Session 5: Evotec Prize for Excellence in Molecular Design
Session chairs
Dr Jean-Yves ORTHOLAND
EDELRIS, Lyon, France
Dr Christophe BOLDRON
EVOTEC, Toulouse, France
08:45
PL10 - Modulation of Protein – Protein Interactions by Means of Peptidomimetics
Prof. Steven BALLET
VRIJE UNIVERSITEIT BRUSSEL, Brussels, Belgium
Session 6: Neurodegenerative Diseases
Session chair
Prof. Patricia MELNYK
INSERM - UNIVERSITÉ DE LILLE, Lille, France
09:45
PL11 - Structural Biology Supporting Medicinal Chemistry of Purine Receptors
Prof. Christa MÜLLER
UNIVERSITY OF BONN, Bonn, Germany
Christa Müller studied pharmacy at the University of Tübingen, Germany, and received her Ph.D. in Pharmaceutical/Medicinal Chemistry from the same university. After postdoctoral stays with John W. Daly (1989-1990 and 1992) in the Laboratory of Bioorganic Chemistry at the National Institutes of Health in Bethesda, Maryland, USA, she became Associate Professor of Pharmaceutical Chemistry at Würzburg University in Germany. Since 1998 she is full professor of Pharmaceutical & Medicinal Chemistry at Bonn University and a founder of the Pharma-Center Bonn and the Bonn International Graduate School of Drug Sciences (BIGS DrugS).
Her scientific interests are focused on the medicinal chemistry, structural biology, and molecular pharmacology of purine-binding membrane proteins (purine receptors, ectonucleotidases), orphan G protein-coupled receptors and G proteins, and recently also on coronavirus therapeutics. Disease indications include neurodegenerative and inflammatory diseases, cancer, and infections. She has published more than 500 scientific papers and patents in the field of medicinal chemistry and pharmacology. Among a number of awards, she received the Nauta Pharmacochemistry Award for Medicinal Chemistry and Chemical Biology by the European Federation of Medicinal Chemistry (EFMC) in 2018. Since 2021, she acts as Editor-in-Chief of ACS Pharmacology & Translational Science.
10:20
OC04 - Unravelling the Potential of the Type 2 Lysophosphatidic Acid Receptor (LPA2) for Central Nervous System Pathologies
Prof. Silvia ORTEGA GUTIERREZ
COMPLUTENSE UNIVERSITY OF MADRID, Madrid, Spain
Silvia is currently Associate Professor at Complutense University of Madrid, Spain.
Her lines of research are mainly focused on medicinal chemistry and biological chemistry devoted to the validation and identification of new therapeutic targets as well as on the development of probes for the study of therapeutically relevant proteins. At present, she works in particular on the central nervous system (including the endogenous cannabinoid system and the lysophosphatidic acid receptors) and also on cancer and progeria. Her work has resulted in more than 75 publications in prestigious journals (such as Science, Nat. Neurosci., ACS Cent. Sci., Angew. Chem. Int. Ed. and J. Med. Chem.) and several international patents transferred and in exploitation by the industry. He has also supervised twelve PhD Theses, given invited lectures, and directed several research projects with both public and private funding.
Silvia obtained her PhD at Complutense University of Madrid (Cum Laude and Extraordinary Award). After that, she moved to The Scripps Research Institute (La Jolla, California, USA) with a Fulbright grant and then she joined the Department of Organic Chemistry at the Complutense University as Ramón y Cajal Researcher where she was promoted to Associate Professor in 2016. Her research career has been recognized with the different awards. Among them, stand out the "Young researchers Sigma-Aldrich Award" of the Spanish Royal Society of Chemistry and the "Runner-up Prize for a Young Medicinal Chemist in Academia" by the European Federation of Medicinal Chemistry.
10:40
Coffee Break, Networking & Exhibition
Session 7: Covalent Inhibitors in Drug Discovery
Session chair
Dr Didier ROCHE
EDELRIS, Lyon, France
11:10
PL12 - Development of SARS Coronavirus 3CL Protease Inhibitors with an Electrophilic aryl-ketone Warhead
Prof. Yoshio HAYASHI
TOKYO UNIVERSITY OF PHARMACY AND LIFE SCIENCES, Tokyo, Japan
Yoshio Hayashi is a professor at Tokyo University of Pharmacy and Life Sciences. His research focuses on peptide chemistry and medicinal chemistry. He created several peptide drug candidates such as Plinabulin (Phase III), negamycin derivative, myostatin inhibitory peptide and SARS-CoV 3CL protease inhibitor for the treatment of cancer, genetic disease, muscle disorder and corona viral infection, respectively. In peptide chemistry, he has recently developed efficient reagents in disulfide formation for the synthesis of cyclic peptides and peptide hybrid molecules.
He received his Ph.D. in 1990 from Faculty of Pharmaceutical Science, Kyoto University. After working for two companies, he joined former Professor Yoshiaki Kiso’s group at Kyoto Pharmaceutical University as a lecturer in 2001, and later became an associate professor. In 2007, he became a professor at Tokyo University of Pharmacy and Life Sciences. In 2009, he was awarded the Pharmaceutical Society of Japan Award for Divisional Scientific Promotions.
