Chair) and Director of the Pharmaceutical Institute, University of Kiel, Germany and is now a Professor emeritus at the same institute and still active in research and teaching.
His main research interests include all aspects of drug metabolism in particular of nitrogen containing functional groups (amidines, guanidines and their N-oxygenated derivatives) focusing on novel metabolic pathways and on prodrugs. His basic research resulted in prodrug principles for amidines further developed in partnership with industry and patent funds. He discovered a new human drug metabolism enzyme, called mARC, capable of transforming several N-oxygenated groups
He is a pharmacist and chemist by training and received his Ph.D. and "Habilitation" in Pharmaceutical (Medicinal) Chemistry.
Exploring Chemical Reactivity with an AI-Driven Chemputer
Prof. Leroy CRONIN
UNIVERSITY OF GLASGOW, Glasgow, United Kingdom Read more
Prof. Leroy CRONIN
Leroy (Lee) Cronin FRSE was born in the UK in 1973 was appointed to be Regius Professor of Chemistry in Glasgow in 2013 after being a professor (2009 & 2006) and reader in Glasgow since 2002. Between 2000-2002 he was a lecturer at the University of Birmingham. Alexander von Humboldt research fellow (Uni. of Bielefeld); 1997-1999: Research fellow (Uni. of Edinburgh); 1997: Ph.D. Bio-Inorganic Chemistry, Uni. of York; 1994 BSc. Chemistry, First Class, Uni. of York. Prizes include 2019 Japan Society of Coordination Chemistry International Prize, 2018 ACS Inorganic Lectureship, 2018 RSC Interdisciplinary Prize, 2015 RSC Tilden Prize, 2013 BP/RSE Hutton Prize, 2012 RSC Corday Morgan, 2011, Election to the Royal Society of Edinburgh in 2009. His research has four main aims 1) the construction of an artificial life form / work out how inorganic chemistry transitioned to biology / searching for new life forms; 2) the digitization of chemistry; and 3) the use of artificial intelligence in chemistry including the construction of ‘wet’ chemical computers; 4) The exploration of complexity and information in chemistry. He runs a team of around 60 people funded by grants from the UK EPSRC, US DARPA, Templeton, Google, BAe, JM and is developing both ‘open-source’ as well as commercial chemputers. See www.chemify.org
Inhaled New Modalities in Respiratory Disease: Past, Present, Future
Werngard Czechtizky is Head of Medicinal Chemistry for Respiratory, Inflammation and Autoimmunity (RIA) at AstraZeneca in Gothenburg, Sweden. She has a track record of delivery of clinical candidates and lead compounds across several therapeutic areas (CV, Diabetes, Pain, CNS, Inflammation and Respiratory). Werngard has continuously implemented state of the art technologies into Medicinal Chemistry. These include e.g. efficient integration of machine learning methods into drug discovery projects, setup of New Modalities Medicinal Chemistry capabilities, implementation of automated synthesis, purification and analytics facilities and efficient integration of compound synthesis with physchem & eADME profiling to accelerate DMTA cycles. Werngard is part of AZ’s Global Chemistry Council, serves on scientific advisory boards of journals and conferences, and is co-/author of ca 80 publications and patents. She has studied at the Technical University of Graz, Austria, received a PhD from ETH Zürich and a postdoctoral training at Harvard University. Before joining AZ in 2017, she has been Head of Chemistry at Sanofi Frankfurt, Germany.
Therapies for Gram-Negative Bacterial Infections: New Approaches and Further Generations of Existing Series
Dr Mike DAWSON
MIKE DAWSON ANTIMICROBIAL RESEARCH CONSULTANCY LTD., Stevenage, United Kingdom Read more
Dr Mike DAWSON
After gaining a degree in Natural Sciences (Biochemistry) at the University of Cambridge and a PhD in Microbial Physiology at the University of Leicester, Mike entered the pharmaceutical industry with Glaxo in 1981. After 20 years in natural product research with Glaxo and subsequently GlaxoWellcome and GSK, Mike moved into the biotech sector as a co-founder of Novacta Biosystems, a company developing new antibiotics for poorly served infections. As CSO he led the Company’s C. difficile programme, taking the novel lantibiotic derivative, NVB302, into clinical evaluation. Subsequently as CEO of Cantab Anti-infectives, Mike led the Company’s next generation polymyxin programme until its acquisition by Spero Therapeutics. Mike is now an independent consultant as well as Head of Biology at Oxford Drug Design. He has authored over 60 papers and is an inventor on over 20 patents.
A Chemical Approach to Controlling Cell Fate
Dr Sheng DING
UNIVERSITY OF CALIFORNIA SAN FRANCISCO, San Francisco, United States Read more
Dr Sheng DING
Dr. Sheng Ding is currently the Dean and Bayer Distinguished Professor in the School of Pharmaceutical Sciences, and Director of Institute for Stem Cell Biology and Regenerative Medicine at Tsinghua University. He is also the founding Institute Director of Global Health Drug Discovery Institute in Beijing, a joint venture by Tsinghua University and the Bill & Melinda Gates Foundation. Dr. Ding also holds a joint appointment as William K. Bowes, Jr. Distinguished Investigator at the Gladstone Institutes, and Professor at Department of Pharmaceutical Chemistry, University of California San Francisco. He obtained his B.S. in chemistry with honors from Caltech in 1999, and a Ph.D. in chemistry from The Scripps Research Institute in 2003. Before moving to back to China, Ding was an Assistant Professor and then Associate Professor of Chemistry at Scripps from 2003 to 2011, and then Senior Investigator/Professor at Gladstone/UCSF from 2011 to 2016. Dr. Ding has pioneered on developing and applying innovative chemical approaches to stem cell biology and regeneration, with a focus on discovering and characterizing novel small molecules that can control various cell fate/function, including stem cell maintenance, activation, differentiation and reprogramming in various developmental stages and tissues. Ding has published over 150 research articles, reviews and book chapters, and made several seminal contributions to the stem cell field and drug discovery. Ding is a cofounder of several biotechnology companies.
