GPCRs: a Discovery Powerhouse
Session Chair
Dr Yves P. AUBERSON
NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH, Basel, Switzerland
Yves P. Auberson obtained his Ph.D. in 1990 at the Swiss Federal Institute of Technology in Lausanne, Switzerland. He joined the Novartis Institute for BioMedical Research in Basel, Switzerland in 1992, after a post-doctoral training in chemical biology at Affymax in Palo Alto, USA.
He is currently Executive Director in Global Discovery Chemistry, where his research group develops tracers for clinical imaging. Previously, he was Head of Chemistry for Neuroscience, and played a leading role in the discovery and development of drug candidates for the treatment of epilepsy, Alzheimer’s disease and narcolepsy.
He is President of the European Federation of Medicinal Chemistry (EFMC), and of the Division of Medicinal Chemistry and Chemical Biology of the Swiss Chemical Society.
09:00
G Protein-Coupled Receptors: the Structural Basis for their Pharmacology (IL10)
Dr Chris TATE
MRC LABORATORY OF MOLECULAR BIOLOGY, Cambridge, United Kingdom
Chris obtained his PhD from the University of Bristol (1989) and then moved to the University of Cambridge (Dept of Biochemistry). After obtaining a research fellowship at Girton College (Cambridge) he moved to the LMB to work in Richard Henderson's group on the serotonin transporter. Chris then worked on the E. coli multidrug transporter EmrE and obtained both 2D and 3D crystals as well as a 3D structure using cryo-EM. In 2005 he started working on the development of conformational thermostabilisation of GPCRs, which resulted in the structure of the 1-adrenoceptor. Subsequent work has focused on understanding the molecular basis of GPCR pharmacology through structure determination of the 1-adrenoceptor and adenosine A2A receptor in multiple different conformations bound to ligands of different efficacy. In 2016 mini-G proteins were developed as a tool for the structure determination of GPCRs in the fully active state. Structures have been determined either by X-ray crystallography of receptors coupled to either mini-Gs or mini-Go, or by electron cryo-microscopy of receptors coupled to mini G protein bound to subunits.
09:30
Design of Orexin 1 Receptor Selective Antagonists (IL11)
Dr Uta LESSEL
BOEHRINGER INGELHEIM, Biberach an der Riss, Germany
Uta Lessel, Principal Scientist in Computational Chemistry within the Department Medicinal Chemistry, working on early projects (special fields of interest: virtual screening, phenotypic screening and macrocycles)
study of Pharmaceutical sciences at the University of Düsseldorf
PhD in Pharmaceutical Chemistry from the University of Düsseldorf
Postdoc at a research institute in Brunswick (Germany) and at the University of Cologne
joined Boehringer Ingelheim in 1998.
10:00
Next Generation GPR119 Agonists as Potential Treatment for Cardiometabolic Diseases (IL12)
Dr Lothar SCHWINK
SANOFI, Frankfurt Am Main, Germany
Lothar studied chemistry at the Philipps-University in Marburg (Germany) were he earned his doctoral degree for his work on asymmetric catalysis under the supervision of Prof. Paul Knochel in 1997. During a postdoctoral stay at the University of California, Irvine, in Prof. Larry Overman’s group, he completed the total synthesis of aloperine and succeeded in assembling a strategic intermediate for asparagamine A.
Since 1999, Lothar is leading research teams directed towards the optimization of small molecule drug candidates for metabolic diseases at Sanofi or its predecessor companies. Examples include natural product derived enzyme inhibitors, and several modulators of nuclear hormone and G-protein coupled receptors.