Currently, he serves as Vice president of the Pharmaceutical Society of Japan (PSJ), Vice chairperson of two Divisions (Organic Chemistry and Medicinal Chemistry) of PSJ, and Trustee of the Japanese Peptide Society.
11:45
PL13 - Inhibitors of the Mitochrondrial Sirtuins 3 and 5
Prof. Christian A. OLSEN
UNIVERSITY OF COPENHAGEN, Copenhagen, Denmark
Christian A. Olsen was born in Copenhagen in 1974. He received his M.Sc. from the Technical University of Denmark in 2000 and his Ph.D. from the Royal Danish School of Pharmacy in 2004. After independently working on the development of novel peptidomimetics, he did his postdoctoral fellowship with Prof. Ghadiri at The Scripps Research Institute. In 2010 he returned to a faculty position at the Technical University of Denmark and in 2014 he accepted his current position as professor at the University of Copenhagen. He is recipient of the Lundbeck Foundation Fellowship (2010), the EFMC award for a young medicinal chemist in academia (2014), and an ERC Consolidator Grant in 2016. His research interests include foldamers, HDAC inhibitors and quorum sensing modulators, as well as investigation of protein lysine acylation.
12:20
Lunch, Networking & Exhibition
12:35
SCHRÖDINGER WORKSHOP (optional but subject to prior registration)
Augmenting Medicinal Chemistry with Digital Chemistry: a CDK2 Inhibitor Design Challenge
13:15
Poster Session II (posters with even), Networking & Exhibition
Session 8: Next Generation of Anti-infective Agents
Session chair
Dr Baptiste VILLEMAGNE
INSERM - UNIVERSITÉ DE LILLE, Lille, France
14:45
PL14 - BacPROTACs Mediate Targeted Protein Degradation in Bacteria
Prof. Francesca Ester MORREALE
THE FRANCIS CRICK INSTITUTE, London, United Kingdom
Dr Francesca Ester Morreale is a Group Leader at the Francis Crick institute (London, UK). Her lab focuses on enabling antibiotic discovery by targeted protein degradation, integrating chemical biology and structural biology.
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Dr Morreale obtained her PhD in Pharmaceutical Sciences in 2014 from the University of Messina (Italy) supervised by Prof. Alba Chimirri. After completing her PhD, she started a postdoc in the group of Prof. Helen Walden at the MRC Protein Phosphorylation and Ubiquitylation Unit (University of Dundee, UK), co-supervised by Prof. Alessio Ciulli. In 2017 Dr Morreale joined the group of Dr Tim Clausen at the Research Institute of Molecular Pathology (IMP) in Vienna, Austria. As a postdoc in the Clausen lab, she led a proof-of-concept study translating targeted protein degradation to bacteria, a technology she is further developing in her independent research group.
15:20
OC05 - Tackling LysS, a New Target for Tuberculosis
Dr Laura A.T. CLEGHORN
UNIVERSITY OF DUNDEE, Dundee, United Kingdom
Dr. Laura Cleghorn is the Tuberculosis Portfolio Manager at the Drug Discovery Unit (DDU) based at the School of Life Sciences, University of Dundee, Scotland. She obtained her BSc (hons) in Chemistry from the University of Edinburgh, following this she became a medicinal chemist working at Organon Laboratories before moving to the University of Leeds to complete a PhD in Chemistry. Laura joined the DDU in 2006 at the point of its inception, initially working as a medicinal chemist working on Human African Trypanosomiasis before changing focus to Tuberculosis (TB) in 2013. She currently leads a team focussed on identifying new chemical series that inhibit TB and with the aim of developing them towards pre-clinical drug candidates.
15:40
OC06 - Historical Evolution and Lessons Learned from an RSV Non Nucleosides Polymerase Inhibitor Program
Dr Sandrine GROSSE
JANSSEN, Beerse, Belgium
Sandrine studied chemistry at the Engineering School of Chemistry of Rennes (ENSCR, France) and completed a PhD in Organic Chemistry at the Institute of Organic and Analytical Chemistry (Orléans, France) under the supervision of Pr. Gérald Guillaumet in collaboration with GreenPharma (Synthesis, functionalization and biological evalution of novel heterocyclic systems. After a short period in production plant (Seqens, France) she joined Janssen Belgium, a company of Johnson and Johnson in 2014. She contributed to and led several hit-to-lead and lead optimization projects mainly in the areas of respiratory diseases or hepatitis. Her work has resulted in 15 published international patents and 8 articles.
16:00
Coffee Break, Networking & Exhibition
16:30
PL15 - Metallo-Enzymes - From Functions to Drugs
Prof. Christopher J. SCHOFIELD
UNIVERSITY OF OXFORD, Oxford, United Kingdom
Chris Schofield studied for a degree in chemistry at the University of Manchester (1979-1982). In 1982 he moved to Oxford for DPhil studies with Jack Baldwin on the synthesis and biosynthesis of antibiotics. In 1985 he became a Departmental Demonstrator in the Dyson Perrins Laboratory, and in 1990 Lecturer in Chemistry and Fellow of Hertford College. In 1998 he became Professor of Chemistry; from 2011-2021 he was Head of Organic Chemistry at Oxford. He is presently Director of Chemistry at the Ineos Oxford Institute for Antimicrobial Research (IOI). He is a Fellow of the Royal Society. His research group works at the interface of chemistry, biology and medicine. His work has opened up new fields in antibiotic research, oxygen sensing and gene regulation in organisms ranging from bacteria to plants and animals; it has helped enable discovery of new medicines.
