Interfacing Chemical Biology and Drug Discovery

Pierre Fabre Award Lecture - Metal Complexes in Medicinal Chemistry (PL19)

Dr Gilles GASSER

CHIMIE PARISTECH, PSL UNIVERSITY, Paris, France
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Dr Gilles GASSER

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http://www.gassergroup.com

Gilles Gasser was born, raised and educated in Switzerland. After a PhD thesis in supramolecular chemistry with Prof. Helen Stoeckli-Evans (University of Neuchâtel, Switzerland), Gilles undertook two post-docs, first with the late Prof. Leone Spiccia (Monash University, Australia) in bioinorganic chemistry and then as an Alexander von Humboldt fellow with Prof. Nils Metzler-Nolte (Ruhr-University Bochum, Germany) in bioorganometallic chemistry. In 2010, Gilles started his independent scientific career at the University of Zurich as a Swiss National Science Foundation (SNSF) Ambizione Fellow before obtaining a SNSF Assistant Professorship in 2011. In 2016, Gilles moved to Chimie ParisTech, PSL University (Paris, France) to take a PSL Chair of Excellence.

Paul Ehrlich Award Lecture - 30 Years of Molecular Glues: Controlling Cell Circuitry in Biology and Medicine (PL12)

Prof. Stuart SCHREIBER

HARVARD UNIVERSITY, Cambridge, United States
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Prof. Stuart SCHREIBER

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http://www.broadinstitute.org/chembio/lab_schreiber/home.php

Stuart Schreiber is a co-Founder of the Broad Institute, the Morris Loeb Professor of Chemistry and Chemical Biology at Harvard University, and is a member of the National Academy of Sciences, National Academy of Medicine and American Academy of Arts and Sciences.

His lab integrates chemical biology and human biology to advance the science of therapeutics. He is known for having developed systematic ways to explore biology, especially disease biology, using small molecules and for his role in the development of the field of chemical biology. Key advances include the discoveries of mTOR, histone deacetylases and evidence that chromatin marks regulate gene expression, and small molecules that promote protein–protein interactions. His research has been acknowledged through awards including most recently the Wolf Prize in Chemistry. His approach to therapeutics discovery guided the development of many biotechnology companies including Vertex Pharmaceuticals and Ariad Pharmaceuticals.

Chemical Targeting of DNA and Histone Methylationto Reprogram Cells in Human Diseases: Challenges and Future Perspectives (PL04)

Dr Paola B. ARIMONDO

INSTITUT PASTEUR - CNRS, Paris, France
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Dr Paola B. ARIMONDO

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Dr Paola B. Arimondo studied Chemistry at the University of Pisa (Scuola Normale Superiore, Italy) and received her Ph.D in Biophysics at the MNHN in Paris. Paola Arimondo is Director of Research at CNRS and her research focuses on the interactions between nucleic acids and proteins and their modulation by small chemical molecules. In particular, after a six-month sabbatical in 2005 at the University of California in Berkeley, she develops innovative chemical strategies aiming at the epigenetic control of gene expression in cancers. In 2011, Paola Arimondo was recruited to lead the Laboratory of Epigenetic Targeting of Cancer (ETaC) USR3388, a 5-years joint public-private Laboratory between the CNRS and Pierre Fabre Laboratories, in Toulouse, France. She developed projects at the interface of Chemistry and Biology to discover chemical modulators of DNA and histone methylation in cancer. In 2016, she was appointed Oversea Fellow at the Churchill College in Cambridge UK. In 2018 she started the Epigenetic Chemical Biology Unit at the Institut Pasteur, where she continues to explore the chemical targeting of the epigenetic regulation to fight human diseases. Her research focus now spans beyond cancer, to the field of infectious diseases.

