07:30
08:30
RICT 2019 Opening
Prof. Sebastien PAPOT
UNIVERSITY OF POITIERS, Poitiers, France
Prof. Pascal MARCHAND
UNIVERSITY OF NANTES, Nantes, France
Dr Patricia LEMARCHAND
UNIVERSITY OF NANTES, Nantes, France
Inaugural Conference
Session Chair:
Prof. Sebastien PAPOT
UNIVERSITY OF POITIERS, Poitiers, France
09:00
PL01: What Makes a Great Medicinal Chemist: Some Fresh Thoughts
Dr Mark MURCKO
RELAY THERAPEUTICS, Boston, MA, United States
Research interests: Drug-hunting, mentoring/teaching, company-building, the application of disruptive technology to accelerate R&D
Current positions (partial list):
- Founder, board member & strategic advisor, Relay Therapeutics
- Senior Lecturer, Department of Biological Engineering, MIT
- Board member, Quentis Therapeutics
- SAB member & board advisor, SQZ Therapeutics
- Board of Trustees, Gordon Research Conferences
Education: Ph.D. Organic Chemistry, Yale
Former positions:
- Interim CSO, Relay Therapeutics
- Chief Technology Officer, Vertex Pharmaceuticals
- Senior Scientist, Merck Sharpe & Dohme
Session 1: Recent Advances for Cancer Therapy
Session Chair:
Dr Yannick JACQUES
INSERM/CNRS, Nantes, France
09:45
PL02: Reprogramming the Reactivity of Iron in Cancer
Dr Raphaël RODRIGUEZ
INSTITUT CURIE, Paris, France
Dr. Raphaël Rodriguez, FRSC, was born October 27, 1978 in Avignon (France). He performed his PhD studies under the supervision of Sir Jack E. Baldwin and Prof Maurice Santelli, working on the biomimetic synthesis of complex natural products. Then, he joined the University of Cambridge in 2005 as a postdoctoral research fellow, working under the mentorship of Sir Shankar Balasubramanian, with whom he established a functional link between G-quadruplex structures and genomic instability. Raphaël is Director of Research at the CNRS and group leader at Institut Curie. His work is focused on the chemistry underlying cancer cell biology. In particular, he is interested in elucidating roles of d-Block metals in cancer.
10:30
Coffee Break and Exhibition
11:00
PL03: Quo Vadis Small Molecule Cancer Therapeutics?
Dr Ingo HARTUNG
BAYER HEALTHCARE, Darmstadt, Germany
Dr. Ingo Hartung is VP of Medicinal Chemistry at Bayer AG in Berlin and responsible for Bayer’s early research portfolio in immuno-oncology. Prior to this he headed Bayer’s activities in discovering epigenetic probes within the Structural Genomics Consortium. Ingo joined Bayer in 2004 and led optimization projects in oncology and cardiology research before taking up the role as head of Bayer’s microbiological chemistry lab. His research interests cover oncology drug discovery, innovation in medicinal chemistry and the use of biocatalysis in life sciences. Ingo is lecturer for medicinal chemistry at the Technical University Berlin. Ingo received his PhD in organic chemistry from University of Hannover/Germany and was a post-doctoral fellow at Stanford University/US. Ingo is a member of the American Association for Cancer Research (AACR) and the Gesellschaft Deutscher Chemiker (GDCh).
11:45
KL01: Therapeutic Potential of Macrocyclic ALK2 Inhibitors
Dr Pascal BENDERITTER
ONCODESIGN, Dijon, France
Title and position: Director in medicinal chemistry – Project leader at Oncodesign
Research field: Small molecule therapeutics, especially small macrocycles as kinase inhibitors
Education and former professional experience:
. Education:
. Master (Engineer) degree in organic chemistry (ENSCMu, France)
. Master in Pharmacology (University of Strasbourg, France)
. PhD in organic chemistry (University of Strasbourg, France)
. Professional experience:
. Oncodesign since 2013
. AC Immune 2009-2012
. Janssen Pharmaceutica 2007-2008
12:15
13:00
Posters (Odd numbers) and Exhibition
Session 2: Artificial Intelligence in Drug Discovery
Session Chair:
Prof. Pascal BONNET
UNIVERSITY OF ORLÉANS, Orléans, France
14:30
PL04: Massively Multi-target Profile-QSAR: IC50 Predictions Comparable to 4-Concentration Experiments for most Novartis Assays
Dr Eric MARTIN
NOVARTIS, Emeryville, United States
Eric Martin has a Ph.D. in physical organic chemistry from Yale University. He has worked in computational drug design and herbicide design for 35 years at Dow, DowElanco, Chiron and Novartis. He is currently developing novel methodologies for two areas of drug discovery: 1) Developing “Profile-QSAR”, a multi-target machine learning method that builds experimental-quality virtual screening models for most Novartis IC50 assays, and 2) “rational oral bioavailability design” during lead optimization by applying global sensitivity analysis to physiologically-based pharmacokinetics simulations.
