08:00
09:00
Opening Ceremony
Dr Yves P. AUBERSON
NOVARTIS & EFMC, Basel, Switzerland
Prof. Maja KÖHN
UNIVERSITY OF FREIBURG, Freiburg, Germany
09:15
PL01 - Moving Undruggable Discoveries into the Drug Discovery Pipeline with Chemical Biology
Dr John TALLARICO
NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH, Cambridge, United States
Global Head, Chemical Biology and Therapeutics Department, Novartis Institutes for Biomedical Research since 2021. John has been with Novatis in progressive roles since 2004 when he joined the Global Discovery Chemistry department to help found the Chemical Genetics group there.
Previously, Dr. Tallarico served as Head of Chemical Technology, an Institute Fellow at the Harvard Institute of Chemistry and Cell Biology (ICCB) and an instructor in the Department of Cell Biology. The Harvard ICCB is a joint initiative of Harvard Medical School and Harvard University where research was focused on developing the nascent field of chemical genetics.
Dr. Tallarico’s post-doctoral studies were performed at Harvard Medical School and Harvard University as a Fellow of the Cancer Research Fund of the Damon Runyon-Walter Winchell Foundation. It was at this time, that Dr. Tallarico began his work in the field of chemical genetics where he worked with a team of researchers to build the chemical technology platform central to the ICCB discovery efforts. His laboratory was specifically interested in bringing the power of chemistry to help understand biological systems.
Dr. Tallarico received his B.A in Chemistry at Miami University, Oxford, Ohio in 1993, and his Ph.D. in Organic Chemistry at Boston College in 1999.
Session 1: Chemical Proteomics in Drug Discovery
Session Chair
Dr Sebastian ESSIG
BAYER AG, Wuppertal, Germany
10:00
KL01 - Chemoproteomics Approaches and their Contributions to Drug Discovery
Dr Marcus BANTSCHEFF
CELLZOME/GSK, Heidelberg, Germany
Marcus Bantscheff graduated in Chemistry at the University of Konstanz and obtained his PhD degree from the University of Rostock. After a short postdoc at the Proteome Center in Rostock, Marcus joined Cellzome in 2002 where he has served in several functions including Director of Analytical Sciences focussing on developing Cellzome’s core technologies in quantitative proteomics and chemoproteomics including Kinobeads™. Marcus joined GSK upon Cellzome’s acquisition in 2012 where he currently serves as Senior Scientific Director in the Genomic Sciences department heading the Functional and Chemical Proteomics and Metabolomics team and leading an integrated target discovery matrix. Marcus’ published work focuses on the development and application of proteomics, chemical biology and computational approaches to characterize targets, disease mechanisms and mechanism-of-action of bioactive molecules. He is an inventor on several patents including Cellzome’s Kinobeads™ technology, has co-authored more than 100 publications, and serves as a reviewer for reputed journals and funding bodies.
10:45
Coffee Break, Networking & Exhibition
11:15
IL01 - Towards Covalent Inhibitors Addressing Diverse Amino Acids
Dr Stephan HACKER
LEIDEN UNIVERSITY, Leiden, The Netherlands
Stephan Hacker obtained his PhD degree working with Prof. Andreas Marx at the University of Konstanz and performed postdoctoral research with Prof. Benjamin Cravatt at The Scripps Research Institute in La Jolla. Afterwards, he moved to the Technical University of Munich as an independent group leader with a Liebig Fellowship. In 2021, he became Assistant Professor at the Leiden Institute of Chemistry. Stephan Hacker’s group develops covalent protein ligands targeting diverse amino acids as well as chemoproteomic technologies to study their target engagement with resolution of the modified amino acid residue in order to identify new target proteins for antibiotics.
11:40
IL02 - ABPP and its Impact on Drug Discovery - Successful Examples from the MAGL Program
Dr Uwe GRETHER
F. HOFFMANN-LA ROCHE, Basel, Switzerland
Uwe Grether received his Diploma degree in Chemistry at the University of Karlsruhe, Germany, where he subsequently earned his Ph.D. in Organic Chemistry with Professor Herbert Waldmann in 2000. After that, he joined Professor James D. White’s group at Oregon State University for his postdoctoral research. In 2001, Dr. Grether started at the Pharma Research and Early Development unit of F. Hoffmann-La Roche Ltd. in Basel, Switzerland. He has a long standing professional experience as project team leader in drug discovery and development reaching advanced stages up to phase 3 clinical trials with multiple new molecular entities. Dr. Grether has profound knowledge on different target classes, a broad variety of indications, chemical biology, and expertise in due diligences. He has led academic as well as industrial external collaborations and is an intrapreneur of novel technologies for project and platform applications. Dr. Grether is co-author of more than 140 patents, research publications and book chapters. His research interests include medicinal chemistry, late stage functionalization and chemical probes focusing on holistic approaches toward a clinical end-goal.