Multi-Target-Directed Ligands to Combat Neurodegenerative Diseases: All-In-One and One-For-All (PL10)

Prof. Maria Laura BOLOGNESI

UNIVERSITY OF BOLOGNA, Bologna, Italy
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Prof. Maria Laura BOLOGNESI

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Maria Laura Bolognesi is Professor of Medicinal Chemistry, Director of the Chemistry and Pharmaceutical Technologies degree program and Rector Delegate for Latin American International Relations at the University of Bologna. She obtained her PhD under the mentorship of Professor Carlo Melchiorre in 1996 and carried out postdoctoral work at the University of Minnesota with Professor Philip S. Portoghese. Her research explores the development of small molecules in the neurodegenerative and neglected tropical disease therapeutic areas. Maria Laura 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 an Associate Editor of Journal of Medicinal Chemistry and serves in the Advisory Board of the European Federation of Medicinal Chemistry

Daridorexant - a Dual Orexin Receptor Antagonist (PL09)

Dr Christoph BOSS

IDORSIA PHARMACEUTICALS LTD, Basel, Switzerland
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Dr Christoph BOSS

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Christoph Boss is Vice President, Head of Drug Discovery Chemistry

Education:
PhD, synthetic organic chemistry at the University of Bern, Switzerland followed by post-doctoral training at The Scripps Research Institute (TSRI) in LaJolla, California, USA.

Professional background:
From 1999 until 2012, various positions of increasing responsibility in Actelion's drug discovery chemistry department contributing to the identification of several lead compounds including macitentan for PAH and ACT-541468 for insomnia. Senior Group Leader Chemistry Technologies 2012-2017. Joined Idorsia when the company was established in June 2017 as a Senior Group Leader in Drug Discovery Chemistry. Head of Drug Discovery Chemistry at Idorsia since July 2019.

The Second Dimension of the Genetic Code (PL05)

Prof. Thomas CARELL

LUDWIG-MAXIMILIANS-UNIVERSITY, München, Germany
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Prof. Thomas CARELL

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http://www.cup.uni-muenchen.de/oc/carell/

Thomas Carell was born in Herford (Germany) in 1966. He is married and father of three children. His academic career in chemistry began at the Universities of Münster and Heidelberg. In 1993, he obtained his doctorate with Prof. H. A. Staab at the Max-Planck Institute of Medical Research. After postdoctoral training with Prof. J. Rebek at MIT (Cambridge, USA) from 1993 – 1995, Thomas Carell moved to the ETH Zürich (Switzerland) into the group of Prof. F. Diederich to start independent research. He obtained his habilitation in 1999. In 2000, he accepted a full professor position for Organic Chemistry at the Philipps-Universität in Marburg (Germany). In 2004, he moved to the Ludwig-Maximilians-Universität (LMU) in Munich (Germany) where he is heading a research group in chemical biology focused to analyze the chemistry of epigenetic programming in DNA and RNA. Thomas Carell is a member of the German National Academy Leopoldina and of the Berlin-Brandenburgische Academy of Arts and Sciences. He is the recipient of the Cross of Merit from the Federal Republic of Germany.

Bioorthogonal Protein Activation in Living Systems (PL03)

Prof. Peng CHEN

PEKING UNIVERSITY, Beijing, China
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Prof. Peng CHEN

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- Peng Chen, Professor of Chemical Biology, Peking University, Beijing, China
- Chemical Biology, Bioorthogonal Reactions
2014-present, Professor of Chemical Biology, Peking University
2009-2014, Investigator of Chemical Biology, Peking University
2007-2009, Postdoctoral Scientist, The Scripps Research Institute
2002-2007 Ph.D in Chemistry, The University of Chicago
1998-2002 B.S. in Chemistry, Peking University

Recent Advances In Breast Cancer Treatment: Discovery of Amcenestrant (SAR439859), An Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) to Treat ER+ Breast Cancers (PL08)

Dr Youssef EL AHMAD

SANOFI, Vitry Sur Seine, France
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Dr Youssef EL AHMAD

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Youssef El Ahmad is a Group leader of Medicinal Chemistry at Sanofi. After a MsC degree from Lebanese University and a PhD in Pharmaceutical Sciences from the Faculty of Pharmacy of Paris XI University, he joined the Medicinal Chemistry department at Sanofi 30 years ago. During his career, he supports and leads projects in CNS, anti-infective and oncology fields and contributes to the development of several clinical candidates especially for cancer treatment. In this congress, he presents the “Recent Advances in Breast Cancer Treatment: Discovery of SAR439859, a Selective Estrogen Receptor Degrader for the Treatment of Estrogen-Receptor-Positive Breast Cancer”.