15:15
PL05: Automated Syntheses Planning and its Implications for Drug Design
Dr Marwin SEGLER
BENEVOLENTAI, Cambridge, United Kingdom
Marwin Segler studied chemistry at Westfälische Wilhelms-Universität Münster, Germany. During his MSc thesis in synthetic organic chemistry in the group of Prof. Olga Garcia-Mancheño, he worked at the bench on C-H functionalization. After his MSc, he went for 9 months on parental leave. For his PhD, still in Münster, Marwin joined the group of Prof. Mark Waller to study organic chemistry from a computational perspective. He investigated approaches for the computer-aided invention of novel chemical reaction types, introduced neural generative models to de-novo drug design, and introduced machine-learning to computer-aided retrosynthesis. Marwin now works at BenevolentAI in the Chemistry group as Lead Machine Learning Researcher.
16:00
Coffee Break and Exhibition
Session 3: Mechanism Based Approaches
Session Chair:
Dr Maria DUCA
UNIVERSITY OF CÔTE D'AZUR, Nice, France
16:30
PL06: Discovery of Risdiplam, a Selective Survival of Motor Neuron-2 (SMN2) Gene Splicing Modifier for the Treatment of Spinal Muscular Atrophy (SMA)
Dr Hasane RATNI
F. HOFFMANN-LA ROCHE LTD, Basel , Switzerland
Dr H. Ratni is an Expert Scientist, Medicinal Chemistry, at F. Hoffmann-La Roche Ltd., pRED, Pharma Research & Early Development, Roche Innovation Center Basel, Switzerland. During the year 2018, he was also Section head medicinal chemistry for neurosciences, ophtalmology and rare diseases.
He received his PhD at the University of Geneva and did a post-doc at Tokyo before joining F. Hoffmann-La Roche Ltd in 2001. His research has mainly been devoted to the areas of neuroscience (for example neurokinin receptors, or V1a receptor antagonist now in human clinical trials, phase II, for autism). In 2005, he participated in a secondment within the Roche group at Chugai Pharmaceutical Co. Ltd, Gotemba Japan, in the field of renal disease. He was the chemistry discovery project leader of the SMN program aiming for a treatment for spinal muscular atrophy, now completing pivotal clinical trials in patients. His current focus is on gamma secretase modulator for Alzheimer disease.
He is an author or co-author of more than 110 patents and publications. In 2014 he received the Roche Leo Sternbach Award for Innovation in Chemistry and in 2016 the Gold medal at the Roche Patent Inventor’s recognition event.
17:15
PL07: The Influence of Free Ligand Conformations on Mcl-1 PPI Inhibition
Dr Rodrigo CARBAJO
ASTRAZENECA, Cambridge, United Kingdom
Current position: Associate Principal Scientist, Oncology Chemistry, AstraZeneca (since 2015)
Research Field: Structural Chemistry + NMR spectroscopy in Drug Discovery
Education/Professional Experience:
• PhD in Chemistry from University of Oviedo (Spain): NMR on organometallic complexes (1999)
• 1999-2004: postdoctoral researcher at MRC-LMB (Cambridge, UK): biomolecular NMR on the ATPase enzyme
• 2004-2014: Senior Research Scientist at Centro de Investigación Príncipe Felipe, Valencia (Spain): structural biochemistry and drug discovery
• Over 50 articles in peer review journals
18:00
KL02: Tackling a Unique S1 Protease by SBDD - Highly Potent & Selective Factor D Inhibitors - Age-Related Macular Generation (AMD)
Dr Edwige LORTHIOIS
NOVARTIS, Basel, Switzerland
Edwige Lorthiois recieved her PhD in chemistry at the University Pierre et Marie Curie in Paris in 1997 with Prof. J. Normant and I. Marek. Following a post-doctoral training at the ETH in Zürich with Prof. A. Vasella, Edwige worked for 4 years as a medicinal chemist at Pfizer Global Research and Development in the field of Allergy and Respiratory Diseases in Paris and in Neuro Science in Ann-Arbor (Michigan). In 2003, Edwige joined Novartis Institute for Biomedical Research in Basel as a medicinal chemist focusing on the discovery of drug candidates directed against proteases. In 2016, Edwige joined Global Discovery Chemistry as a senior research investigator where she contributes to several Oncology projects.
18:30
Welcome and Networking Reception
20:30