10:30
Coffee Break and Exhibition
Specific and Multi-Targeted Drugs
Session Chair
Prof. Andrzej BOJARSKI
INSTITUTE OF PHARMACOLOGY POLISH ACADEMY OF SCIENCES, Krakow, Poland
11:00
Charting New Paths in Multi-Target Drug Discovery for Alzheimer’s Disease (IL13)
Prof. Maria Laura BOLOGNESI
UNIVERSITY OF BOLOGNA, Bologna, Italy
Maria Laura Bolognesi holds the position of Professor of Medicinal Chemistry and Director of the Chemistry and Pharmaceutical Technologies degree program at the Alma Mater Studiorum - University of Bologna. She received her PhD in Pharmaceutical Sciences in 1996 and carried out postdoctoral work at the University of Minnesota. Her research explores the development of small molecules in the neurodegenerative and neglected tropical disease therapeutic areas. Maria Laura has a track record of more than 160 publications in high-ranked scientific journals, including patents and patent applications, and numerous invited talks worldwide. She was awarded the positions of Distinguished Visiting Professor at the Complutense University of Madrid in 2009, Pesquisador Visitante Especial at the University of Brasilia in 2014 and Professeur Invité at Université Caen Normandie in 2018. She is also an Associate Editor of Journal of Medicinal Chemistry and serves in the Advisory Board of the European Federation of Medicinal Chemistry.
11:30
Multiple Targeting - The Histamine H3 Receptor Pharmacophore as Central Element (IL14)
Prof. Holger STARK
HEINRICH HEINE UNIVERSITY DÜSSELDORF, Duesseldorf, Germany
Prof. Dr. Dr. h.c.Holger Stark studied pharmacy and finished his PhD in Medicinal Chemistry at the Free University of Berlin. He focused on neurotransmitter research with emphasis on histamine as well as dopamine receptor subtypes and expanded this on lipid signalling. In 2000 he became full professor at the Goethe University in Frankfurt, Germany and went in 2013 to the Heinrich Heine University in Düsseldorf, Germany where he has his actual position. He founded some start-up companies on cancer therapeutics (Warburg Glycomed, PSites Pharma) and has received several prices for his successful research as well as for teaching. He is co-inventor of pitolisant (Wakix®), the first histamine H3 receptor antagonist with market approval, and has prepared some back-up candidates in different leads for various targets. Since 2004 Holger Stark is editor-in-chief of the Archiv der Pharmazie – Chemistry in Life Sciences, one of the oldest journals on Medicinal Chemistry.
12:00
Chemical Biology for Drug Discovery: A Click and Play Approach Exemplified by ERK1/2 Probes (OC03)
Dr Charlotte GRIFFITHS-JONES
ASTEX PHARMACEUTICALS, Cambridge, United Kingdom
Charlotte Griffiths-Jones gained a PhD from Cardiff University in 2004 then undertook a post doc in Cambridge under the supervision of prof Steve Ley. After 1 year at GSK working in the technology development lab, she moved to Astex in 2007 where she is now an Associate Director. Charlotte has worked on a number of fragment based drug discovery projects from early stage right through to clinical development. This includes the recently launched oncology drug Erdafitinib.
12:15
Identification and in-vivo Efficacy Studies of a Nicotinamide Derivative as Novel NNMT Inhibitor (OC04)
Dr Sven RUF
SANOFI-AVENTIS DEUTSCHLAND GMBH, Frankfurt am Main, Germany
Dr. Sven Ruf completed his PhD studies in synthetic organic chemistry with Prof. Regitz at the University of Kaiserslautern in 1999. Afterwards he spent the year 2000 with postdoctoral studies in the group of Prof. Trost at Stanford University. In 2001 he joined the medicinal chemistry department of the Sanofi-Aventis Deutschland GmbH and currently holds the position of a senior scientist. He has been responsible for the lead discovery strategies deployed in several early resarch projects and is a team and project leader at the Sanofi research site in Frankfurt
12:30
Opioid, Pain, Endo-Cannabinoid
Session Chair
Prof. Katarzyna KIEC-KONONOWICZ
JAGIELLONIAN UNIVERSITY, Krakow, Poland
14:00
Cannabinoid Receptor Type 2 Modulation to Improve Outcomes for Cartilage Repair in the Osteoarthritic Joint (IL15)
Prof. Katarzyna STAROWICZ-BUBAK
INSTITUTE OF PHARMACOLOGY, POLISH ACADEMY OF SCIENCES, Krakow, Poland
Katarzyna Starowicz (PhD, DSc) is a neuropharmacologist leading Department of Neurochemistry based at the Institute of Pharmacology Polish Academy of Sciences (www.if-pan.krakow.pl).
