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Keynote Speakers
Sequence-Based Design of RNA-Targeted Small Molecules (KL01)
Prof. Matthew DISNEY (UF SCRIPPS, Jupiter, United States) Read more
Matt Disney is a native of Baltimore and is currently Professor in the Department of Chemistry at Scripps Research on the Florida Campus. His laboratory works in the area of small molecule targeting of RNA. The lab seeks to answer fundamental questions regarding molecular recognition events between RNA folds and small molecules to study problems of biomedical importance. Indeed, they have developed a strategies to: (i) design structure-specific small molecules from the RNA’s sequence; (ii) synthesize drugs on-site in disease-affected cells to affect their function and to image them; (iii) study the biology of coding and non-coding RNAs, with a focus on incurable rare diseases and difficult-to-treat cancers; and (iv) interface RNAs with quality control machinery using small molecules and chimeras thereof to eliminate them from cells and animal models of disease. The lab’s research has garnered various awards including the Sackler Prize in the Physical Sciences, Barry Cohen Award in Medicinal Chemistry, NIH Director’s Pioneer Award, the Tetrahedron Young Investigator Award, the Eli Lily Award in Biological Chemistry, the David W. Robertson Award in Medicinal Chemistry, and others. Close window
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Reimagining Druggability using Chemoproteomic Platforms (KL03)
Prof. Daniel NOMURA (UC BERKELEY, Berkeley, United States) Read more
Dan Nomura is a Professor of Chemical Biology and Molecular Therapeutics in the Department of Chemistry and the Department of Molecular and Cell Biology in the Division of Molecular Therapeutics at the University of California, Berkeley and an Investigator at the Innovative Genomics Institute. He is also an Adjunct Professor in the Department of Pharmaceutical Chemistry at UCSF. Since 2017, he has also been the Director of the Novartis-Berkeley Translational Chemical Biology Institute focused on using chemoproteomic platforms to tackle the undruggable proteome. He is also Co-Founder of Frontier Medicines, a start-up company focused on using chemoproteomics and machine learning approaches to tackle the undruggable proteome. He is also the Founder of Vicinitas Therapeutics based on his group’s discovery of the Deubiquitinase Targeting Chimera (DUBTAC) platform for targeted protein stabilization. He is also on the Scientific Advisory Boards for Frontier Medicines, Vicinitas Therapeutics, Photys Therapeutics, Apertor Pharma, and the Mark Foundation for Cancer Research and is on the Investment Advisory Board of Droia Ventures. He earned his B.A. in Molecular and Cell Biology and Ph.D. in Molecular Toxicology at UC Berkeley with Professor John Casida and was a postdoctoral fellow at Scripps Research with Professor Benjamin F. Cravatt before returning to Berkeley as a faculty member in 2011. Among his honors include the National Cancer Institute Outstanding Investigator Award, Searle Scholar, American Cancer Society Research Scholar Award, and the Mark Foundation for Cancer Research ASPIRE award. Close window
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How Ligand-Binding Biophysics can Advance a Small-Molecule Neuroscience Portfolio (KL02)
Dr Laura SILVIAN (BIOGEN, Cambridge, United States) Read more
Dr. Laura Silvian, Sr. Director, leads the innovative Physical Biochemistry and Molecular Design group within the Biotherapeutic and Medicinal Sciences department at Biogen in Cambridge, MA. We use structure-based, rational drug design and biophysical assessments to improve potency, selectivity or developability of therapeutics for the treatment of neurodegenerative diseases. We influence program team decisions in engineering different therapeutic modalities --biologics, small molecule, and gene therapy-- using cutting-edge techniques in structural biology, biophysical methods, and protein science.
In past years we have embraced several new technologies including:
• assembly of recombinant protein complexes including membrane proteins and RNA/protein complexes,
• small molecule compound binding measurements,
• Cryo-EM in addition to longstanding capabilities in X-ray Crystallography, and NMR for structure solution,
• and molecular design strategies for improved biologics efficacy and developability.
