Revisiting Freidinger Lactam for the Development of Bioactive Foldamers
Prof. Muriel AMBLARD
CNRS-UNIVERSTY OF MONTPELLIER I, Montpellier, France Read more
Prof. Muriel AMBLARD
Dr Muriel AMBLARD is a CNRS Research Director at the « Institut of Biomolecules Max Mousseron » (IBMM) in Montpellier. After completing her PhD in Organic Chemistry at the University of Montpellier in the Lab of Prof Jean Martinez, she joined the group of Dr Paul Anderson at Merck Sharp & Dohm in USA as a post-doctoral fellow. In 1996, she received a position at the Laboratory of Amino Acid Peptide and Proteins in Montpellier and became a team leader at the IBMM in 2007. Her research interests are mainly at the interface of chemistry, biology and analysis. She developed a number of potent receptor agonists and antagonists of several peptide hormones. Her recent work focuses on the design and synthesis of predictable and stable ribbon and helical molecular architectures that are applied to the identification of cell penetrating compounds and inhibitors of protein/protein interactions. Another part of her research interest is devoted to the development of peptide-based biopolymers by new approaches relying on bottom up polymerization of peptide-activated monomers.
Chemical Physiology of Antibody Conjugates and Natural Products
Dr Goncalo BERNARDES
INSTITUTO DE MEDICINA MOLECULAR, PORTUGAL & UNIVERSITY OF CAMBRIDGE, Cambridge, United Kingdom Read more
Dr Goncalo BERNARDES
After completing his D.Phil. degree in 2008 at the University of Oxford, U.K., he undertook postdoctoral work at the Max-Planck Institute of Colloids and Interfaces, Germany, and the ETH Zürich, Switzerland, and worked as a Group Leader at Alfama Lda in Portugal. He started his independent research career in 2013 at the University of Cambridge as a Royal Society University Research Fellow, and in 2018 he was appointed University Lecturer. His research group interests focus on the use of chemistry principles to tackle challenging biological problems for understanding and fight cancer.
Complex Glycans in Health and Disease
Prof. Geert-Jan BOONS
UTRECHT UNIVERSITY, Utrecht, The Netherlands Read more
Prof. Geert-Jan BOONS
Geert-Jan Boons is the UGA Foundation Distinguished Professor in Biochemical Sciences at the Department of Chemistry and the Complex Carbohydrate Research Center (CCRC) of the University of Georgia (USA) and Professor and Chair of the Department of Medicinal and Biological Chemistry of Utrecht University (The Netherlands). He received a B.S. and Ph.D. in Chemistry from the Leiden University (The Netherlands) and spent seven years in the UK, first as a postdoctoral fellow at Imperial College, London, and the University of Cambridge, and then as a lecturer and professor at the University of Birmingham. In 1998, he joined the faculty of the Department of Chemistry and CCRC of the University of Georgia, and in 2015 he accepted an academic appointment at Utrecht University. Among others, he has received the Creativity in Carbohydrate Science Award by the European Carbohydrate Association (2003), the Horace Isbell Award by the Division of Carbohydrate Chemistry of the American Chemical Society (ACS) (2004), the Roy L. Whistler International Award in Carbohydrate Chemistry by the International Carbohydrate Organization (ICO) (2014), the Hudson Award (2015), and the Cope Mid Career Scholar Award from the ACS (2016). His research program deals with the synthesis and biological functions of carbohydrates and glycoconjugates. The diversity of topics to which the group has significantly contributed includes the development of new and better methods for synthesizing exceptionally complex carbohydrates and glycoconjugates. A hallmark of Dr. Boons’ research program is to employ chemical synthesized target compounds for biological and biomedical explorations and in particular, his research group has made important contributions to the understanding of immunological properties of complex oligosaccharides and glycoconjugates at the molecular level. A highlight of such program has been the design, chemical synthesis, and immunological examination of three-component vaccine candidates that offer a prospect to be employed as a therapeutic vaccine for many types of epithelial cancer.
Modulating Different Components of the Ubiquitin System with Small Molecules and Cyclic Peptides
Prof. Ashraf BRIK
TECHNION-ISRAEL INSTITUTE OF TECHNOLOGY, Haifa, Israel Read more
Prof. Ashraf BRIK
Ashraf Brik is a Professor of Chemistry at the Schulich Faculty of Chemistry in the Technion-Israel Institute of Technology. Professor Brik received his B.Sc. in Chemistry from the Ben-Gurion University of the Negev (1996) and his M.Sc. degree in Organic Chemistry from the Technion-Israel Institute of Technology (1998). His Ph.D. was obtained in 2001 from the Faculty of Chemistry in the Technion in Bioorganic Chemistry. From 2002 to 2006, Professor Brik was a Research Associate in the Scripps Research Institute. In 2007, Professor Brik joined the Department of Chemistry in the Ben-Gurion University of the Negev as an Assistant Professor and was promoted to an Associate Professor in 2011 and to a Full Professor in 2012. In 2015, Professor Brik Joined the Schulich Faculty of Chemistry in the Technion. Brik is well known for his contributions for the development of chemical approaches to prepare posttranslationally modified proteins for biochemical, biophysical and functional analyses. Professor Brik is the recipient of the Bessel Award of the Humboldt Foundation for 2015, the 11th Hirata Award, Teva Award for Excellence in memory of Eli Hurvitz for 2013, the Tetrahedron Young Investigator Award in Bioorganic and Medicinal Chemistry for 2013 and the 2011 Israel Chemical Society prize for Outstanding Young Chemist.