12:05
OC01 - Lessons for Covalent Drug Development from Deep Chemoproteomic Profiling of Approved Covalent Drugs
Dr Micah NIPHAKIS
LUNDBECK, San Diego, CA, United States
Micah Niphakis received his Ph.D. in Medicinal Chemistry at the University of Kansas, where he developed synthetic approaches to access phenanthropiperidine natural products for studying their anti-cancer properties. He then joined the Cravatt lab at Scripps Research as a postdoctoral fellow to study chemical biology. During this time, his research focused on developing chemical tools to study the endocannabinoid system, which led to the discovery of highly selective, covalent MAGL inhibitors and photoaffinity probes to globally map lipid binding proteins.
>
In 2014, Micah joined Abide Therapeutics, where he led the development and implementation of an industrialized serine hydrolase-directed chemoproteomics platform. He also spearheaded chemical library enhancement efforts to facilitate the discovery of novel covalent inhibitors targeting active-site nucleophiles.
>
Micah joined Lundbeck as a part of Abide’s acquisition in 2019. He has continued his role in leading platform and chemical library development efforts, with an expanded mission to uncover chemical tractability for historically challenging targets using proteome-wide ligand discovery platforms.
12:25
Lunch, Networking & Exhibition
12:30
Company Workshop by WuXi AppTec
Emerging Modalities in Drug Discovery
Dr Tao GUO
WUXI APPTEC, St Pauls, United States
Session 2: Computational Chemical Biology (LS-EuChemS Session)
Session Chair
Dr Sonsoles MARTIN-SANTAMARIA
CIB-CSIC, Madrid, Spain
13:55
KL02 - Unravelling the Molecular Mechanism of Pre-mRNA Splicing via All-atom Simulations
Prof. Alessandra MAGISTRATO
CNR-IOM, Trieste, Italy
Dr. Alessandra Magistrato is research director at of Italian National Research Council (CNR-IOM) c/o International School for Advanced studies, Trieste Italy, where she leads the group computational biology. She obtained her PhD in computational Chemistry at ETH Zentrum, Zuerich, Switerland, and she was postdoctoral fellow at the University of Pennsylvania, Philadelphia, PA, USA.
The Magistrato Lab research activity is devoted to the development and application of state-of-the-art computational methods for multi-scale molecular simulations. We aim to investigate the structure, function, and dynamics of complex biological systems and to the development of small-molecule inhibitor to modulate their function. Our research activity ranges from the study of pharmacologically relevant enzymes, to that of protein/RNA machineries, metal ions transporters and cytolytic toxins. Our research lies at the interface of chemistry, biology and medicinal chemistry and involves collaborations with various experimental labs
14:40
IL03 - Challenges in Simulating Molecular Recognition Using Coarse-grain Models
Prof. Manuel MELO
UNIVERSITY NOVA DE LISBOA, Oeiras, Portugal
Manuel N. Melo is an auxiliary researcher and the head of the Multiscale Modeling lab within the MOSTMICRO unit of ITQB – Universidade NOVA de Lisboa. His work is centered on elucidating the molecular-level details of lipid-lipid, lipid-protein, and protein-protein interactions; recent collaborations also focus on modeling bacterial structures. Manuel's research employs coarse-grained, atomistic, and hybrid molecular dynamic simulations, and tackles both the construction of models (as a developer within the Martini coarse-grain framework) and their application to biological questions. Additionally, Manuel’s lab actively develops simulation and analysis software, with emphasis on large-scale parallelization of analysis.
Manuel pursued his Ph.D. on the molecular level interactions of antimicrobial peptides with cellular membranes, using spectroscopic techniques coupled to mathematical modeling. As a Marie Curie Fellow, and later as a Dutch NWO VENI Fellow, Manuel carried out postdoctoral work at the Marrink lab, at the University of Groningen — where he became involved in the development and application of the Martini coarse grain model.
15:05
OC02 - Molecular Binding Studies in G Protein Coupled Receptors: Insights for Drug Discovery
Prof. Vittorio LIMONGELLI
UNIVERSITÀ DELLA SVIZZERA ITALIANA USI, Lugano, Switzerland
Prof. Limongelli graduated in medicinal chemistry in 2004 at University of Naples (Italy) where he also did his PhD in drug sciences. He moved to ETH Zurich in the group of Prof. Michele Parrinello for the postdoc. Then, he got a tenure position at University of Naples before reaching the Università della Svizzera italiana in Lugano where he is currently full professor in pharmacology at the faculty of biomedical sciences and director of the Euler Institute.
He obtained an ERC grant on computational methods development applied to GPCRs and received awards and recognitions for his research including the USERN Prize as top 5 scientists in physical and chemical sciences. He is in the top 2% of most cited scientists in the world.
15:30
Coffee Break, Networking & Exhibition
Session 3: Chemically Induced Proximity
Session Chair
Prof. Gonçalo BERNARDES
UNIVERSITY OF CAMBRIDGE & IMM LISBOA, Cambridge, United Kingdom
After completing his D.Phil. 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. In 2018 he was appointed University Lecturer (Tenured) and recently has been promoted to Reader (Associate Professor). Gonçalo is the recipient of two European Research Council grants; a starting grant and a proof-of-concept grant, and was awarded the Harrison–Meldola Memorial Prize in 2016 and the MedChemComm Emerging Investigator Lectureship in 2018, both from the Royal Society of Chemistry. His research group interests focus on the use of chemistry principles to tackle challenging biological problems for understanding and fight cancer.