Session 9: Small Molecules for Immunooncology or Autoimmunity
Session chair
Prof. Rebecca DEPREZ-POULAIN
INSERM - UNIVERSITÉ DE LILLE / INSTITUT PASTEUR OF LILLE, Lille, France
17:05
PL16 - Discovery of the Clinical Candidate ACT-777991, a Potent CXCR3 Antagonist with Therapeutic Potential in Autoimmune Diseases
Dr Eva CAROFF
IDORSIA PHARMACEUTICALS LTD, Allschwil, Switzerland
Eva Caroff studied science focusing on mathematics, physics and chemistry and obtained a MSc in Chemistry from the Haute Alsace University, France, combined with a Chemistry Engineering Diploma from the Ecole Nationale Superieure de Chimie de Mulhouse, France, in 1997. She performed her PhD studies under the supervision of Prof. W. D. Woggon at the Institute of Organic Chemistry in Basel, Switzerland.
Following post-doctoral studies in the group of Prof. S. Roberts at Liverpool University, UK, and at Axovan AG in Allschwil, Switzerland, Dr. Caroff joined Actelion Pharmaceuticals Ltd. in Allschwil, Switzerland, as a medicinal chemist, in 2003. Dr. Caroff started her career as a laboratory head and project leader, and evolved as a group leader, now working since 2018 at Idorsia Pharmaceuticals Ltd in Allschwil, Switzerland. As project leader, together with her team, Dr. Caroff discovered 2 molecules that are now undergoing clinical studies, namely selatogrel (phase 3 ongoing) and ACT-777991 (phase 1 completed).
Dr. Caroff and her group continue to aim at identifying novel drugs interfering with biological mechanisms associated with immune diseases. Dr. Caroff has published approx. 30 scientific papers and patent applications.
17:40
OC07 - Discovery of an Oral, Rule-of-5 Compliant, IL-17A Protein-Protein Interaction Modulator (IL-17A PPIm) for the Treatment of Psoriasis and other Inflammatory Diseases.
Dr Mark D. ANDREWS
LEO PHARMA, Ballerup, Denmark
After completing a DPhil in organic chemistry with Dr Mark Moloney at Oxford in 1995 I moved to Canada for 2 years, carrying out post-doctoral research with Prof. John Vederas at the University of Alberta. Returning to the UK, I spent a year as a temporary lecturer in organic chemistry at the University of Bristol, working with Prof. Tim Gallagher, before joining Pfizer at their Sandwich research site in 1998. At Pfizer I worked as a medicinal chemist on numerous targets across several therapeutic areas (Sexual Health, Obesity, Pain), helping to deliver clinical candidates and potential candidates for SSRIs, 5HT2C, MC4, TRPM8 and TRK (Tropomyosin receptor kinase).
Following the closure of Pfizer’s Sandwich site in 2011 I stayed in East Kent and joined Peakdale (now Concept life sciences), where I spent 3 years. In 2015, I moved to LEO pharma in Denmark, where I am now a Senior Principal Scientist, with responsibilities as a Medchem Lead/Project Lead, helping LEO discover new, safe and effective medicines to treat skin diseases.
I am a named inventor on 26 patents and an author of 31 papers/book chapters.
18:00
OC08 - Small-Molecule Inhibitor Targeting PD-1/PD-L1 Interaction Restores T-Cell Function
Prof. Helena FLORINDO
IMED - UNIVERSITY OF LISBON, Lisbon, Portugal
Helena Florindo graduated in Pharmaceutical Sciences in 2003 (University of Lisbon) and obtained her Ph.D. degree in Pharmaceutical Technology in 2008 (University of Lisbon), in collaboration with the University of London.
Currently, she is an Associate Professor with tenure and habilitation in the department of Pharmacy, Pharmacology, and Health Technologies at the Faculty of Pharmacy, University of Lisbon. Since 2015, she is the head of the BioNanoSciences – Drug Delivery & Immunoengineering Research Group, at the Research Institute for Medicines (iMed.ULisboa), University of Lisbon.
Helena is also a member of the Portuguese Medicines Agency Evaluation Board (INFARMED) and an expert to the European Medicines Agency (EMA), thus supporting the evaluation of marketing authorization procedures for new drugs and biologics. This knowledge also guides her research, which has been motivated by the immune-oncology field toward the rational development of functionalized nano/biomaterials as novel immunotherapies for cancer treatment. It includes the characterization of the anti-tumor effects induced by the combination of nano-vaccines with nano-therapeutics, including small molecules, designed to modulate the functions of key cells within tumor microenvironment, such as T cells, myeloid-derived cells, and tumor cells.
18:20
20:00
Symposium Banquet (subject to prior registration)