The Influence of Free Ligand Conformations on Mcl-1 PPI Inhibition
Current position: Associate Principal Scientist, Oncology Chemistry, AstraZeneca (since 2015)
Research Field: Structural Chemistry + NMR spectroscopy in Drug Discovery
• 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
Carbohydrate-Lectin Interactions - What Makes Them Unique?
Beat Ernst, Professor em. of the Department of Pharmaceutical Sciences, has been at the University of Basel since 1998. His research interests lie at the interface between carbohydrate chemistry and glycobiology, with a particular focus on the synthesis of glycomimetics and their pharmacological profiling.
After studying chemistry at the ETH Zürich, he spent two years as a post-doctoral associate at the California Institute of Technology in Pasadena, CA. In 1981, he joined Ciba-Geigy’s Central Research Laboratories in Basel and after the merger with Sandoz moved to Transplantation Research within Novartis Pharma AG. Beat Ernst received the Werner Prize of the Swiss Chemical Society in 1991, became Ciba Fellow for his contributions to natural product synthesis in 1993, and was awarded with the Phoenix Pharmacy Science Award in 2013.
Empowering Cancer Target Validation with High Quality Chemical Probes
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).
Identification of S 64315, a Potent and Selective Mcl-1 Inhibitor through Fragment-based Drug Discovery
Dr Andras KOTSCHY
SERVIER RESEARCH INSTITUTE OF MEDICINAL CHEMISTRY, Budapest, Hungary Read more
Dr Andras KOTSCHY
András Kotschy is the managing director of the Servier Research Institute of Medicinal Chemistry in Budapest, Hungary. After completing his PhD degree he joined the staff of Eötvös Loránd University where he rose through the ranks to associate professor also completing his habilitation and obtaining a DSc degree. In 2007 he moved to the newly established Servier Research Institute of Medicinal Chemistry as director of the Discovery Chemistry division and in 2015 became director of the institute. He is the author of 57 refereed publications that received over 1200 citations, 1 book, 2 book chapters, and 15 patents. He is also the recipient of multiple scientific awards and fellowships.
Increasing Brain Exposure of Therapeutic Antibodies
Dominique Lesuisse is Head of the CNS Barriers Research group in the Rare and Neurologic Disease Therapeutic Area at Sanofi,based in Chilly Mazarin, France.
Dominique received a B.Sc. and a Ph.D. in Organic Chemistry from the University of Louvain, Belgium in the lab of Léon Ghosez. She then spent 2 years at the University of Irvine, California in Larry Overman’s lab and 2 years at MIT in Glenn Berchtold’s lab as a postdoctoral fellow.
In 1987, Dominique joined Roussel-Uclaf, a French Pharmaceutical company which evolved into Sanofi after several successive mergers. She has been managing medicinal chemistry departments in the different organizations giving rise to over 14 candidates to development (one is on the market). She has published over 45 articles and book chapters, along with 36 patents. She is member of several Editorial Boards and Vice-President of the Therapeutic Chemistry Society. Among other recognitions, in 2017, Dominique was honored by the French Chemistry Society for her work in drug discovery and development.
Massively Multi-target Profile-QSAR: IC50 Predictions Comparable to 4-Concentration Experiments for most Novartis Assays
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.
What Makes a Great Medicinal Chemist: Some Fresh Thoughts
Dr Mark MURCKO
RELAY THERAPEUTICS, Cambridge, United States Read more
Dr Mark MURCKO
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
- Interim CSO, Relay Therapeutics
- Chief Technology Officer, Vertex Pharmaceuticals
- Senior Scientist, Merck Sharpe & Dohme
Cysteine Arylation to Engineer, Deliver, and Discover Proteins
Prof. Bradley Lether PENTELUTE
MASSACHUSETTS INSTITUTE OF TECHNOLOGY, Cambridge, United States Read more
Prof. Bradley Lether PENTELUTE
Bradley L. Pentelute, Associate Professor of Chemistry. He is also an Associate Member, Broad Institute of Harvard and MIT, an Extramural Member of the MIT Koch Cancer Institute, and Member, Center for Environmental Health Sciences MIT. He received his undergraduate degree in Psychology and Chemistry from the University of Southern California, and his M.S and Ph.D. in Organic Chemistry from the University of Chicago with Prof. Steve Kent. He was a postdoctoral fellow in the laboratory of Dr. R. John Collier at Harvard Medical School, Microbiology.
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 Read more
Dr Hasane RATNI
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.