Laura is an inventor or coauthor on more than 40 publications and 5 patents on protein and RNA targets. She served as chair of the Industrial Scientific Interest group at the ACA, reviewed grants for Michael J Fox Foundation, and has chaired sessions at Discovery on Target conferences. Close window
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Session 1: EMERGING TECHNOLOGIES - NEW BIOPHYSICAL APPROACHES FOR MEASURING MOLECULAR INTERACTIONS
Kinetic Characterization of Ligand and Antibody Binding to Cell Surface Expressed CCRL2 Using Surface Plasmon Resonance Microscopy (SPRM) (IL01)
Dr Jonathan BROOKS (PFIZER, Cambridge, United States) Read more
Principal Scientist, Pfizer Pharmaceuticals
Jonathan began his career at Genetics Institute in 1990 developing immunoassays for use in pharmacokinetics and process development. Jon has over 30 years of experience in label free analysis of receptor ligand interactions and small molecule target binding associated with several respiratory and inflammatory disease areas. Currently, he is a principal scientist in the inflammation and Immunology research unit at Pfizer in Cambridge, Massachusetts. Close window
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High-Throughput Protein Analysis and Binding Assays Enabled by IR-MALDESI-MS (IL02)
Dr Nathaniel ELSEN (ABBVIE INC., North Chicago, United States) Read more
Principal Research Scientist, AbbVie
Nate received his Ph.D. from the University of Wisconsin-Madison Biochemistry Department where he studied the impact of protein-protein interactions on the kinetics of di-iron containing enzymes. After graduate school he worked six years at Merck in the small molecule protein biochemistry group contributing to early drug discovery projects in a variety of roles including biophysical assay development, fragment screening, in vitro pharmacology, and protein biochemistry for x-ray crystallography, NMR, and HTS. For the last seven years Nate has been in the Assay Development and Screening group at AbbVie and has continued to support small molecule drug discovery in the In Vitro Pharmacology space. Close window
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Single-Molecule Analysis of Drug-Target Interactions Using a Molecular Forceps (OC01 - virtual presentation)
Prof. Terence STRICK (ECOLE NORMALE SUPÉRIEURE, Paris, France) Read more
Terence Strick is an experimental biophysicist known for inventing the magnetic trap system widely used today in single-molecule experimentation. The research group he heads develops novel hardware and molecular tools to augment the single-molecule toolkit. One such tool is a "molecular forceps" which extends the range of applicability of single-molecule mechanical manipulation to analysis and high-throughput screening of drug-protein interactions. Close window
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NMR Reporter Assays for the Quantification of Weak-Affinity Receptor–Ligand Interactions (OC02)
Dr Reto WALSER (ASTEX PHARMACEUTICALS, Cambridge, United Kingdom) Read more
Reto studied biochemistry and biophysics at the ETH Zurich and obtained his PhD in biomolecular NMR from the University of Zurich. Following postdoctoral studies in the Structure & Biophysics group of Astrazeneca in Alderley Park, Reto joined Astex Pharmaceuticals in 2017 where he is currently an Associate Director in the Biophysics group of the Molecular Sciences department. In this role he oversees the delivery of biophysical fragment screening and hit validation cascades for Astex’s early-stage discovery projects. Reto has a particular interest in increasing the throughput and sensitivity of NMR experiments for the quantitation of weak affinity interactions. Other aspects of his work include the expansion and further development of Astex’s biophysics platform and fragment library. Close window
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Session 2: COVALENT DRUG DISCOVERY
Discovery of the KRAS G12C Covalent Drug Adagrasib and Beyond (OC04)
Dr Robin GUNN (MIRATI THERAPEUTICS, San Diego, United States) Read more