16:00
OC03 - Molecular Glues for the 14-3-3 Interactome
Dr Richard DOVESTON
UNIVERSITY OF LEICESTER, Leicester, United Kingdom
Richard is an Associate Professor in Chemical Biology within the Leicester Institute of Structural and Chemical Biology and School of Chemistry at the University of Leicester, UK. His research is focussed on the application of chemical synthesis and chemical biology approaches for the development of novel pharmaceutical modalities. In particular, his group has a keen interest in the discovery, design and evaluation of molecular glues. Prior to joining the University of Leicester Richard held a Marie Curie fellowship at the Eindhoven University of Technology (NL) and undertook a post-doctoral research project at the University of Leeds (UK).
16:20
IL04 - Tumor Targeting
Prof. Dario NERI
ETH ZÜRICH, Zürich, Switzerland
Dario Neri was born in Rome on 1. May 1963 and grew up in Siena (Italy). He studied Chemistry at the Scuola Normale Superiore of Pisa and earned a PhD in Chemistry from the Swiss Federal Institute of Technology (ETH Zürich), under the supervision of Professor Kurt Wüthrich (Nobel Prize Chemistry 2002). After a post-doctoral research internship (1992-1996) at the Medical Research Council Centre in Cambridge (UK), under the supervision of Sir Gregory Winter (Nobel Prize Chrmistry 2018), he became professor at ETH Zürich in 1996. Dario Neri has been Full Professor of Biomacromolecules at the Department of Chemistry and Applied Biosciences, ETH Zürich. In October 2020, he moved full-time to Philogen (www.philogen.com), a Swiss-Italian Biotech Company which he had co-founded in 1996 and in which he currently serves as Chief Executive Officer and Chief Scientific Officer, while retaining the ETH Professor title. He is also Honorary Senior Visiting Fellow at the University of Cambridge, UK.
The research activities of the Neri group and of Philogen focus on the engineering of therapeutic antibodies for the therapy of cancer and other angiogenesis-related disorders and on the development of DNA-encoded chemical libraries. Two of the antibody products of Philogen are currently being investigated in Phase III clinical trials in Europe and in the United States, while the broader clinical-stage pipeline of Philogen is composed both of antibody-based and of small molecule-based pharmaceuticals.
Dario Neri has published more than 400 articles in peer-reviewed scientific journals. He is the recipient of the ISOBM Abbott Prize 2000, of the Amgen-Dompe’ Biotec Award 2000, of the Mangia d’Oro 2001, of the Prous Award 2006 of the European Federation of Medicinal Chemistry, of the Robert-Wenner-Prize 2007 of the Swiss Cancer League, of the SWISS BRIDGE Award 2008, of the Prix Mentzer of the French Medicinal Chemistry Society in 2011, of the Phoenix Prize 2014, of an ERC Advanced Grant in 2015, the 6th World ADC Award in 2019 and the Paul Harris Fellow Award in 2022.
16:45
IL05 - Small Molecule Therapeutics Targeting Fibroblast Activation Protein in the Tumor Microenvironment
Dr Samuele CAZZAMALLI
PHILOCHEM AG, Otelfingen, Switzerland
Samuele Cazzamalli studied Medicinal Chemistry at Universitá degli Studi di Milano, where he graduated with a thesis on the development of novel techniques for the application of biocatalysts in flow chemistry under the supervision of Prof. Carlo De Micheli. Samuele performed his PhD at ETH Zurich in the group of Professor Dario Neri with a focus on non-internalizing antibody- and small molecule-drug conjugates for the treatment of cancer. Samuele currently heads research in the field of Small Molecule Therapeutics at Philochem.
17:10
KL03 - Chemogenetic and Optogenetic Technologies for Probing Molecular and Cellular Networks
(Virtual Lecture)
Prof. Alice TING
STANFORD UNIVERSITY, Stanford, United States
Alice Ting is a Professor of Genetics, Biology, and by courtesy, Chemistry at Stanford University. Alice’s work straddles the interface of chemistry and biology and the molecular technologies she has developed, including enzyme-catalyzed proximity labeling, have been widely adopted in cell biology and neuroscience to probe organelle proteomes and protein interaction networks. She has received the NIH Pioneer Award, the Arthur Cope Scholar Award, and the McKnight Technological Innovations in Neuroscience Award. Alice has been a Chan Zuckerberg Biohub investigator since 2017. Prior to Stanford, Alice was Professor of Chemistry at MIT and she received her training at Harvard with EJ Corey, UC Berkeley with Peter Schultz, and UCSD with Roger Tsien.
17:55
Poster Session I (Odd), Networking & Exhibition
18:30
Welcome Reception & Poster Session I (Odd), Networking & Exhibition
19:30