Proteomimetics as Inhibitors of Transcription Factor Complexes (PL15)

Prof. Tom GROSSMANN

VU UNIVERSITY AMSTERDAM, Amsterdam, The Netherlands
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Prof. Tom GROSSMANN

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Tom Grossmann holds the Chair of Biomimetic Chemistry at the VU University Amsterdam. He studied chemistry at the Humboldt University Berlin, including undergraduate research with Peter Vollhardt at the University of California Berkeley. In 2008, he received his PhD with Oliver Seitz at the Humboldt University Berlin. After postdoctoral research in the group of Gregory Verdine at Harvard University, he became group leader at the Technical University and the Chemical Genomics Centre in Dortmund. Since 2016, he is full professor at the VU University Amsterdam, currently being supported by an ERC Starting Grant.

Ligand-Directed Labeling of Endogenous Proteins in Live Cells (PL02)

Prof. Itaru HAMACHI

KYOTO UNIVERSITY, Kyoto, Japan
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Prof. Itaru HAMACHI

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Itaru Hamachi was born in Fukuoka Prefecture, Japan, in 1960 and received his Ph.D. in 1988 from Kyoto University under the guidance of the late Professor Iwao Tabushi. Immediately thereafter he joined Kyushu University, where he worked as an assistant professor for 3 years in Kunitake laboratory and became an associate professor in Shinkai laboratory in 1992. In 2001, he became a full professor of IFOC, Kyushu University and then moved to Kyoto University in 2005.

He had been a PRESTO investigator for 7 years (from 2000 to 2006), a team leader of two CREST projects (from 2008 to 2013 and then from 2013 to 2018) and has been ERATO research director (from2018 to 2023) which all are supported by Japan Science and Technology (JST) Agency. He is now a supervisor of a PRESTO project (Single cell analysis) in JST program from 2014-2019.

His research interests include live-cell organic chemistry, chemical biology, bioorganic and bioinorganic chemistry, and supramolecular biomaterials.

Selecting Targets to Harness the Therapeutic Opportunities Afforded by PROTAC-mediated Protein Degradation (PL14)

Dr John HARLING

GLAXOSMITHKLINE, Stevenage, United Kingdom
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Dr John HARLING

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I conducted both my B.Sc and Ph.D at Imperial followed by two years as a Postdoctoral Researcher at the University of Texas at Austin. Joined GlaxoSmithKline (then SmithKlineBeecham) as a Medicinal Chemist in 1991. During my >25 years at GSK I have worked in programs spanning Neurosciences, Cardiovascular and Respiratory therapeutic areas. In 2007 I was appointed as a Medicinal Chemistry Department Head in the Respiratory therapeutic area. In 2012 I became involved in the initiation of an exploratory effort to assess the potential of a new protein degradation technology through collaboration with Professor Craig Crews at Yale. My current position is Senior Scientific Director within Medicinal Chemistry at GSK where I have a remit to develop protein degradation capability at GSK.

