Current title: Scientific Director & Fellow, Janssen R&D
Position: Group Leader of the Oncology Discovery Chemistry team at Val de Reuil site (Normandy).
Research field: Medicinal chemistry, mainly in oncology area (kinases, epigenetic targets, PPI inhibitors).
Education: Engineer (INSCIR) and PhD in organic chemistry (Rouen University/ asymmetric synthesis/ 1991).
Professional experience: 26 years at Janssen. As project leader participated in the discovery of several clinical candidates (Farnesyltransferase inhibitor tipifarnib, Histone Deacetylase inhibitor quisinostat, Fibroblast Growth Factor Receptors inhibitor erdafitinib). Co-author/co-inventor of ~ 95 articles and patents
Chemoinformatics-Driven View of Kinase Drug Discovery (Lecture sponsored by ChemMedChem)
Jürgen Bajorath is Professor and Chair of the Life Science Informatics Department at the University of Bonn since 2004. His research focuses on the development and application of chemoinformatics methods and computational medicinal chemistry. Jürgen received diploma and
Ph.D. degrees in biochemistry from the Free University in West-Berlin and was a Postdoctoral Fellow at Biosym Technologies in San Diego. He spent seven years at the Bristol-Myers Squibb Pharmaceutical Research Institute in Seattle where he became a Principal Scientist (and was subsequently involved in starting a biotech company). In 1995, Jürgen was appointed Affiliate Associate and later Full Professor of Biological Structure at the University of Washington, Seattle.
Kinase Inhibitors for Non-oncological Indications: Is there a Future ?
Doriano Fabbro, PhD in Biology, has 25 years of experience in drug discovery in Pharma (Ciba-Geigy, Novartis) as well as Biotech (Piqur Therapeutics) following 10 years in academia. He has led the NIBR Expertise Platform Kinases dedicated to global Kinase Drug Discovery Projects for several Oncology, Immunology, Inflammation, Respiratory Disease, Muscular Disease and Cardiovascular.
Since 2012 he is Chief Scientific Officer of Piqur Therapeutics (Basel Switzerland), a small company devoted to the discovery of PI3K/mTOR inhibitors as well as scientific advisor for several pharmaceutical companies in the area of kinase drug discovery.
During his career he contributed to the development of the following approved anticancer drugs Glivec® (Imatinib, BcrABL inhibitor), Tasigna® (Nilotinib, BcrAbl inhibitor), Afinitor® (Everolimus, mTOR inhibitor), Rydapt® (Midostaurin, Kit and Flt-3 inhibitor). In addition he contributed to the development of Apelisib (PI3K inhibitor), Buparlisip (PI3K inhibitor), Vatalinib (VEGFR inhibitor, Luminespib (hsp90 inhibitor) and many more.
CDK8 Inhibitors with Pre-Engineered Long Residence Time: From Design to Tumor Xenograft Models
Dr Koen HEKKING
MERCACHEM-SYNCOM, Nijmegen, The Netherlands Read more
Dr Koen HEKKING
Dr. Koen Hekking is a group leader in the medicinal chemistry department at Mercachem (The Netherlands). He obtained his PhD in natural product synthesis and catalysis at the Radboud University in Nijmegen under the supervision of Prof. Floris Rutjes. In 2006 he joined Mercachem as senior scientist, and has held a group leader position since 2008, supervising a variety of (medicinal) chemistry projects. For the past 4 years, he has acted as project manager for two kinase projects as well as for Mercachem’s internal innovation projects. These projects currently involve protein degradation, novel macrocyclic scaffolds, and early stage medicinal chemistry projects in the areas of epigenetics and kinases.