Robin Gunn is the Director of Structural Biology at Mirati Therapeutics where she has made key contributions on the KRAS, PRMT5, and SOS1 drug discovery programs. All three programs have compounds currently in clinical trials (MRTX-1133, MRTX-1719, MRTX-0902, respectively). Krazati, a covalent KRAS G12C inhibitor, is now FDA approved for the treatment of non-small cell lung cancer. She earned her PhD from The Scripps Research Institute. Robin was an early adopter of structure-based fragment screening, which she implemented at ActiveSight. Throughout her career she has combined insights from biophysical methods, x-ray crystallography, and protein science to drive projects forward. Close window
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In-Cell Covalent Inhibitors Discovery (IL04)
Dr Brent MARTIN (SCORPION THERAPEUTICS, Boston, United States) Read more
Brent Martin received his Ph.D. in Pharmacology at the University of California in San Diego followed by postdoctoral studies at the Scripps Research Institute developing new strategies for activity-based profiling, high-throughput screening, and chemical proteomics. As faculty member at the University of Michigan in Ann Arbor, he continued expanding the scope of activity-based profiling methods, while also establishing new bioconjugation reactions to detect and profile protein lipidation, redox modifications, and cysteine occupancy. Brent is the recipient of the NCI Howard Temin K99/R00 award in Cancer Research, the NIH Director’s New Innovator Award, and the NIGMS MIRA Established Investigator Award. He later led the Chemical Biology at Janssen and is currently Vice President and Head of Chemical Biology at Scorpion Therapeutics. Close window
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Covalent Screening and Hit Characterization Methods for Efficient Covalent Drug Discovery (OC03)
Dr Mela MULVIHILL (GENENTECH, INC., South San Francisco, United States) Read more
Mela Mulvihill is a Director and Senior Principal Scientist in the Biochemical and Cellular Pharmacology department at Genentech leading the biophysics group. Mela has been instrumental in expanding the application of information-rich biophysical techniques such as SPR and MS to small molecule lead finding, characterization, and optimization. She is a project team leader and has significantly contributed to Genentech’s fragment, covalent, and degrader drug discovery strategies. Mela earned her B.S. in Chemistry at Sonoma State University, Ph.D. in Biochemistry at the University of California, San Diego, and was a postdoctoral fellow at the University of California, Berkeley. Close window
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Developing Covalent Small Molecules for Protein Targets from Kinases to Transcription Factors (IL03)
Dr Tinghu ZHANG (STANFORD, Stanford, United States) Read more
Dr. Zhang is a senior scientist at Cancer Institute of Stanford. Dr. Zhang is an experienced medicinal chemist and chemical biologist. Dr. Zhang leads and supervises drug discovery projects with the targets of kinases and transcription regulators. His research focuses on the discovery of covalent modality and protein degradation. He has led the discoveries of covalent inhibitor of CDK7, CDK12/13, JNK, PIP4K, MKK4, Src and TEAD and degrader molecules for CDK12, CDK4/6, FGFR1/2, CDK2/5 et al. Under his leadership, Dr. Zhang has contributed several prototype chemical leads for further drug development including THZ1. Dr. Zhang was also a chemistry group leader at the Center of Protein Degradation (CPD) of Dana-Farber from 2018 to 2021. Dr. Zhang received his Ph.D in chemistry from USTC (China) in 2004. Close window
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Session 3: HYBRID METHODS AND TECHNIQUE COMBINATIONS
Identification and Characterization of Modulators of DEAH-Box Helicase DHX9 (OC08)
Dr Ann BORIACK-SJODIN (ACCENT THERAPEUTICS, Lexington, United States) Read more
Ann Boriack-Sjodin, Ph.D. is Senior Vice President of Molecular Discovery at Accent Therapeutics. She has a passion for early stage drug discovery, with contributions to dozens of targets spanning multiple disease indications and experience in both large organizations (Biogen, AstraZeneca) and small biotech (Epizyme, Accent). Ann joined Accent Therapeutics in 2017 where she has applied her expertise in novel target drug discovery to RNA modifying proteins utilizing both internal and external resources.