Novel Molecular Targets for the Treatment of Fibrotis
Prof. Joerg DISTLER
UNIVERSITY OF ERLANGEN–NUREMBERG, Erlangen, Germany Read more
Prof. Joerg DISTLER
Jörg Distler is currently holding a Heisenberg professorship at the Department of Internal Medicine 3 and Institute for Clinical Immunology at the University of Erlangen-Nuremberg in Germany. His clinical focuses are connective tissue diseases and fibrotic diseases. Jörg Distler is heading the outpatient clinic of the Department of Internal Medicine 3. Moreover, he is principal investigators in numerous international clinical trials (investigator-initiated and industry-sponsored). His research focuses on tissue remodeling in inflammatory diseases. He published > 280 Pubmed-listed articles including > 200 original publications including contributions as senior and corresponding author in journals such as Nature, Nature Medicine, Nature Communications, Journal of Experimental Medicine, Journal of Clinical Investigation and PNAS. His work has a strong translational focus: Preclinical work from his group provided the scientific basis for several clinical trials in fibrotic diseases such as systemic sclerosis.
The Discovery of a Novel Inhaled PI3Kd Inhibitor by Lung Retention Optimisation
Montse Erra is the Head of Medicinal Chemistry at Almirall, Barcelona, Spain. In 1999 she started her career in the pharmaceutical industry by joining the Medicinal Chemistry department at Tibotec (Belgium) as junior research scientist working in the field of HIV protease inhibitors. In 2002 she joined Almirall, where she has played a key role in the design and identification of several clinical candidates and their back-ups in different therapeutic areas such as autoimmune diseases, respiratory and dermatology. In 2011 she was nominated as Chemistry Program Leader, since then she has been directing the research activity of three different programs which also culminated in the identification of 3 development candidates and 3 back-up molecules. She is the co-author/inventor of 26 articles, posters and patents. Montse has 20 years’ experience in pharmaceutical discovery and holds a broad knowledge in small molecule based therapeutics by different administration routes (oral, inhaled and topical).
Understanding Immune Cell Interactions via Photocatalysis
Niyi completed his B.Sc. in Chemistry at Obafemi Awolowo University where he conducted undergraduate research under the direction of Professor Craig Obafemi and later moved to the US for graduate studies. He obtained his Masters in 2007 from Tennessee State University and completed two internships at Eli Lilly pharmaceutical company. He continued to the doctoral program at Vanderbilt University, Department of Chemistry and Chemical Biology under the mentorship of Prof. Craig Lindsley.
In 2011, Niyi obtained his doctorate degree and moved to Harvard University as a UNCF/Merck postdoctoral fellow in the lab Prof. Matthew Shair’s laboratories at the Department of Chemistry and Chemical Biology. He joined Pfizer Inc., Groton in 2014, where he was a Principal Scientist with the Inflammation & Immunology-Rare Diseases division in World Wide Medicinal Chemistry. After 3 years at Pfizer, he joined the Molecular Discovery and Chemical Biology group at Merck Exploratory Science Center in Cambridge where he’s a Molecular Discovery and Chemical Biology Scientist and co-leads a team of multidisciplinary scientists that integrates chemistry and biology to study novel mechanistic basis of human diseases to develop new therapeutics.
Discovery and Disclosure of GLPG1205, a First in Class GPR84 Negative Allosteric Modulator in Phase II Clinical Trial
Dr Romain Gosmini is Director of Medicinal Chemistry at Galapagos, Romainville, France. In 1991 he did his PhD in organic synthesis under the guidance of Prof. Jean Normant at the University Paris VI. He completed a postdoctoral fellowship in Geneva with Prof. Peter Kundig.
In 1994 he joined Glaxo where he worked as medicinal chemist and led the chemistry of several programs until 2009.
Just after he started working at Galapagos as Group Leader.
He is Interested in the different phases of DD (HF, H2L, LO until PCC identification) and involved in various projects such as kinases, proteases, GPCRs and phenotypic, new modalities and degraders, DEL Technology, tissue delivery, Photo-probes, chemical biology.
