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Confirmed Speakers
Why Fragments Make Sense and Actually Work
Computational Approaches for Fragment Screening and Fragment Evolution
| Prof. Xavier BARRIL (UNIVERSITY OF BARCELONA & GAIN THERAPEUTICS, Barcelona, Spain) Read more
Xavier Barril is an ICREA Research Professor at Barcelona University’s School of Pharmacy. His research focuses on the discovery of bioactive molecules exploiting unusual mechanisms of action through a combined use of computational and experimental techniques. Prof. Barril received his Ph.D. from the University of Barcelona in 2001 for theoretical studies on the ligand-receptor molecular recognition process. He then joined Vernalis (Cambridge, UK), where he was involved in a range of projects at all stages of the discovery process and in the development of a fragment screening platform. In 2005 he was appointed ICREA Research Professor and rejoined Barcelona University’s. In 2011 he co-founded Minoryx Therapeutics to develop allosteric pharmacological chaperones as new treatments for rare diseases. In 2018 this activity was transferred to Gain Therapeutics where Prof. Barril acts as CSO. Close window
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Biophysical Fragment Based Screening
| Dr Ben DAVIS (VERNALIS RESEARCH, Cambridge, United Kingdom) Read more
Dr Ben Davis is a Research Fellow at Vernalis Research, a biotech company based in Cambridge UK which has been at the forefront of fragment-based approaches since 1998. An NMR spectroscopist and biophysicist by training, his current research focus is applying biophysics and FBLD methods to enable challenging therapeutic targets and systems.
Dr Davis studied for his PhD in protein folding and ligand binding with Professor Alan Fersht at Cambridge University, and then studied small molecule interactions with a range of biomolecules. He has over 20 years’ experience of biophysics in the drug discovery industry. He has contributed to six books over the last decade and is an author on more than thirty scientific publications. He is a frequent speaker at scientific conferences and has been running FBLD training workshops since 2007. Close window
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Applications of FBDD
| Prof. Iwan DE ESCH (VU AMSTERDAM, Amsterdam, The Netherlands) Read more
Iwan de Esch is professor at the Medicinal Chemistry division of VU University Amsterdam. He obtained a Ph.D. in pharmacochemistry and in 1998 became research associate at the Drug Design Group of the University of Cambridge. Dr de Esch is a co-founder of De Novo Pharmaceuticals Ltd (2000) where he worked as a group and project leader. Prof. de Esch returned to academia in 2003. The group focuses on two research lines, G-protein-coupled receptors (GPCRs) and fragment-based lead discovery (FBLD). FBLD is applied on a variety of targets (including GPCRs, kinases, PDEs and PPIs) and also to study ligand-protein binding in terms of affinity, thermodynamics and kinetics. Prof. de Esch is co-founder of IOTA Pharmaceuticals Ltd (2007) and Griffin Discoveries BV (2009). Close window
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| Dr Gregg SIEGAL (ZOBIO BV, Leiden, The Netherlands) Read more
Gregg Siegal obtained his Ph.D. on studies of eukaryotic DNA replication at the University of Rochester in the USA under the supervision of Professor Robert Bambara. Subsequently he post-Doc’ed in the laboratories of Professor Kurt Wüthrich at the ETH in Switzerland and Professor Paul Driscoll at the Ludwig Institute of Cancer Research in the UK. It was during his post-Doctoral work that Dr. Siegal was exposed to NMR as a tool for both structural biology and drug discovery. He moved to Leiden University in 1997 where he received a Dutch Royal Society Fellowship to form his own research group. His research focused on the development and application of innovative drug discovery technologies. In 2004 he spun out the company ZoBio to commercialize the TINS ligand screening technology and eventually left Leiden University to serve as the Chief Executive Officer. In 2018 he was appointed as an extraordinary Professor in the Division of Medicinal Chemistry at the Free University, Amsterdam. Close window
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Experiences and Issues with Biochemical Assays in Fragment-Based Drug Discovery
| Dr Paul ENGLAND (IOTA PHARMACEUTICALS LTD., Cambridge, United Kingdom) Read more
Current Position: Director, IOTA Pharmaceuticals Ltd
Research Field: Biochemistry, Drug Discovery
The first part of my career was in academia, where my initial work was on the control of carbohydrate metabolism. Subsequently my research focussed on signal transduction and the role of protein phosphorylation in the control of the cardiovascular system.
The second half of my career has been spent in the pharmaceutical and biotechnology industries, where I was involved in high throughput screening, assay development, enzymology and compound management in a wide range of therapeutic areas and drug target classes.
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Introduction to Fragment Based Discovery – Overview of the Process and a Historical Perspective
| Prof. Rod HUBBARD (UNIVERSITY OF YORK & VERNALIS, Cambridge, United Kingdom) Read more
Rod Hubbard has been an academic at York for over 35 years working with methods for analysis and exploitation of protein structure, developing molecular graphics and modelling methods in the 1980s and building Structural Biology at York during the 1980s and 1990s. In 1997, he was a founding SAB member of what became Vernalis. Since 2001 he has split his time between Vernalis (fragment and structure based drug discovery) and York (fragment methods for chemical biology and industrial biotechnology). In addition, he works with UK Research Councils and consults with pharmaceutical and technology companies around the world. Close window
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Design Principles for Fragment Libraries
| Prof. György KESERU (HUNGARIAN ACADEMY OF SCIENCES, Budapest, Hungary) Read more
György M. Keserű is heading the Medicinal Chemisty Group at RCNS, Hungary. He obtained his Ph.D. at Budapest and spent almost 20 years in the pharma industry at different R&D management positions (Sanofi-Aventis and Gedeon Richter). Since 2007 he was appointed as the Head of Discovery Chemistry at Gedeon Richter. He was involved in the discovery of 10 clinical candidates (36 patent applications) entered into clinical development in neurological and psychiatric indications. He contributed to the discovery of the antipsychotic Vraylar® (US)/ Reagila® (EU) that has been approved by the US FDA in 2015 and European authorities in 2017. The drug is on the US market from 2016 and available to European patients from 2018. From 2013 he served as a director general of the Research Centre for Natural Sciences (RCNS) at the Hungarian Academy of Sciences. He played a significant role in the development of physicochemical profiling in drug discovery, the concept of compound quality and the improvement of optimization strategies in medicinal chemistry. His results has been acknowledged by the George A Olah Award and the Prous Institute Overton and Meyer Award of the European Federation of Medicinal Chemistry. In 2016 he has been elected as a Fellow (FRSC) of the Royal Society of Chemistry. From 2015 he is a full professor at the Budapest University of Technology and Economics and heading the Medicinal Chemistry Research Group at RCNS. His research interests include medicinal chemistry and drug design. He has published over 200 papers and more than 10 books and book chapters. Close window
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