12th EFMC Short Course on Medicinal Chemistry

Andy joined Pfizer in 1980 following studies at York University, UK. He spent the first 9 years of his career working on Phosphodiesterase (PDE) inhibitors leading to the inotrope/vasodilator (PDE3) candidate, nanterinone, and the PDE5 inhibitor, sildenafil (Viagra®). Andy subsequently moved to the Antifungals Project, where he contributed to development of the broad-spectrum agent voriconazole (Vfend®). Since leaving Pfizer in 2011, Andy has been at Imperial College, London, leading a medicinal chemistry effort to discover novel inhibitors of Plasmodium N-myristoyltransferase for the treatment of malaria.

Paul Brennan received his PhD in organic chemistry from UC Berkeley working on combinatorial chemistry and antibiotics. Following post-doctoral research in Cambridge University on total synthesis, Paul returned to California to take a position at Amgen. His research was focussed on kinase inhibitors for oncology. After two years at Amgen, Paul moved to Pfizer in Sandwich, UK. In 2011, Paul joined the Structural Genomics Consortium as the Associate Professor of Medicinal Chemistry to discover chemical probes for epigenetic proteins. Since 2015, Paul has been the Head of Chemistry at the ARUK ODDI. His current research is focused on epigenetic proteins and new dementia targets.

With a broad interest in both chemistry and physics I studied for a BA in Natural Sciences (Chemistry) and PhD in NMR techniques development at the University of Cambridge. Broaden these skills to include protein biochemistry, biophysics (ITC, SPR, MS) and X-ray crystallography, I now lead the structural biology & biophysics group at GSK’s major European research site in Stevenage. The group supports activities from mode-of-action analysis to fragment based screening across a wide range of therapeutic areas and drug modalities (e.g. small molecule, biopharmaceuticals, vaccines). My recent personal research focus has been in the field of epigenetics (epi-readers and epi-enzymes), where in additional to crystallography support on many of these targets I co-lead a drug discovery program focused on bromodomains.

Prof. Dr Iwan de Esch did his PhD research at the Department of Pharmacochemistry, VU University Amsterdam, The Netherlands. In 1998, he became research associate at the Drug Design Group of the University of Cambridge. He is a co-founder of De Novo Pharmaceuticals (2000) where he worked as a group and project leader. He returned to academia in 2003 and is now professor at the Medicinal Chemistry Department of VU University Amsterdam. The group focuses on two research lines, namely G-protein-coupled receptors (GPCRs) and Fragment-Based Drug Design (FBDD). Prof. de Esch is co-founder of IOTA Pharmaceuticals Ltd (2007) and Griffin Discoveries BV (2009). In 2011, he was awarded the Galenus Research Price for his work on FBDD.

Beat Ernst, Professor of Molecular Pharmacy, Pharmacenter, University of Basel, Switzerland. Professor Ernst studied chemistry at the ETH Zürich, where he also completed his Ph.D. supervised by Proff. Oskar Jeger and Camille Ganter. He spent the following two years as a post-doctoral associate at the California Institute of Technology, Pasadena, CA, in the research group of Prof. Robert E. Ireland. In 1981, he joined Ciba-Geigy’s Central Research Laboratories in Basel. After his promotion to section head Carbohydrate Chemistry and Biology in 1992, he initiated the Selectin program. In 1997, he moved to Transplantation Research within Novartis Pharma AG, which had been formed through the merger between Ciba-Geigy and Sandoz. Beat Ernst’s research interests are at the interface between carbohydrate chemistry and glycobiology, with a particular focus on the synthesis of glycomimetics and their pharmacological profiling. His research on one hand aims at understanding the conformational and structural requirements for biological activity of glycomimetics, and on the other hand, in collaboration with academic and industrial groups, he explores the therapeutic potential of such compounds in disease models, and in one case, in the clinic (Rivipansel, currently in clinical phase III for the treatment of sickle cell disease) with the ultimate goal to discover new therapeutics.