He worked in various disease areas such as cardiovascular, metabolic, inflammation, fibrosis, infectious disease, Cystic Fibrosis, osteoarthritis…
Title of talk to be confirmed
Dr Gerhard HESSLER
SANOFI-AVENTIS DEUTSCHLAND, Frankfurt am Main, Germany
Donald Hilvert obtained his Ph.D. in Chemistry in 1983 from Columbia University. Following postdoctoral work at Rockefeller University, he joined the faculty of the Scripps Research Institute in La Jolla, California in 1986 as an Assistant Professor. He was subsequently promoted to associate Professor in 1989 and full Professor in 1994. In 1995, he was named the Janet and W. Keith Kellogg II Professor of Chemistry and an affiliate of the Skaggs Institute for Chemical Biology at Scripps. Since October 1997, he has been Professor in the Laboratory of Organic Chemistry at the ETH Zurich (Zurich, Switzerland). Professor Hilvert’s research program focuses on understanding how enzymes work and evolve and on mimicking the properties of these remarkable catalysts in the laboratory. These efforts have been recognized by a number of awards, including the Arthur C. Cope Scholar Award from the American Chemical Society, the Pfizer Award in Enzyme Chemistry, the Protein Society Emil Thomas Kaiser Award, and the Ronald Breslow Award for Achievement in Biomimetic Chemistry. He received an honorary doctorate from Uppsala University and is an elected member of the American Academy of Arts and Sciences.
Lectins from Pathogens: From Structural Glycobiology to Antiadhesive Strategies
Dr. Imberty is the Head of the Centre de Recherches sur les Macromolécules Végétales (CERMAV), a CNRS laboratory affiliated with University Grenoble Alpes. CERMAV is a research center of 100 persons devoted to Glycosciences. Her research interests are in the field of structural glycosciences, with main focus on protein receptors for complex carbohydrates. In particular, structural studies of lectins from pathogenic organisms opened strategies to design glyco-derived compounds with anti-infectious properties. She graduated in biology from Ecole Normale Supérieure in Paris. In 1984, she joined the CNRS in Grenoble and did her PhD on starch structure. She started modeling studies of protein-carbohydrate interaction during her post-doc in Toronto. Since 1999 she has a senior research position in CNRS-Grenoble.
AI Assisted and Automated Chemical Synthesis
Prof. Klavs F. JENSEN
MASSACHUSETTS INSTITUTE OF TECHNOLOGY, Cambridge, United States Read more
Prof. Klavs F. JENSEN
Klavs F. Jensen is Warren K. Lewis Professor in Chemical Engineering and Materials Science and Engineering at the Massachusetts Institute of Technology. From 2007- July 2015 he was the Head of the Department of Chemical Engineering. He received his MSc in Chemical Engineering from the Technical University of Denmark (DTU) and his Ph.D. in chemical engineering from the University of Wisconsin-Madison. His research interests include on-demand multistep synthesis, methods for automated synthesis, and machine learning techniques for chemical synthesis and interpreting large chemical data sets. He is a co-director of MIT's Pharma AI consortium that aims to bring machine learning into pharmaceutical discovery and development workflows.
Discovery of a Novel Class of Small Molecule Dengue Virus Inhibitors
Tim Jonckers obtained his Ph. D in Organic chemistry from the University of Antwerp, Belgium in 2002. Currently, he is Scientific Director, Discovery Chemistry at Janssen Pharmaceutica, Beerse Belgium. His main activities are directed towards finding novel small molecule inhibitors useful for the treatment of various infectious diseases. His scientific work has culminated in co-inventorship on 51 patent applications and co-authorship on 31 publications in peer reviewed journals. During his free time, he likes spending time with his family, playing tennis, and riding his bicycle.
Discovery of M3258, a Potent, Selective and Orally Efficacious Amino-Boronic Acid Based LMP7 Inhibitor for the Treatment of Multiple Myeloma
Dr. Markus Klein is a Principal Scientist in the Department of Medicinal Chemistry at Merck Healthcare KGaA, Darmstadt, Germany. He studied chemistry and theology at Philipps University, Marburg and Heriott Watt University, Edinburgh, and received his PhD in Organic Chemistry under the supervision of Professor Gernot Boche. Prior to moving into drug discovery in 2005, he completed a postdoctoral fellowship in liquid crystal research at Merck KGaA. He is involved in teaching pharmacy students in Organic Chemistry. Over the past years his research has focused on the identification and development of small molecules on various target classes in oncology. In the immunoproteasome inhibitor project, he was leading the design and optimization of M3258 which entered clinical studies in 2019.
Discovery of AZD4831: -a Mechanism-Based, Covalent Inhibitor of Myeloperoxidase
John Liddle is currently Director of Medicinal Chemistry within Cardiovascular, Renal and Metabolic Diseases at AstraZeneca in Gothenburg, Sweden. Prior to joining AstraZeneca in 2019, he was Senior Director in Discovery Partnerships with Academia (DPAc) at GSK. Medicinal chemistry expert with over 20 years of experience within the pharmaceutical industry. Accomplished drug discovery project leader, spanning 15 years, delivering multiple development candidate molecules across various therapeutic areas, biological target classes and routes of administration. Graduated with BSc in chemistry and PhD in synthetic organic chemistry from the University of Manchester, UK.
Living in the World of RNA Therapeutics using Biomimetic Chemistry
Dr Mano MANOHARAN
ALNYLAM PHARMACEUTICALS, Cambridge, United States Read more
Dr Mano MANOHARAN
Dr. Muthiah (Mano) Manoharan serves as the Senior Vice President of Drug Innovation, a Scientific Advisory Board Member, and Distinguished Research Scientist at Alnylam Pharmaceuticals, Cambridge, Massachusetts, USA. He and his team pioneered the discovery and development of the chemical modifications and delivery platforms (Lipid Nanoparticles and GalNAc Conjugates) that make RNA interference-based human therapeutics possible. This work led to the approval of four RNAi therapeutics: ONPATTRO® (patisiran, 2018), GIVLAARI® (givosiran, 2019), OXLUMO® (lumasiran, 2020) and LEQVIO®* (inclisiran, 2020).