Lead Optimization as a Playground for New Concepts, Reactions and Chemical Modalities: Development of Several Generations of Clinical CDK Inhibitors at Bayer AG
Ulrich Lücking is a Principal Scientist at Bayer AG in Berlin. He started his industrial career in 2001, working across multiple therapeutic areas, mainly in lead optimization, to successfully deliver multiple clinical candidates. His efforts were e.g. instrumental in the discovery of clinical candidates in the CDK inhibitor projects, the Androgen Receptor Suppressor project, the PTEFb inhibitor projects and the ATR inhibitor project. Moreover, he has a longstanding interest in neglected sulfur (VI) pharmacophores and macrocyclic compounds in drug discovery. Prior to joining industry, he studied chemistry at the University of Hannover. As an Erasmus student and later for his diploma work, he spent time in the laboratory of Prof. Steven V. Ley. In 1999 he completed his Ph.D. under the direction of Prof. Andreas Pfaltz, and then carried out postdoctoral work in the laboratories of Prof. Julius Rebek.
Discovery, Development and In Vivo Profiling of a Novel Class of Immunosuppressive PI4KIIIβ Lipid Kinase Inhibitors
Joined Celltech in 1994 as a research associate, working on PDEIV and integrin programs. After 6 years moved to AZ Charnwood, joining the respiratory and inflammation hit to lead group working on small molecule projects in lead identification and lead development, before moving into the lead optimisation area, supporting the delivery of key inhaled projects. In 2007 returned to Slough to take up a position at UCB, after their acquisition of Celltech Chiroscience. Joined the ‘breakthrough’ chemistry group, looking at fragment screening for both classical small molecule targets and more complex protein-protein interaction targets. In 2012 became the lead chemist on the PI4K program in a joint venture with KUL and UCB which is the basis of today’s talk. Currently working on late stage PPI program as well as working with computational chemistry and biophysics groups to identify new starting points for a variety of challenging PPI targets.
OC02 - Discovery And Development Of Highly Potent And Selective FLT3 Kinase Inhibitors, A New Class of Peripheral Drugs for Treating Neuropathic Pain
Claire Amiable completed her chemistry studies at the Ecole Supérieure de Chimie Organique et Minérale. She also obtained a master's degree from Chimie ParisTech. Claire then received her PhD in organic chemistry from the University of Paris Descartes working on the design and synthesis of DNPH1 inhibitors at the Institut Pasteur of Paris under the supervision of Dr Sylvie Pochet.
Since 2014, she has joined BCI Pharma as a research scientist.
OC01 - A Fast in Silico Fragment-Based Design Tool for the Discovery of Novel Kinase Inhibitors
In 2012, Pascal Bonnet joined the Institute of Organic and Analytical Chemistry (ICOA) from the University of Orléans as full professor. He set up the team “Structural Bioinformatics and Chemoinformatics”, which develops and integrates novel computational methods for drug discovery. His research interests also focus on the development of an integrative in silico platform for kinase research. Since 2016, he was appointed director of the ICOA. After completing his PhD in 2001 at the University of Orléans (France) and the University of Barcelona (Spain), he moved to a postdoctoral position at the University of Manchester, UK. As a scientist, he joined Janssen-Cilag in France and then Janssen-Pharmaceutica in Belgium in 2003. He was involved in several drug discovery projects mainly in the oncology therapeutic area. Promoted Principal Scientist in 2010, he was leading the Kinase Platform at Janssen. He contributed to the development of a clinical drug candidate, erdafitinib, a kinase inhibitor discovered by FBDD currently in Phase II clinical trials.
OC03 - Imidazo[4,5-B]Pyridine Derivatives as Potent Tam Inhibitors: From Synthesis To Cellular Imaging
Sandrine Piguel received her Ph.D. in organic chemistry from the University of Paris Sud in France in 1998. She worked on the total synthesis of enediynes under the supervision of Dr. D. S. Grierson at the Institut de Chimie des Substances Naturelles. In 1999, she joined the group of Pr. M. Lautens at
the University of Toronto as a post-doctoral fellow (Prize from the Fondation Bettencourt-Schueller), developing palladium-catalyzed domino reactions with C-H bonds functionalization. After a short stay with Pr. T. Wirth at the University of Basel, she was appointed assistant professor at the University of
Rennes 1 in 2001 working on the synthesis of proteasome inhibitors. In 2006, she moved to University of Paris Sud and joined the Institut Curie (Orsay, France) where she became Associate Professor in 2010. Her research interests include medicinal chemistry in the field of small molecule kinase inhibitors for cancer therapy but also new synthetic methodologies such as C-H bond functionalization reactions.