Prof. Dr. Groll (b. 1971) conducts research in the field of biochemistry, investigating the structure and function of biological multimeric protein complexes. He is also interested in the basic structure of protein-protein and protein-ligand interactions. Another area of research is the medical relevance of synthetic and natural molecules in terms of their interaction with proteins.

Michael Groll (*23.09.1971) studied Chemistry at the Technische Universität München and then joined the group of Prof. Dr. Robert Huber for postgraduate studies. In 1998, he received his Ph.D. for crystallographic and biochemical studies on the yeast 20S proteasome. He continued to work as a postdoctoral fellow at the Max-Planck-Institute in Martinsried, at the Ludwig Maximilians Universität München and at the Harvard Medical School in Boston. In 2004, Michael Groll received his Habilitation from the Charité in Berlin. Since 2007, he is Chair of Biochemistry at the Department Chemie of the Technische Universität München.

Laurie LeBrun received her Ph.D. in Biochemistry from the University of Iowa specializing in enzymology. She went on to complete two postdoctoral fellowships. The first was in the Department of Medicinal and Natural Products Chemistry at the University of Iowa with a focus characterizing the interactions between polysaccharides and proteins. The second was in the Department of Pharmaceutical Chemistry at University of California, San Francisco with a focus on P450’s. Laurie then joined Anadys Pharmaceuticals for six years working in the Biochemistry and Drug Metabolism departments. She then moved to join the Biochemistry Department at Celgene and is currently a Principal Scientist. Laurie has been at Celgene for eight years and is responsible for the Assay Development Group and Project Leadership. Laurie has helped progress eight compounds into the clinic in the following therapeutic areas: virology, oncology, and inflammation.

Dr. Gerhard Müller, Senior Vice President Medicinal Chemistry at Mercachem, Nijmegen, NL core expertise in small molecule drug discovery entertaining a broad variety of lead finding approaches, ranging from Fragment-Based Lead Generation over Structure-Based Design to DNA-encoded Library methodologies. Expert knowhow developed around the Privileged Structure Concept centered around target families such as protein kinases, PDEs, GPCRs, epigenetic enzymes, and protein-protein interactions. Strong emphasis laid on post-Lipinski optimization parameters in Lead Optimization such as binding kinetics. Prior to Mercachem, permanent positions at pharmaceutical companies (Glaxo, Bayer, Organon), CSO at Axxima Pharmaceuticals, VP Research at GPC Biotech in Munich. PhD from Technical University Munich in the group of Prof. Dr. Horst Kessler

Dr. Holger Sellner is a medicinal chemist at the Novartis Institutes for Biomedical Research, Basel, Switzerland. He received his PhD from the ETH Zürich in 2001 working in the field of organic methodology. After a postdoctoral stay in the group of Professor Andrew Myers at Harvard University contributing to the synthesis of complex natural products he joined the Expertise Platform Proteases at Novartis in Basel in 2003. There, he has been involved in numerous drug discovery projects centered around protease targets which ultimately led to the identification of clinical candidates.

Leon van Berkom studied chemistry at the University of Nijmegen and received his master degree in 2000. His masters dissertation was awarded with the Organon Young Research Talent Award for most outstanding thesis in the field of pharmaceutical research. He received his Ph.D. in organic synthesis in 2004 from the University of Nijmegen. Immediately thereafter he joined Mercachem BV as senior scientist. Since then he has been leading multiple projects for small, midsize and large pharmaceutical companies and worked in Lead Generation and Lead Optimization on numerous target classes from a number of different disease areas. His current position is group leader at Mercachem BV.

Toine van den Bergh received his Bachelor degree at the Hogeschool Arnhem Nijmegen in 1999 and in sequence he studied chemisty at the Universityof Nijmegen. After obtaining his Master degree in 2002 he started working at Mercahem BV as Scientist. Toine has been involved in numerous projects for European and American pharmaceutical companies. During the last 3 years Toine is taking part in several Lead generation and lead optimization programs. His current position is Senior Scientist at Mercachem.