Dr. Manoharan received his B.Sc. and M.Sc. degrees in chemistry at the American College, Madurai, India. He earned his Ph.D. in chemistry (with Professor Ernest L. Eliel) at the University of North Carolina, Chapel Hill and carried out post-doctoral research (with Professor John A.Gerlt) in the field of oligonucleotide chemistry at Yale University and at the University of Maryland. Dr. Manoharan is the winner of the Lifetime Achievement Award of the Oligonucleotide Therapeutics Society (2019) and the M. L. Wolfrom Award from the American Chemical Society (2007).
Tethered Peptide Macrocycles, a Novel Antibiotic Class Targeting Acinetobacter Baumannii
Dr Patrizio MATTEI
ROCHE INNOVATION CENTER BASEL, Basel, Switzerland Read more
Dr Patrizio MATTEI
Dr. Patrizio Mattei is an Expert Scientist, Medicinal Chemistry at the Roche Innovation Center Basel, Pharma Research & Early Development (pRED).
His research interests have been mainly devoted to the areas of vascular and metabolic diseases, ophthalmology, and more recently antibiotics, contributing to 6 molecules in human clinical trials (e. g., carmegliptin, a DPP-IV inhibitor for the treatment of diabetes). He is a co-inventor in more than 60 patent applications and has co-authored 18 peer-reviewed articles in the field of drug discovery.
Before joining Roche in 1999, he earned a Doctor of Sciences degree from the ETH Zürich and was a postdoctoral research fellow at The Scripps Research Institute in La Jolla, California.
Neladenoson Bialanate Hydrochloride: A Prodrug of a Partial Adenosine A1 Receptor Agonist
Daniel Meibom received his PhD degree in Organic Chemistry under the supervision of Professor Ekkehard Winterfeldt at the University of Hannover. In 2001 he joined Bayer working on combinatorial chemistry, then quickly moved on to medicinal chemistry projects in therapeutic areas like CNS and antibacterials. From 2007-2013 he was responsible for the chemical optimization of several medicinal chemistry projects in the cardiovascular field. Since 2014 he is heading cardiovascular lead optimization projects as a senior scientist. Besides drug design, his is interested in IT tools for medicinal chemists und laboratory safety.
Discovery of Entrectinib: a Potent and Brain-Penetrant Inhibitor of TRKs, ROS1 and ALK Oncogenic Kinases
Dr Maria MENICHINCHERI
NERVIANO MEDICAL SCIENCES, Nerviano, Italy Read more
Dr Maria MENICHINCHERI
Dr Maria Menichincheri work for Nerviano Medical Sciences Srl, a company strongly committed to the identification of novel drugs for cancer treatment, and she is in charge of the Chemistry Department. She has a scientific background in synthetic organic chemistry and a solid experience in medicinal chemistry. As a chemistry project leader she has worked on several research projects, particularly in the kinase field, aimed at the identification of a Product Candidate suitable for development, as exemplified by the successful story of Entrectinib. She has a Master of Science in Chemistry from Università di Roma “La Sapienza” and a two years Postdoctoral degree on Synthetic Chemistry from Università Statale di Milano. She spent one year as a Postdoctoral Fellow at “Massachusetts Institute of Technology” Cambridge (MA) working on the synthesis of allene and cyclopropylidene derivatives.
Bioorganic Synthesis – Adventures at the Chemistry/Biology Interface
Prof. Marko D. MIHOVILOVIC
VIENNA UNIVERSITY OF TECHNOLOGY, Vienna, Austria Read more
Prof. Marko D. MIHOVILOVIC
Marko D. Mihovilovic graduated in technical chemistry at TU Wien in 1993, also receiving his doctorate from the same university in 1996, in the field of organic synthetic chemistry. Post-doc placements as an Erwin Schrödinger fellow then followed at the University of New Brunswick (Canada) and the University of Florida (USA), in the fields of biocatalysis and molecular biology. Returning to the Institute of Applied Synthetic Chemistry (IAS) at TU Wien, he set up his own research group in 1999. He completed his habilitation in 2003 in bio-organic chemistry and was appointed Associate Professor in 2004. In 2014 he became Full Professor and Chair in Bioorganic Synthetic Chemistry at IAS. Marko Mihovilovic has been Head of the Institute of Applied Synthetic Chemistry with some 120 researchers and staff from 2013-2019 and was appointed as Dean of the Faculty for Technical Chemistry at TU Wien in 2020.
Herbert Nar is Director of the Structural Research Group at the Boehringer Ingelheim German Research Centre Biberach. The group comprises units for protein expression and purification, biophysics of ligand binding, NMR, protein crystallography and cryo-EM. He graduated from the Technical University Munich in Chemistry and obtained his Ph.D. from the same institute. After postdoctoral work with Robert Huber at the Max-Planck-Institute für Biochemie, Martinsried, Germany, he joined Boehringer Ingelheim to establish a protein crystallography laboratory, before taking over responsibility for the Structural Research Group. He is author or co-author of >80 publications and >50 patents and was involved in numerous projects yielding clinical candidate chemical matter.
