Development of Generic G Protein Peptidomimetics Able to Stabilize Active State Gs Protein-Coupled Receptors for Application in Drug Discovery (PL03)
|Prof. Steven BALLET|
(VRIJE UNIVERSITEIT BRUSSEL, Brussels, Belgium)
Dr Steven Ballet completed his PhD at the Vrije Universiteit Brussel (VUB, Brussels, Belgium) in 2007. Directly following his PhD training, Dr Ballet went for a first postdoctoral stay in Australia at the University of Adelaide with Professor Andrew Abell. During this stay he applied ring closing and cross metathesis reactions on amino acid and peptide substrates. As such, dimeric but also ring closed peptide scaffolds could be obtained. More specifically, RCM was used to stabilize ('staple') the helical conformation of alpha and beta peptides. As a second postdoctoral training, Dr Ballet went to the Institut de Recherches Cliniques de Montréal (IRCM, Montreal, Canada) for a specialized training in the opioid peptide field. Together with Prof. Peter W. Schiller, he designed bifunctional opioid ligands with dual MOR/DOR agonist profiles and hybrid opioid/non-opioid multitarget ligands. Since 2010 Dr Ballet is appointed as a faculty member at his alma mater, where he pursues his efforts in the peptide and peptidomimetic field. The main research topics involve injectable peptide hydrogels for sustained release of bioactive peptides, the synthesis of turn/helix/loop mimetics as receptor ligands or PPI modulators, and transition metal-catalyzed derivatization of peptides in aqueous media.Close window
Short Stories in Medicinal Chemistry (PL01)
|Prof. Gilles BERGER|
(ULB, Brussels, Belgium)
Gilles Berger is a Principal Investigator and Associate Professor at the University of Brussels (Université Libre de Bruxelles). He is a chemist and pharmacist with broad interest in organic and theoretical chemistry, drug discovery, biomedical sciences and oncology. He has conducted research in Brussels, Paris, Montreal and Boston; has gathered hands-on experience at the interface of drug design, nanotechnologies, biology and human disease. In recent years, he has developed as a translational scientist, allowing the use of his complementary multi-disciplinary skills toward the advancement of various projects, such as drug discovery and cancer therapy, organocatalysis, theoretical chemistry and halogen bonding. Recent work comprised intracranial immunotherapies for brain cancers.
Dr Berger has received numerous awards and fellowships, such as Fulbright and the Belgian American Educational Foundation, worked as a Fellow of the Belgian Science foundation (FNRS) and received the UCB Young Investigator Award in 2016. He was awarded in 2021 the Andrew Parsa Young Investigator Award from the American Society for Neuro-Oncology, for his work on innate immunity for brain cancer. He has been published in high impact journals, including multiple covers. Besides his appointments in Brussels, he is a Research Associate at MIT.
Dr Berger received his Pharm.D. (magna cum laude) and Ph.D. from the University of Brussels, then worked as a postdoc with Stephen Hanessian (University of Montreal), Stephen Lippard (MIT) and Sean Lawler (Harvard Medical School). In 2021, in was a Visiting Scholar at the Wyss Institute at Harvard (with Prof. David Mooney).
Discovery of Novel Small Molecule Modulators of TNFα Binding and Signalling (PL05)
|Dr Dan BROOKINGS|
(UCB, Slough, United Kingdom)
Dan Brookings is currently a Director of Medicinal Chemistry at UCB Pharma where he has pursued his drug discovery career for the last 21 years. His research interests and projects cover a wide range of target classes from kinases to small molecule modulation of protein/protein interactions in the fields of oncology and immunology. Dan has led project and chemistry teams that have successfully identified 3 clinical candidates and is an inventor on 40 patent applications.Close window
Development of Positive Allosteric Modulators for Glutamate Ionotropic Receptors (PL12)
|Dr Pierre FRANCOTTE|
(ULIÈGE, Liège, Belgium)
Pierre Francotte is a pharmacist (University of Liège) and completed a Mastère in Drug Design at the Ecole Supérieure de Chimie de Lille & University of Lille 2. He worked on the development of AMPA potentiators in collaboration with the industry and obtained his PhD in Biomedical and Pharmaceutical Sciences (University of Liège).