Andrea Rentmeister studied chemistry at the TU Graz and at the University of Bonn. She received her PhD in 2007 from the University of Bonn under the supervision of Prof. Michael Famulok and was a postdoctoral scholar in the group of Prof. Frances H. Arnold at the California Institute of Technology from 2007-2010. After a junior professorship at the University of Hamburg from 2010-2013, she became Professor of Biochemistry within the Cluster of Excellence “Cells in Motion” at the University of Münster. Research in her group focuses on RNA biochemistry at the interface of chemistry and biology and is directed to understand and control processes affecting RNA expression and turnover at the molecular level.
Click-Cleavable Antibody-Drug Conjugates
Dr Marc ROBILLARD
TAGWORKS PHARMACEUTICALS, Eindhoven, The Netherlands Read more
Dr Marc ROBILLARD
Marc Robillard is founder and CEO of Tagworks Pharmaceuticals, a spin-out of Philips Healthcare, originating from its molecular imaging expertise. Tagworks develops in vivo chemistry to improve the efficacy of cancer therapies and to enable novel approaches in companion diagnostics. Prior to spinning out in 2011 he worked at Philips Research on molecular imaging and drug delivery and at Kreatech Diagnostics on microarray detection. Marc obtained his MSc and PhD in bio(in)organic chemistry at, respectively, the University of Groningen and the Leiden Institute of Chemistry, The Netherlands.
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.
Title to be announced
Dr Marwin SEGLER
BENEVOLENTAI, London, United Kingdom
Paul Ehrlich Award Lecture - Chemotype, Phenotype, Target
Prof. Herbert WALDMANN
MAX PLANCK INSTITUTE OF MOLECULAR PHYSIOLOGY, Dortmund, Germany Read more
Prof. Herbert WALDMANN
Herbert Waldmann was born in Neuwied, Germany and studied chemistry at the University of Mainz where he received his PhD in organic chemistry in 1985 under the guidance of Horst Kunz. After a postdoctoral appointment with George Whitesides at Harvard University, he completed his habilitation at the University of Mainz in 1991. In 1999 he was appointed Director at the Max Planck Institute of Molecular Physiology Dortmund and Professor of Organic Chemistry at the University of Dortmund. His research interests lie in the syntheses of signal transduction modulators and the syntheses of natural product inspired compound libraries and their biological evaluation.
He has been the recipient of the Friedrich Weygand Award for the advancement of peptide chemistry, of the Carl Duisberg Award of the Gesellschaft Deutscher Chemiker, the Otto-Bayer-Award, the Steinhofer Award of the Steinhofer Foundation, the Max Bergmann Medal, the GSK Award on Chemical Biology, the Hans-Herloff Inhoffen-Medal, the Emil-Fischer-Medal, he is a Member of „Deutsche Akademie der Naturforscher Leopoldina, Halle/Saale“, of the NRW Akademie der Wissenschaft und der Künste and since 2005 he is a Fellow of the Royal Society of Chemistry. In 2014 he received the Honorary Doctorate (Dr. h. c.) bestowed by Leiden University, NL.
Unlocking Drug Discovery Power through Collaborative Efforts between Academia and CRO : Bringing Novel Tankyrase Inhibitors towards the Clinic
Dr Anita WEGERT
MERCACHEM-SYNCOM, Nijmegen, The Netherlands Read more
Dr Anita WEGERT
Dr. Anita Wegert is a Director Medicinal Chemistry at Mercachem with extensive knowledge in Medicinal Chemistry regarding GPCRs, PPIs, epigenetic targets and anti-infectives. Currently, she is leading various projects from hit to lead up to the development of preclinical candidates.
A major interest is currently the work in a collaborative team with Stefan Krauss from the University Hospital Oslo, Lari Letio from the University of Oulo and with Marc Nazare from the FMP in Berlin to develop new inhibitors of tankyrase 1 and 2, which are central biotargets in the WNT/β-catenin signalling pathway. In particular, the recently described role of the WNT/β-catenin pathway in regulating immune cell infiltration in the tumour micro-environment suggests an impact of the pathway on immunotherapy, an area of significant developmental focus.
Before joining Mercachem in 2014 Anita Wegert gained extensive experience as a lab head and project leader at Grünenthal, Aachen in the disease area pain.
Therapeutic Potential of Macrocyclic ALK2 Inhibitors
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:
. 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
Dr. Chevrel, after graduating from the ‘INSA Lyon’ engineering school with a specialty in Biotechnology, integrated the Paris Sud University PhD program and acquired extensive training in protein engineering focused on alternative protein scaffolds. Following a brief experience in the pharma industry for the development of analytical QC for biologics, she joined the scientific team of Affilogic in 2015 with the aim of developing innovative therapeutic products based on Nanofitins®. Today, Mrs. Chevrel, applies her protein engineering skills to propose original approaches based on Nanofitins® technology and manage preclinical research programs with international pharmaceuticals partners.
Tackling a Unique S1 Protease by SBDD. Discovery of Highly Potent & Selective Factor D Inhibitors
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.