Antibody-Drug Conjugates (ADCs) and Small Molecule-Drug Conjugates (SMDCs): a Direct Comparison
Dario Neri was born in Rome on 1 May 1963, but grew up in Siena (Italy). He studied Chemistry at the Scuola Normale Superiore of Pisa and earned a PhD in Chemistry at the Swiss Federal Institute of Technology (ETH Zürich), under the supervision of Professor Kurt Wüthrich (Nobel Prize Chemistry 2002). After a post-doctoral research internship (1992-1996) at the Medical Research Council Centre in Cambridge (UK), under the supervision of Sir Gregory Winter (Nobel Prize Chemistry 2018), he became professor at ETH Zürich in 1996.
Dario Neri is currently Full Professor of Biomacromolecules at the Department of Chemistry and Applied Biosciences, ETH Zürich. The research of the Neri group focuses on the engineering of therapeutic antibodies for the therapy of cancer and other angiogenesis-related disorders and on the development of DNA-encoded chemical libraries.
Dario Neri is a co-founder of Philogen (www.philogen.com), a Swiss-Italian biotech company which has brought various antibody products into multicenter clinical trials for the treatment of cancer and of chronic inflammatory conditions.
Dario Neri has published ~400 articles in peer-reviewed scientific journals. He is the recipient of the ISOBM Abbott Prize 2000, of the Amgen-Dompe’ Biotec Award 2000, of the Mangia d’Oro 2001, of the Prous Award 2006 of the European Federation of Medicinal Chemistry, of the Robert-Wenner-Prize 2007 of the Swiss Cancer League, of the SWISS BRIDGE Award 2008, of the Prix Mentzer of the French Medicinal Chemistry Society in 2011, of the Phoenix Prize 2014, of an ERC Advanced Grant in 2015 and of the 6th World ADC Award in 2019.
MAP4K4 Inhibitors for the Treatment of Myocardial Infarction
Dr Gary NEWTON
THE INSTITUTE OF CANCER RESEARCH, London , United Kingdom Read more
Dr Gary NEWTON
Dr Gary Newton, recently joined the Institute of Cancer Research, as a Team Leader in medicinal chemistry. Prior to this role he was a Group Leader in medicinal chemistry at Domainex working in a range of therapeutic areas, including inflammation, cardiovascular disease and oncology. During this time he led a number of multi-disciplinary teams to discover pre-clinical candidates on behalf of Domainex’s clients. One such collaboration with Prof. Michael Schneider of Imperial College has led to the discovery of MAP4K4 inhibitors suitable for the treatment of myocardial infarction. Dr Newton studied chemistry at the University of Sheffield before completing his PhD in the asymmetric synthesis of tropane alkaloids with Prof. Varinder Aggarwal. After which time he joined OSI Pharmaceuticals working in oncology.
Design, Synthesis, and Development of Lectin Ligand Mimetics
Ulf Nilsson obtained his PhD at Lund University 1995 working with oligosaccharide synthesis under the supervision of professor Göran Magnusson. He did post-doctoral studies 1995-1997 at University of Alberta, Canada, with professor Ole Hindsgaul developing methods for combinatorial carbohydrate chemistry. He initiated his independent research career at Lund University 1998 as an assistant professor and was promoted full professor in 2009. Research interests are on molecular recognition studies in biological systems and in artificial model systems, biology and medicinal chemistry of galectins, sialic acid transport proteins, and DHODH enzymes, and chemistry at brain-machine interfaces.
Sensing Enzymatic Reactions with Quantum Dots
Dr Valle PALOMO
CENTRO DE INVESTIGACIONES BIOLÓGICAS-CSIC, Madrid, Spain Read more
Dr Valle PALOMO
Valle Palomo is a Junior Leader researcher at the Centre for Biological Research CSIC in Madrid. She studied Chemistry and obtained her PhD from the Autónoma University of Madrid in 2012 in Organic Chemistry. She performed a postdoctoral research stay at The Scripps Research Institute with Prof. Dawson from 2013 to 2016. In 2018 she started her own group focused on Medicinal Chemistry, Chemical Biology and Nanotechnology. Her lab focuses on the understanding of neurodegenerative diseases, especially amyotrophic lateral sclerosis, and in the discovery of novel agents for its treatment.
Drugging mRNA with Drug-like Small Molecules
Dr Jennifer PETTER
ARRAKIS THERAPEUTICS, Waltham, United States Read more
Dr Jennifer PETTER
Dr. Jennifer Petter is the Founder and CSO of Arrakis Therapeutics. Previously she was Vice President of Chemistry at Celgene, Vice President of Drug Discovery at Avila Therapeutics, Vice President of Research at Mersana Therapeutics, Director of Small Molecule Drug Discovery at Biogen, Section Head in Oncology Chemistry at Sandoz/Novartis, and Assistant Professor of Chemistry at the University of Pittsburgh. Dr. Petter graduated from Dartmouth College with an AB in chemistry, earned her PhD in organic chemistry at Duke University with Ned Porter, and was a post-doctoral fellow in Ron Breslow’s group at Columbia University. She has ushered multiple compounds into clinic trials for the treatment of cancer, cardiovascular disease, autoimmune disorders, and sepsis.