her education includes M.Sc. degree in Biotechnology from the Jagiellonian University (2000), PhD in Pharmacology at the Medical Sciences at the Utrecht University (2005) and Habilitation in Medical Biology at the Faculty of Medicine of the Jagiellonian University Medical College (2013). After receiving a PhD degree she started a postdoctoral fellowship in Endocannabinoid Research Group under the supervision of prof. Vincenzo Di Marzo. After completing the postdoctoral fellowship she returned to Poland where she have established and maintained a laboratory focused on understanding of the mechanisms of chronic pain and on the characteristics of endogenous system involved in the transmission of pain stimuli with particular attention to endocannabinoid system. Subsequently, my research interests expanded to include the issue of degenerative joint disease (particularly osteoarthritis, OA).
Please visit http://www.painlab.pl for more details and full description of current research interests.
Laureate of the Powroty / Homing program of the Foundation for Polish Science, the habilitation scholarship of L'Oréal Poland for Women and Science in 2012 and the National Science Centre Award in Life Science in 2016. Member of British Journal of Pharmacology Editorial Board. President of the Alumni Association of the Foundation for Polish Science (2017-2019). V-ce President of the Board of National Agency for Academic Exchage (NAWA, www.nawa.gov.pl).
14:30
Potential of Natural Cannabinoids and Synthetic Cannabinoids in Neuroprotection (IL16)
Prof. Rafael FRANCO
UNIVERSITY OF BARCELONA, Barcelona, Spain
I am Molecular Neuropharmacologist coming with Biochemistry and Molecular Biology background.
I did a first postdoc stay in the lab of Prof. Geoffrey Burnstock in UCL (Univ College London) where I get acquainted with purinergic nerves and purinergic actions.
Back in Spain I founded one of the first labs in Europe devoted to the work from a molecular point of view of G protein-coupled receptors (GPCRs).
Other stays abroad were: in Max Planck Institute Dortmund with Prof. Rolk Kinne, in Harvard Medical School with Prof. Cox Terhorst and in Pasteur Institute with Prof. Ara Hovanessian.
My laboratory is internationally known for the discovery of GPCR heteromers and for research on their physiological relevance.
The main focus is the central nervous system and we now have taken a translational approach for which we collaborate with Medicinal Chemistry laboratories in different Countries.
GPCRs in our portfolio include, among other, those for adenosine, cannabinoids, epinephrine, orexin, dopamine and ghrelin.
We are interested in neurodegenerative diseases and in drug addiction (cocaine, ethanol and amphetamine)
I have circa 400 papers mainly in international journal and h index as of Nov 2018 is: 68.
Number of citations is >15,000.
15:00
Discovery of Best in-class, Novel, Selective, Potent and Peripheral FLT3 Inhibitors, a New Way to Treat Neuropathic Pain (OC05)
Dr Dominique SURLERAUX
BCI PHARMA, Liège, Belgium
Dominique Surleraux is Chief Executive officer (CEO) of BCI Pharma. BCI Pharma was founded in March 2013 and is actually located in France (Montpellier) and Belgium (Liège).
Dominique Surleraux has a Ph.D in organic chemistry from university of Namur (BE) and a master in drug design (Lille, FR).
Dr. Dominique Surleraux started his career at Janssen Phamaceutica (J&J (BE), 5 years), then moved to Tibotec (J&J (BE), 7 years) and was managing worldwide anti-infective research for J&J.
He then moved to France and supervised the HCV research (60 scientists) for idenix Pharmaceutical, a Boston based company acquired by MSD (4b$).
He was directly involved on the discovery of blockbusters (Prezista (HIV protease Inh.) and Simeprevir (HCV protease Inh.) and bring more than 10 drugs in clinical development.
He is inventor/co-inventor of more than 100 patents.