Expanding the Genetic Code - Chemistry in Living Systems (PL01)

Prof. Kathrin LANG

ETH ZURICH, Zurich, Switzerland
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Prof. Kathrin LANG

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Kathrin Lang studied Chemistry at the University of Innsbruck, Austria where she obtained a PhD in 2008 working on chemically modified RNA to study ribosome catalysis and riboswitch folding. After postdoctoral research in the group of Venki Ramakrishnan on ribosome crystallography and in the lab of Jason Chin on synthetic biology at the MRC-LMB in Cambridge, UK, she was appointed in 2014 as a Rudolf Mössbauer Tenure Track Professor at the Technical University of Munich, Germany, where she was tenured and promoted to permanent W3 Professor for Synthetic Biochemistry in 2020. Since April 2021 she is Full Professor of Chemical Biology at the ETH Zürich, Switzerland. Her general research interests lie in the interdisciplinary area between Chemistry and Biology, applying concepts from Organic Chemistry to develop new tools to study and control biological systems. Her group is especially active in enabling and advancing approaches to expand the genetic code and in developing new in vivo chemistries that are amenable to physiological conditions, a combination that is ideally suited to address unmet challenges in studying and manipulating biological processes with a new level of spatial, temporal and molecular precision.

Converting Drug Delivery Technologies into Drugs in Unmet Medical Needs (PL11)

Prof. Jean-Christophe LEROUX

ETH ZÜRICH, Zürich, Switzerland
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Prof. Jean-Christophe LEROUX

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Jean-Christophe Leroux is full professor of Drug Formulation and Delivery at the Institute of Pharmaceutical Sciences at ETH Zurich, Switzerland. He was trained as pharmacist at the University of Montreal (Canada), obtained his Ph.D. in Pharmaceutical Sciences from the University of Geneva (Switzerland) and worked as postdoctoral fellow at UCSF (USA). Dr. Leroux was professor of Pharmaceutical Technology at the University of Montreal from 1997 to 2008. He has made important fundamental and applied contributions to the fields of biomaterials and drug delivery, and has also been involved in the development of innovative bio-detoxification systems. He is a fellow of the AAPS and the CRS, and the co-founder of Versantis AG and Inositec AG, two start-up pharmaceutical companies.

Biomimetic Chemistry of Human RNAi Therapeutics (PL18)

Dr Muthiah MANOHARAN

ALNYLAM PHARMACEUTICALS, Cambridge, United States
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Dr Muthiah MANOHARAN

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Dr Muthiah (Mano) Manoharan serves as a Senior Vice President of Drug Innovation, a Scientific Advisory Board Member, and a Distinguished Research Scientist at Alnylam Pharmaceuticals, Cambridge, Massachusetts, USA. Dr. Manoharan has had a distinguished career as a world-leading chemist in the areas of oligonucleotide chemical modifications, conjugation chemistry, and delivery platforms (lipid nanoparticles, polymer conjugates, and complex-forming strategies). Dr. Manoharan and his research group designed, synthesized and demonstrated for the first time the human therapeutic applications of GalNAc-conjugated oligonucleotides at Alnylam, a platform that has revolutionized the nucleic acid-based therapeutics field with several compounds presently in the advanced clinical trials. He is an author of more than 215 publications (nearly 44,000 Google Scholar citations with an h-index of 96 and an i10-index of 375) and over 400 abstracts, as well as an inventor of over 240 issued U.S. patents.

Dr. Manoharan earned his Ph.D. in chemistry at the University of North Carolina, Chapel Hill with Professor Ernest Eliel in Organic Chemistry. He started working in the field of oligonucleotides at Yale University as a post-doctoral research associate with Professor John Gerlt.

Dr Manoharan has been recognized as the Lifetime Achievement Awardee of the Oligonucleotide Therapeutics Society for the year 2019. He received the M. L. Wolfrom Award from the American Chemical Society in 2007.

Drugging KRAS with Medchem 2.0 (PL16)

Dr Darryl MCCONNELL

BOEHRINGER INGELHEIM, Austria
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Dr Darryl MCCONNELL

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Darryl McConnell is currently Senior Vice President and Research Site Head at Boehringer-Ingelheim Regional Centre Vienna, Austria. His goal is to discover new chemical therapeutics for cancer’s so-called undruggable targets together with the team at BI.

Darryl’s interests lie in drugging protein-protein interactions, kinases and pushing the frontiers of PROTACs for cancer patients. Fragment screening, protein crystallography, protein NMR, drug resistance, agile methods in drug discovery and natural product inspired medicinal chemistry are some of his areas of scientific interest.