After her PhD at the University of Padua (Italy), Paola Picotti joined as a postdoc the group of Ruedi Aebersold at ETH Zurich, where she developed targeted proteomic technologies based on mass spectrometry. In 2011, she was appointed Assistant Professor at the Institute of Biochemistry of ETHZ and in 2017 tenured Associate Professor at the Institute of Molecular Systems Biology at ETHZ. Major contributions of the Picotti group include the development of structural proteomics technologies to probe in situ protein structural changes, the characterization of the determinants of proteome thermostability, the large-scale identification of protein small molecule interactions and the discovery of regulators of toxic proteins involved in Parkinson’s disease. Dr. Picotti was awarded the Latsis Prize, the Cotter Award of the US HUPO, the SGMS award, the EMBO Young Investigator Award, the Friedrich Miescher Award, the Juan-Pablo Albar award of the European Proteome Association, an ERC Starting grant, an ERC Consolidator Grant and the EMBO Gold Medal.
Dr. Rademacher earned his BSc in Molecular Biotechnology and MSc in Molecular Life Science at the University of Lübeck. In 2009, he received his doctorate from the same University, where he worked on virus/carbohydrate interactions using NMR spectroscopy under the supervision of Prof. Dr. Thomas Peters (Department of Chemistry). He then underwent postdoctoral training with Prof. Dr. James C. Paulson at The Scripps Research Institute (USA) in the Department of Chemical Physiology, where he entered the field of glycoimmunology. Since December 2011, Dr. Rademacher is appointed at the Max Planck Institute of Colloids and Interfaces in the Department of Biomolecular Systems, where he became Emmy-Noether Research Group Leader in June 2012. Since 2017, Dr. Rademacher holds an ERC Starting Grant. His research is focused on the development and application of novel molecular probes to understand the role of carbohydrates in immune cell regulation.
Daniel Rauh studied pharmacy at the University of Greifswald and completed his Ph.D. 2003 with Gerhard Klebe in Marburg. After postdoctoral stays with Milton Stubbs in Halle and Kevan Shokat in San Francisco, he became a junior group leader at the Chemical Genomics Centre of the Max Planck Society in Dortmund. Since 2013 he has been a full Professor and Chair of Chemical Biology and Medicinal Chemistry. He is active in the field of chemical oncology, targeting acquired drug resistance. At TU Dortmund University, he heads a research group of 30 scientists and staff whose focus is on early drug discovery. Daniel is the founder and coordinator of the Zentrum für integrierte Wirkstoffforschung (ZIW) and the Drug Discovery Hub Dortmund (DDHD) both at TU Dortmund University to translate basic academic research into pharmaceutical application. He also serves as an associate editor for ACS Chemical Biology.
Prodrug Strategies in Medicinal Chemistry
Prof. Jarkko RAUTIO
UNIVERSITY OF EASTERN FINLAND, Kuopio, Finland Read more
Prof. Jarkko RAUTIO
Jarkko Rautio is professor in pharmaceutical chemistry and a vice head at the School of Pharmacy, University of Eastern Finland. He graduated from the University of Kuopio and did his post doc at the University of Maryland, Baltimore. He has also spent two years at GSK, North Carolina, as a visiting scientist.
His research focuses on the chemistry-based methods, especially prodrugs, to overcome drug delivery liabilities of problematic drugs. Much of the research is currently focusing on exploiting two of the body’s natural mechanisms for transporting nutrients, the LAT1 and GLUT1 proteins, for targeted drug delivery across the blood-brain barrier and cancer cells that express these transporters.
The Role of Cryo-EM in Fragment-Based Drug Discovery
Dr Judith REEKS
ASTEX PHARMACEUTICALS, Cambridge, United Kingdom Read more
Dr Judith REEKS
Judith Reeks is a senior research associate in the Molecular Sciences department of Astex Pharmaceuticals. Her main focus is using structural biology for drug discovery. She gained a PhD from the University of St Andrews in the lab of Prof. James Naismith, studying the structural biology of CRISPR-associated proteins. She then moved to the lab of Prof. Martin Noble and Prof. Jane Endicott in the Northern Institute for Cancer Research as a post-doctoral research associate to work on drug discovery projects. She joined Astex in 2015.
Pablo Rivera-Fuentes is assistant professor of chemical biology at EPF Lausanne. His laboratory works on the development of chemical and biological probes to visualize and control biological problems with sub-cellular precision. Prior to his appointment at EPFL, he was an independent group leader at ETH Zurich (2015–2019). His training includes a PhD in chemistry from ETH Zurich (2012), as well as postdoctoral training at MIT and the University of Oxford (2012–2015).
Discovery of Small Molecules to Manipulate Cell Fate in vivo: Towards New Therapies for Degenerative Diseases
Prof. Angela RUSSELL
UNIVERSITY OF OXFORD, Oxford, United Kingdom Read more
Prof. Angela RUSSELL
Angela Russell is Professor of Medicinal Chemistry in the Departments of Chemistry and Pharmacology at the University of Oxford. She gained her MChem degree from the University of Oxford in 2000 and her DPhil in Organic Chemistry in 2004. In 2007 she was awarded a Research Councils’ UK Fellowship in Medicinal Chemistry jointly between the Department of Chemistry and Pharmacology in Oxford. In 2018 she was made Professor of Medicinal Chemistry. Her work lies at the interface of Chemistry, Biology and Medicine and aims to discover new small molecules and mechanisms to manipulate cell fate and translate them into therapeutic agents, particularly for degenerative diseases and cancer.
Discovery of Pecavaptan: A Novel Dual Acting Vasopressin V1a/V2 Receptor Antagonist for the Treatment of Congestive Heart Failure
Dr. Carsten Schmeck, Principal Scientist, BAYER AG, Pharmaceuticals, Medicinal Chemistry Wuppertal
He joined Bayer in 1994, working on projects in the fields of atherosclerosis and lipid disorders, peripheral vascular disease and heart failure. Since 2014, He is working on projects in the field of kidney disease being a team member of the Bayer Evotec kidney research alliance.