15:15
The Discovery and Development of the Clinical FAAH Inhibitor JNJ-42165279 (OC06)
Prof. James BREITENBUCHER
UNIVERSITY OF CALIFORNIA SAN FRANCISCO, San Francisco, United States
Dr. Breitenbucher has over 20 years of drug discovery experience and is currently Professor at the Institute for Neurodegenerative Diseases at UCSF.
Prior to joining UCSF, Dr. Breitenbucher was senior director of Chemistry at Dart Neurosciences. During his 8 years at DNS he built a robust department that discovered 10 novel pre-clinical candidates for 7 different biological mechanisms for the treatment of Stroke, Alzheimer’s, and Parkinson’s Disease.
Prior to DNS Guy was a research fellow at Johnson & Johnson as head of the Pain Discovery Chemistry. At J&J, Dr. Breitenbucher worked on or led drug discovery projects on 10 different biological mechanisms which advanced compounds into pre-clinical or clinical development. Dr. Breitenbucher received his B.Sc. and M.Sc. in chemistry at California State University at Long Beach and his Ph.D. in organic chemistry at University of California at Riverside. Dr. Breitenbucher is co-author on over 50 peer reviewed scientific papers, an inventor on over 40 patents.
15:30
Coffee Break and Exhibition
Session Chair
Prof. Terry MOORE
UNIVERSITY OF ILLINOIS, Chicago, United States
16:00
Next Generation Pain Therapeutics for the Opioid Crisis: Design of Bifunctional Nociceptin/Mu Opioid GPCR Ligands as non-Addicting Analgesics (PL03)
Dr Nurulain ZAVERI
ASTRAEA THERAPEUTICS, Mountain View, United States
Dr. Zaveri is the Founder, President and Chief Scientific Officer of Astraea Therapeutics, a preclinical discovery company she founded in 2009, whose mission is medication development for under-served diseases of the central nervous system (such as opioid and substance abuse and addiction, chronic pain and Parkinson’s disease). A PhD medicinal chemist by training, Dr. Zaveri is a recognized expert in the field of G-protein coupled receptor-targeted- and ion channel-targeted drug discovery for CNS medications, that are being advanced into medication development. Before her entrepreneurial venture at Astraea Therapeutics, Dr. Zaveri was Principal Investigator and Director of the Drug Discovery Program at the Stanford Research Institute International in Menlo Park, CA, for 16 years. Dr. Zaveri is a Fellow of the American Association of Pharmaceutical Scientists (AAPS). Dr. Zaveri is the lead inventor on over 12 patents and has authored over 60 research publications and 10 reviews/book chapters in fields of her research. Dr. Zaveri also serves on several NIH grant review committees and is a long-time member of ACS and the MEDI Section.
Pharma Research Highlights in Poland
16:45
Discovery of OAT-2068 - A Potent, Selective, Orally Bioavailable Inhibitor of Mouse Chitotriosidase and its In Vivo Activity in the Bleomycin-Induced Pulmonary Fibrosis Model in Mice (OC07)
Dr Agnieszka BARTOSZEWICZ
ONCOARENDI THERAPEUTICS SA, Warszawa, Poland
Agnieszka completed her PhD studies in organic chemistry under the supervision of Prof. Belén Martín-Matute at Stockholm University, Sweden in 2012. Afterwards she spent 2 years as a postdoctoral fellow in the group of Prof. Gregory Fu at Caltech, Pasadena, CA, USA. She joined Oncoarendi Therapeutics SA in 2015 as a medicinal chemist. Agnieszka is currently a team and project leader at Oncoarendi working on design and synthesis of small molecule inhibitors targeting chitinase-like-proteins.
17:00
DPD-inspired Small Heterocyclic Libraries Characterized as Novel LsrK Kinase Inhibitors: an Opportunity to Fight Antimicrobial Resistance (OC08)
Dr Anna KARAWAJCZYK
SELVITA, Krakow, Poland
17:15
Poster Session 2
(Posters with even numbers)
18:15
20:00