He achieved his postdoc at the University of Copenhagen in Prof. Bente Frølund’s team where he was involved in the development of pharmacological tools targeting the GABAA receptors. After this research stay, he came back in Liège where he is now Assistant Professor in the Lab. of Medicinal Chemistry (Prof. B. Pirotte).
His research interests include the design/synthesis of AMPA/KA modulators but also the optimization of natural products using total synthesis approach.
Interrogating the Lactate Dehydrogenase (LDH) Tetramerization Site with (stapled) Peptides (PL11)
|Prof. Raphaël FREDERICK|
(UCLOUVAIN, Brussels-Woluwe, Belgium)
Prof. Raphaël Frédérick is Chemist by training. After a Master in Drug Design awarded from the University of Lille (France), he performed a PhD in Medicinal chemistry at the University of Namur (UNamur, Belgium), which he obtained in 2006. Thereafter, he joined the team of Prof. Sir Bill Denny at the Auckland Cancer Society Research Center (ACSRC) at the University of Auckland, New Zealand for a 2-year postdoc stay. His research project aimed at discovering novel p110α-PI3 kinase inhibitors for cancer therapy, and led to the identification of several novel small molecule inhibitors, some of them having been evaluated in clinical settings. In 2008, he became a postdoctoral researcher of the F.R.S.-FNRS and then, a F.R.S.-FNRS Research Associate at the University of Namur where he pursued his research in the discovery of new drug candidates in the field of anticancer immunotherapy. His research notably led to the discovery of LM10, the first bioavailable, selective tryptophan-2,3-dioxygenase (TDO2) inhibitor that helped establishing the proof-of-concept of TDO2 inhibition for cancer immunotherapy. In 2013, he was recruited as a Professor of organic and medicinal chemistry at the Université catholique de Louvain (UCLouvain) in Brussels, Belgium, where he is heading the lab of Medicinal Chemistry.
His team comprises ~10 researchers and is active in medicinal chemistry/chemical biology in oncology in two main fields: (1) cancer immunotherapy and (2) tumor metabolism. His strategy involves the discovery and study of novel small molecules targeting enzymes at their active-site, and the development of chemical biology tools to interrogate protein self-assembly.
To date, Prof. Frédérick authored more than 60 peer-reviewed papers and is inventor of 4 patent applications. His research achievements translated in various awards such as the French SCT Award for young investigator in Medicinal Chemistry and the Johnson and Johnson Pharmaceutical Research and Development Award for Young Medicinal Chemists (Dr. Paul Janssen award), Belgium.
Purines and Trypanosomatids – a Neglected Match for New Therapeutics? (PL02)
|Dr Fabian HULPIA|
(JANSSEN, Beerse, Belgium)
Dr Hulpia is a pharmacist by training, and obtained his PhD in Pharmaceutical Sciences in 2018. Currently, he is a postdoctoral fellow at Ghent University in the laboratory for Medicinal Chemistry. One of his research interests include infectious disease drug discovery, more particularly neglected tropical diseases. He has joined Janssen Pharmaceutica in Beerse in March 2021. Close window
Discovery of GLPG2451, a novel Once Daily Potentiator for the Treatment of Cystic Fibrosis (PL04)
|Dr Hans KELGTERMANS|
(GALAPAGOS NV, Mechelen, Belgium)
After obtaining my masters degree in chemistry in 2007, I started a PhD in organic chemistry at the KULeuven in the group of prof. Wim Dehaen. My research focussed mainly on supramolecular chemistry (helicenes) which allowed me to build up a solid basis in terms of heterocyclic chemistry. During this period I was also able to broaden my knowledge in the field by working for 4 months in China in the group of prof. Xi Zhang (Tsinghua University, Beijing). Soon after obtaining my PhD I started working at Galapagos NV as a Scientist on the Cystic Fibrosis program in 2013, and currently I’m working there as Team Leader in the chemistry department.
Step by Step Towards Fully Modified Aptamers | Chemistry Europe Talk (PL08)
|Prof. Eveline LESCRINIER|
(REGA INSTITUTE - KU LEUVEN, Leuven, Belgium)
Eveline Lescrinier (°1972) is a pharmacist (KULeuven, 1995). In 1999, she obtained her PhD in Pharmaceutical Sciences supported by the Flemish Fund for Scientific Research (FWO) with a thesis entitled ‘Structure determination of a HNA-RNA duplex by NMR spectroscopy’.