For his education, he studied chemistry in Göttingen in Germany, receiving his Ph.D in 1991 from Prof. Dr. U. Groth working on an asymmetric synthesis of non-proteinogenic amino acids and dipeptides. From 1992 to 1994, he joined the group of Prof. Dr. L.S. Hegedus in Fort Collins, Colorado working chiral amino chromium carbene complexes and their use in the synthesis of amino acids.
Augmenting Drug Hunters with Generative Chemistry Models
Dr. Nadine Schneider obtained a BSc and MSc in Bioinformatics from the Saarland University in Germany. She did her PhD in Molecular Modeling in the group of Prof. Dr. Matthias Rarey at the University of Hamburg, Germany. In her PhD she worked on a novel protein-ligand scoring function which was integrated in the commercial modeling software SeeSAR (BioSolveIT GmbH). In 2014 she joined the Novartis Institutes for BioMedical Research (NIBR) in Basel for a postdoc focusing on Cheminformatics and Data Science under supervision of Dr. Gregory Landrum and Dr. Nikolaus Stiefl. Since 2017 she is an investigator in the Computer-Aided Drug Design team in Global Discovery Chemistry in the Novartis Institutes for BioMedical Research, Basel.
Photopharmacology: Towards Light-Controlled Therapy
Dr Wiktor SZYMANSKI
UNIVERSITY OF GRONINGEN, Groningen, The Netherlands Read more
Dr Wiktor SZYMANSKI
Wiktor Szymanski received his PhD degree from The Warsaw University of Technology, Poland, in 2008, working under the supervision of Prof. Ryszard Ostaszewski. He spent two years working on the use of biotransformations in organic chemistry with Prof. Ben L. Feringa and Prof. Dick B. Janssen at the University of Groningen. Since 2010 he has been working on the construction of photoactive protein- peptide- and DNA-bioconjugates and photopharmacology in the Feringa Labs. In 2014, he joined the Department of Radiology, University Medical Center Groningen, where he was appointed in 2015 as tenure track assistant professor and in 2019 as associate professor.
Chemical Probes to Study Lipid Signaling
Dr Mario VAN DER STELT
LEIDEN UNIVERSITY, Leiden, The Netherlands Read more
Dr Mario VAN DER STELT
Mario van der Stelt (1975) is professor and chair of the department of Molecular Physiology of the Leiden University (the Netherlands). He is a medicinal chemist and worked as a project leader for almost 8 years in the pharmaceutical industry (Merck Research Laboratories). He and his group discovered highly selective and peripherally restricted cannabinoid CB2 receptor agonists and the first brain active inhibitors for the biosynthesis of endocannabinoids. His group reported the off-target profile of the FAAH inhibitor BIA 10-2474 that killed a healthy volunteer in a phase 1 clinical trial in France in 2016. Dr. Van der Stelt received for his research the Prix Galien Research for best preclinical drug discovery research in the Netherlands (2017), the Young Investigator Award of the International Cannabinoid Research Society (2017) and a VICI-award from the Netherlands Organisation for Scientific Research (2018). He is elected as a senior investigator of Oncode Institute (2019) and (vice)-chair of the Gordon Research Conference on Cannabinoid Function in the CNS (2021-2023). Multidisciplinary collaboration is key in his research to connect chemistry and biology to discover drug candidates modulating the endocannabinoid system.
Scaffold-Assisted Peptide Cyclizations: Towards Protein Mimics
Prof. Jan VAN MAARSEVEEN
UNIVERSITY OF AMSTERDAM, Amsterdam, The Netherlands Read more
Prof. Jan VAN MAARSEVEEN
Jan van Maarseveen obtained obtained his Ph.D. in 1994 at the University of Nijmegen on the total synthesis of indole alkaloids. From 1994-1999 he joined Solvay-Pharmaceuticals (Weesp, The Netherlands) as a farmacochemist involved in combinatorial druglike molecule library synthesis and as a group leader in a traditional lead optimization program. In november 1999 he moved back to academia as an assistant professor at the University of Amsterdam. Meanwhile, he rose through the ranks and was promoted in 2015 to full professor. His research focusses on the development of methodology to enable the synthesis of small and strained cyclic peptides together with the development of enantioselective catalytic methods with applications in alkaloid synthesis. Currently, the group shifts the research towards covalent scaffold-based methodology development to synthetically disclose the natural lasso peptide series and other mechanically interlocked molecules. Jan is an enthousiastic teacher and obtained several prices of which the “best teacher of the year of the University of Amsterdam in 2012” award is the most prestiguous one. In 2016 he was awarded the Royal Dutch Chemical Society Van Marum Medal for his contributions to chemistry outreach and excellence in teaching.
NLRP3 inflammasome inhibitors for Inflammatory and Neuroinflammatory Disease
Dr Alan WATT
NODTHERA, Little Chesterford, United Kingdom Read more
Dr Alan WATT
Alan has spent 35 years in pharmaceutical and biotech R&D working to discover drugs within the fields of neuroscience, inflammation, metabolism and cancer. Alan was Head of Drug Metabolism at the Merck Neuroscience Research Centre in the UK before establishing and leading the Innate Immunity discovery group at GSK in Philadelphia. Latterly, he had led R&D for a number of biotechs including Cellzome, Trident Biopharma and Bicycle Therapeutics.