Ann received her PhD from the University of Pennsylvania with Dr. David Christianson and performed postdoctoral research with Dr. John Kuriyan at the Rockefeller University. She has contributed to more than 50 publications and over 20 patents in her career. Close window
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HDX-MS Use as a Complementary Technique to X-ray Crystallography and Cryo-EM to Better Understand Small Molecule Binding Events (OC06)
Dr Fabrice CIESIELSKI (NOVALIX, Illkirch, France) |
Drug Discovery for the Oncogenic Protein KRAS on a Model Membrane (OC05)
Dr Fenneke KLEINJAN (UHN, Toronto, Canada) Read more
Fenneke KleinJan, is a postdoctoral researcher at the Princess Margaret Cancer Centre, University Health Network in Toronto, Canada. Her research focuses on fragment-based drug discovery of small GTPases using applied biophysical methods. Fenneke has a PhD in Experimental Physics from the University of Ulm in Germany. Close window
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Leishmania Translation Initiation Factor IF4E: a Potential Target for Antiparasitic Drug Development (IL05)
Dr Mélissa LÉGER-ABRAHAM (BLAVATNIK INSTITUTE | HARVARD MEDICAL SCHOOL, Boston, United States) Read more
Mélissa Léger-Abraham is a research scientist who obtained a bachelor’s and a Ph.D. degree in Biochemistry from Université de Montréal, Montréal, Canada, where she grew up. She then completed postdoctoral studies in the field of structural biology at Harvard Medical School in the Department of Biological Chemistry and Molecular Pharmacology. During that time, she became proficient in biophysical characterization of proteins and structure determination using NMR spectroscopy and X-ray crystallography. She is currently an Assistant Professor of Pediatrics in the Division of Molecular Medicine at Boston Children’s Hospital, and an Assistant Professor of Microbiology in the Department of Microbiology at the Blavatnik Institute | Harvard Medical School. She is dedicated to contributing to the field of infectious diseases, more specifically to neglected tropical diseases. Close window
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Biophysical Characterization of Allosteric Cooperativity in PRMT5 (OC07)
Prof. Till MAURER (IDEAYA BIOSCIENCES, South San Francisco, United States) Read more
Senior Principal Research Scientist in Biophysics, Lead Discovery, Ideaya Bioscience, South San Francisco, Adjunct Professor, Fakultät für Biologie und Vorklinische Medizin Lehrstuhl Biophysik II, Regensburg University
Research field: Using the Biophysics toolchest in observing and understanding molecular interaction, and its application in drug discovery
Past Positions: 2019-2022: Director and Principal Scientist, MSD, Rahway and West Point
2009-2018: Senior Scientist, Genentech, South San Francisco
2008-2009: Principal Scientist, Merck KGaA, Darmstadt
2001-2008: Senior Scientist Boehringer Ingelheim, Biberach/Ingelheim
1995-2001: Assistant professor, Regensburg University
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Integration of Biophysics and Simulation to Drive Drug Discovery (IL06)
Dr Holly SOUTTER (BROAD INSTITUTE, Cambridge, United States) Read more
Holly Soutter is Director of Biochemistry and Biophysics within the Center for the Development of Therapeutics (CDoT) at the Broad Institute of MIT and Harvard. Her research group supports projects across multiple therapeutic areas to identify, validate, and mechanistically characterize potential small molecule therapeutics. Her team has expertise in multiple techniques including SPR, NMR, mass spectrometry, enzymology, and many others. Dr. Soutter has over 15 years of experience in the pharmaceutical and biotech sectors. She has made key contributions to multiple clinical candidates, and has co-authored more than 20 scientific publications. She received her B.A. in Chemistry from Hunter College, and her M.A. and Ph.D. in Chemistry from Clark University. Close window
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Session 4: BIOPHYSICAL ASSAYS FOR PROTACS AND MOLECULAR GLUES
A Covalent BTK Ternary Complex Compatible with Targeted Protein Degradation (IL08)