In 2005, she became responsible for the ‘Impulse Financing’ of the Flemish government to start up an interfaculty center for biomolecular research using NMR spectroscopy at KU Leuven (BioMacs) which launched in 2006. Since then, several students have started a PhD under her supervision. In 2016, she became the head of the laboratory for Medicinal Chemistry of KU Leuven, a multidisciplinary laboratory including bio-organic chemistry, molecular modeling, mass spectrometry, NMR spectroscopy and synthetic biology.
Her general research interest is on structure determination of (modified) oligonucleotides and their interaction with nucleic acid processing enzymes. Obtained results of this fundamental research are applied in the development of folded xenobiotic nucleic acids that bind a specific target (XNA aptamers).
The Confo Therapeutics Technology Platform Enabling GPCR Fragment-Based Drug Discovery (PL06)
|Dr Christel MENET|
(CONFO THERAPEUTICS, Brussels, Belgium)
Christel joined Confo Therapeutics as CSO in 2016. She previously was Director of Medicinal Chemistry at Galapagos from 2014 to 2016. Christel was one of the first chemists at Galapagos in 2005. She is the inventor of filgotinib and under her leadership it was moved forward to pre-clinical development (today filgotinib has successfully completed Phase III for rheumatoid arthritis and is explored in several other indications). She also played a key role in a number of other projects and advanced several compounds into preclinical phase.
Christel started her professional career as a Medicinal Chemist at Evotec in 2002. She then joined Faust Pharmaceuticals in 2004, today called Domain Therapeutics, a biotech company specializing in GPCR drug discovery. She is an inventor on more than 25 patent applications.
Christel completed a PhD in Organic Chemistry at the University of Manchester (UK) in Prof Jonathan Clayden’s lab.
Scaffold Development for the Inhibition of FXIIa, a Promising Therapeutic Target (PL09)
|Dr Lionel POCHET|
(UNAMUR, Namur, Belgium)
Lionel Pochet is an associate professor at the University of Namur. He obtained his Ph.D. degree in Pharmaceutical Sciences at the University of Namur and was Post-Doctoral Fellow at the Laboratory of Biomolecular Analysis at the VU University of Amsterdam.
His research interests include medicinal chemistry in the field of serine proteases inhibitors for antithrombotic therapy and the development of analytical methodologies for biological screening.
Meddling with Cell Death Control: Development of MCL-1 Inhibitors for the Treatment of Cancer (PL10)
|Dr Frederik ROMBOUTS|
(JANSSEN, Beerse, Belgium)
Dr Frederik Rombouts, Senior Principal Scientist at Janssen Pharmaceuticals, did his PhD at K.U. Leuven in the group of Prof. Hoornaert, and a post-doc in the group of Prof. Lubell at the Université de Montréal. He joined the Janssen Discovery Chemistry department in 2003 as synthetic chemist doing combinatorial chemistry. In 2008, he moved to Neuroscience where he first became team leader responsible for hit generation, and later a project leader. In this role he discovered a tau pathology PET imaging tracer and a beta-secretase inhibitor for treating Alzheimer’s Disease. He moved to the oncology field in 2018 where he led the MCL1 inhibitor program until 2020, and is now still project leader in oncology. He is the author of 46 peer-reviewed synthesis and medicinal chemistry publications and co-inventor on 22 patent applications.Close window
UAMC1110 as the Starting Point for a new Generation of Therapeutics and Diagnostics Targeting Fibroblast Activation Protein (FAP) (PL07)
|Prof. Pieter VAN DER VEKEN|
(UANTWERP, Antwerp, Belgium)
Pieter Van der Veken obtained his PhD in 2004 under the supervision of Profs. Koen Augustyns and Achiel Haemers at the University of Antwerp. After a post-doctoral stay in the Netherlands supervised by Prof. Rob Liskamp (University of Utrecht), he returned to Antwerp as a post-doctoral fellow of the Fund for Scientific research (FWO). In 2010 he was appointed professor of Medicinal Chemistry. His research interests are situated in selective chemical tool development (inhibitors, probes) for serine and cysteine proteases, with special attention for the so-called proline-selective peptidases. He also works on methodology development for medicinal chemistry, including so-called ‘target-assisted’ discovery approaches. Finally, he his interested in modulators of pathways involved in cell death/survival, including pyroptosis and autophagy. Both human and microbiological targets are studied.Close window