Most recently Alan led the formation of start-up biotech NodThera Limited focused on the discovery and development of novel NLRP3 inflammasome inhibitors for inflammatory and neuroinflammatory diseases. He serves as the Chief Scientific Officer where his team have taken a molecule from discovery to first-in-human in just three years. Alan holds a BSc in chemistry, a PhD in drug metabolism and an MBA. He has published over 50 scientific papers in peer-reviewed journals.
Cryo-Electron Microscopy, a New Tool for Drug Discovery at Novartis
Christian Wiesmann is director and the head of the cryo-EM facility at the Novartis Institutes for Biomedical Research in Basel. He is a structural biologist and interested in the structure and function of macromolecules and the characterization of protein interactions with their receptors, Fab fragments, or small molecule ligands with the goal to better understand the mechanism of molecular machines and to facilitate the discovery of new medicines. Christian studied chemistry at the Albert-Ludwigs-University Freiburg, Germany and received his Ph.D. for a project in protein crystallography in 1996. He joined Genentech, Inc. in South San Francisco as a post-doctoral fellow where he investigated growth factors and their complexes before moving to Sunesis Pharmaceuticals, a biotech company developing new technologies for fragment based drug discovery (tethering). In 2002, Christian moved back to Genentech as a structural biologist and in 2009 joined Novartis in Basel as the Head of the structural sciences group in the expertise platform proteases before moving to his current position in 2015.
Chemical Probes to Explore Cancer Biology and Validate Drug Targets
Prof. Paul WORKMAN
INSTITUTE OF CANCER RESEARCH, London, United Kingdom Read more
Prof. Paul WORKMAN
Professor Paul Workman FRS FMedSci FRSC is Chief Executive and President of The Institute of Cancer Research (ICR), London and Harrap Professor of Pharmacology and Therapeutics at ICR. He is the founding Director of the CRUK Convergence Science Centre at ICR and Imperial College. From 1997-2016 Paul was Director of the CRUK Centre for Cancer Therapeutics at ICR. Previously he was head of the cancer biology section at Zeneca Pharmaceuticals (now AstraZeneca) and before that he held academic positions at Leeds University, MRC Clinical Oncology Unit/Cambridge University, Stanford University, CRUK Beatson Laboratories/Glasgow University. Paul is an internationally recognized a leader in the discovery of innovative molecularly targeted cancer drugs and chemical probes, including inhibitors of PI3 kinase, AKT, CDKs, HSP90 and the HSF1 pathway, and is the originator of the widely-used Pharmacologic Audit Trail for biomarker-led drug development. He has won numerous honours and awards for his research. He is a Board Director of the Chemical Probes Portal, Royal Marsden and Storm Therapeutics; was scientific founder of Chroma Therapeutics and Piramed Pharma (acquired by Roche); and is a Science Partner at Nextech.
Development of Fluorinated PET Tracers for Imaging of α1 Receptors in the Brain
Bernhard Wünsch studied Pharmacy at the Ludwig-Maximilians-University in Munich. After finishing the PhD and habilitation in the field of Pharmaceutical and Medicinal Chemistry, in became a professor for Pharmaceutical Chemistry in Freiburg and later in Münster. Currently, he is the director of the Institute of Pharmaceutical and Medicinal Chemistry in Münster. He is working on the development of novel ligands for various receptors such as glutamate, opioid and sigma receptors. Furthermore, he is interested in subtype selective modulation and imaging of ion channels. Since the target proteins have a particular 3D structure, the stereochemistry of the ligands plays a particular role in the projects. Relationships between structure, in particular stereochemistry, and affinity and activity are investigated.
Sheng-Yong Yang, Dr., Professor of the State Key Laboratory of Biotherapy, West China Hospital, Sichuan University (Sichuan, China). Dr. Yang obtained his PhD degree from Sichuan University in 1999. Then, he did his postdoc research in Hongkong University of Science and Technology from 1999-2001. In 2002-2005, he worked in the University of Calgary (Alberta, Canada) as a research scientist. Since 2005, Dr. Yang has been working in the State Key Laboratory of Biotherapy, West China Hospital, Sichuan University. His research interests include computer aided drug discovery (CADD), medicinal chemistry, and small molecule drug R&D against cancer and immunological disease.
Allosteric Modulator Discovery: from Method Development to Applications
Prof. Jian ZHANG
SHANGHAI JIAO TONG UNIVERSITY, Shanghai, China Read more
Prof. Jian ZHANG
Prof. Jian Zhang, Director of Medicinal Bioformatics Center in Shanghai Jiaotong Unversity School of Medicine. In the last ten years, he has made a series of cutting-edge breakthroughs in drug discovery, which were achieved through the development of allosteric drug design methods to identify new anti-cancer drug targets and discover first-in-class lead compounds. The representative works include: development and improvement of allosteric methods based on the induced fit of conformation, and precise identification of anti-cancer drug targets from clinical samples; discovery of first-in-class allosteric modulators for undruggable targets using our developed allosteric methods. He has published more than 150 papers in Nature, Nat Chem Biol, etc. Moreover, the developed allosteric methods from Prof. Zhang have been accessed by more than 60,000 users over 100 countries. More significantly, some of the first-in-class lead compounds developed by Prof. Zhang have been advanced into pre-clinical studies.