Darryl commenced his career with Boehringer-Ingelheim in 2002 as a Research Laboratory Head and is in his current role since 2015. Prior to this Darryl has worked for Intervet in Vienna from 2001, for Biota Holdings Ltd in Melbourne, Australia from 1999 in the area of respiratory viruses and Chiron Technologies in Melbourne from 1997.

Darryl McConnell received his Bachelor of Science with First Class Honours in 1991 with Professor John Elix at the Australian National University in Canberra. He performed his PhD at the University of New South Wales in Sydney with Professor David Black for which he was awarded the Cornforth Medal for the best chemistry PhD thesis in Australia for that year. Following this he performed a 2 year Postdoctoral study at the University of Sydney with Professor Leslie Field in organometallic chemistry.

Steroid Sulfatase Inhibition: from Concept to Clinical and Beyond (PL07)

Prof. Barry POTTER

UNIVERSITY OF OXFORD, Oxford, United Kingdom
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Prof. Barry POTTER

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Barry Potter studied Chemistry at Oxford, completing a DPhil on enzyme-catalyzed phosphoryl transfer stereochemistry with a DSc in 1993. After postdocs in Oxford and at the Max-Planck-Institute in Göttingen, he was lecturer in Biological Chemistry at Leicester, winning a Lister Institute Fellowship, then moved to the chair of Medicinal Chemistry at Bath. Research interests are in mechanistic enzymology, signal transduction chemistry and anticancer drug discovery. He has published over 550 papers, is inventor of 45 granted US patents and has brought academically-discovered drugs to multiple human clinical trials with clinical benefit. In 2015 he became Professor of Medicinal & Biological Chemistry at Oxford. He has won four interdisciplinary RSC medals, the GSK International Achievement Award, a European Life Science Award, held the 2015 RSC Medicinal Chemistry Endowed Lectureship and won the 2018 Tu Youyou Award for his work in Medicinal and Natural Product Chemistry. He was elected to the Academy of Medical Sciences and Academia Europaea.

From Simple to Complex in Natural Product Chemistry: Bio-Inspired Strategies to Escape “Flatland” (PL06)

Prof. Erwan POUPON

PARIS-SACLAY UNIVERSITY, Châtenay-Malabry, France
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Prof. Erwan POUPON

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Erwan Poupon is full professor of natural product chemistry at Paris-Saclay University. He obtained his PharmD from the University of Rennes in 1996 and his PhD from Paris-Descartes University in 2000 under the guidance of Pr Henri-Philippe Husson and Dr Nicole Kunesch. After a post-doctoral period in the group of Pr Emmanuel Theodorakis (University of California in San Diego, USA), he joined the faculty at Paris-Sud University and BioCIS. He is particularly interested in understanding mechanisms involved in the biosynthetic pathways of specialized metabolites and leading to high levels of molecular complexity. Other interests include chemical ecology, chemical evolution and the discovery of new natural products from plants, marine invertebrates and micro-organisms as well as natural product-based drug design.

Targeting Protein-Protein Interactions in Receptor Complexes (PL13)

Prof. Kristian STROMGAARD

UNIVERSITY OF COPENHAGEN, Copenhagen, Denmark
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Prof. Kristian STROMGAARD

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Professor Kristian Strømgaard graduated from the Royal Danish School of Pharmacy (1999), with part of the studies carried out at the Danish pharmaceutical company H. Lundbeck A/S and previous studies at University College London. He did his postdoctoral training at Columbia University (USA) and was subsequently appointed assistant professor at University of Copenhagen, and thereafter promoted to full professor in chemical biology 2006. His research spans chemistry and biology with focus on protein-protein interactions, including inlcuding peptide and protein engineering. In 2014 he was appointed Director of Center for Biopharmaceuticals at University of Copenhagen and 2016-17 he was a visting professor at Harvard Medical School. He is co-founder of the biotechnology company Avilex Pharma.

Identification of the Potent, Highly Selective and Orally Bioavailable ATR Inhibitor BAY 1895344 (PL17)

Dr Franz VON NUSSBAUM

NUVISAN, Berlin, Germany
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Dr Franz VON NUSSBAUM

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Current title and positions:
Executive Vice President, Life Science Chemistry, Innovation Campus Berlin, Nuvisan GmbH
EC Member EFMC/Head of Medicinal Chemistry Division GDCh

Research field:
Oncology, Cardiology, Bacteriology; Fungicides

Education and former professional experience:

CV
Medicinal Chemistry Berlin, Bayer Pharmaceuticals
Head Fungicide Chemistry, Lyon & Monheim, Bayer Crop Science
Medicinal Chemistry Wuppertal, Bayer Pharmaceuticals

Education
PostDoc Columbia University, New York, Danishefsky Group, Total Synthesis of Alkaloids
PhD, University Munich, Steglich Group, Natural Products, Synthesis & Biosynthesis

Taming Random Conjugation: a General Approach for Equimolar Linking of Proteins and Payloads (IL02)

Dr Sergii KOLODYCH

SYNDIVIA, Strasbourg, France
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Dr Sergii KOLODYCH

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Dr. Sergii Kolodych is a CSO of Syndivia. He received his Ph.D. from the Laboratory of Molecular Labelling and Bio-Organic Chemistry in the CEA Saclay Center. During his Ph.D., he developed an immunological screening platform for the discovery of new biocompatible coupling reactions. His further research work focused on the development of bioconjugation technologies and their application in the field of targeted cancer therapies. At Syndivia, Dr. Kolodych has led preclinical development of a number of Antibody-Drug Conjugates and small molecule cancer therapeutics. He is an author of 19 peer-reviewed publications and an inventor on 5 patent families.

Anti-Virulence Agent to Treat S. Aureus Infections (IL03)

Dr Alessia MICHELOTTI

BIOVERSYS AG, Lille, France
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Dr Alessia MICHELOTTI

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Alessia Michelotti received her M.Sc. at the University of Turin where she studied carborane-based theranostic agents for Boron Neutron Capture Therapy applications with Prof. Annamaria Deagostino. She obtained her PhD in Chemistry in 2019 at Paris-Saclay University in collaboration with CortecNet, under the supervision of Dr. Charlotte Martineau-Corcos and Dr. Maxime Roche where she developed metal-catalyzed C-H deuteration and 13C labelling of endogenous bioactive molecules for DNP-NMR/MRI studies. She then joined BioVersys in Lille in 2019 as a junior researcher in medicinal chemistry, involved in the development of first-in-class stand-alone anti-virulence small molecule drugs for the treatment of MRSA (Methicillin-resistant Staphylococcus Aureus) infections.

Chemical Biology Tools for Enlightening Therapies (IL01)

Prof. Olalla VÁZQUEZ

PHILIPPS-UNIVERSITÄT MARBURG, Marburg, Germany
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Prof. Olalla VÁZQUEZ

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Olalla Vázquez is currently enjoying an Assistant Professorship in Chemical Biology at Philipps-Universität Marburg (Germany). Her independent work focuses on the design and synthesis of novel photosensitive molecules capable of sensing biological processes, and remotely controlling the cellular machinery behind relevant disease-related processes. Olalla obtained her PhD in Chemistry at the Universidade de Santiago de Compostela in Spain (Prof. Mascareñas and Prof. Vázquez) in 2010. As FPU fellow, she was a visiting PhD student at both Harvard University (Prof. Verdine; 2006) and Humboldt Universität zu Berlin (Prof. Seitz; 2008). In 2011 she received a Marie Curie fellowship to conduct her postdoctoral studies (Prof. Seitz). During her career path, Olalla has received several awards, including Research Lilly Award (2009), European Young Chemist Award (EYCA 2012), Fulbright-Cottrell Award (2016), Next Generation Optogenetics (2017) and MarBiNa Förderpreis (2018).