Dr Matthew CALABRESE (PFIZER, Groton, United States) Read more
Matt Calabrese obtained his PhD in Molecular Biophysics and Biochemistry from Yale University where he studied protein folding in the lab of Dr. Andrew Miranker. He then moved on to a postdoctoral fellowship with Dr. Brenda Schulman at St. Jude Children’s Research Hospital where he studied the structure and function of the ubiquitin proteasome system, with a focus on cullin-RING E3 ligases. In 2011, Matt joined Pfizer as a Senior Scientist in structural biology, and at present, he is Senior Director and Head of the Structural and Molecular Sciences department. Close window
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An Integrated Biophysical Approach to Discover Ligands for a Novel E3 Ligase (IL07)
Dr Nichole O'CONNELL (KYMERA THERAPEUTICS, Watertown, United States) Read more
Nichole O’Connell received her PhD in Biochemistry and Molecular Biophysics from Columbia University where she studied protein dynamics by NMR. Following her PhD, she took a moved to Brown University as a postdoctoral student in the lab of Wolfgang Peti, studying phosphatase structure and function. Next, she moved to AstraZeneca for an industrial postdoc. In 2013, she transitioned to Senior Scientist in the Structure and Biophysics group at AstraZeneca. Nichole then ventured into biotech at Nurix and Cedilla Therapeutics before joining Kymera Therapeutics in 2019 where she is presently Associate Director, Head of Platform Discovery. Close window
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Capturing the Flexibility of CRBN Protacs with Cryo-EM (OC10)
Dr Daniel PETER (BOEHRINGER INGELHEIM, Vienna, Austria) Read more
Principal Scientist, Boehringer Ingelheim RCV
Daniel obtained his Ph.D. at the Max Planck Institute, Tuebingen, in the Lab of Prof. Dr. Elisa Izaurralde. There he studied the mechanism of translational regulation by eIF4E-binding proteins, focusing on x-ray crystallography, ITC, and protein biochemistry. He then moved to the EMBL in Grenoble for a postdoctoral fellowship where he studied pre-mRNA splicing complexes by using single-particle cryo-EM. After that he went for an industrial postdoc at BASF before he joined Boehringer Ingelheim in Vienna as an Associate Principal scientist in 2021. Since then, he progressed to Principal Scientist and is supporting oncology research projects by single-particle cryo-EM, with the main interest in PROTACS and ternary E3 ligase complexes. Close window
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Targeted MDM2 Degradation Reveals a new Vulnerability for P53-Inactivated Triple Negative Breast Cancer (OC09)
Dr Joseph SALVINO (THE WISTAR INSTITUTE, Philadelphia, United States) Read more
I am a Medicinal Chemistry Professor and the Scientific Director of the Molecular Screening Shared Resource at The Wistar Institute. My primary research interests focus on applying my medicinal chemistry, synthetic chemistry, and drug discovery expertise to interesting academic programs to add value and facilitate translation into the clinic. I have over thirty years of industrial pharmaceutical research and academic experience in drug discovery. I have served in senior level roles in both large and small pharmaceutical companies with the goal of advancing programs from target validation through lead optimization and pre-clinical development. I received my PhD at Brown University in Organic Chemistry and was a Post-doctoral research fellow at the University of Pennsylvania working under the mentorship of KC Nicolaou and Ralph F. Hirschman in Synthetic Organic Chemistry and Medicinal Chemistry. I moved to The Wistar Institute, a biomedical research institute founded in 1894 as the first and now the oldest research institute in the US, about five years ago to become their first medicinal chemist, and to establish synthetic and medicinal chemistry capabilities to expand academic drug discovery efforts. Close window
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Session 5: SMALL MOLECULES TARGETING RNA / UNDERSTANDING SMALL-MOLECULE SELECTIVITY TOWARDS RNA
A Structure-based Approach to Discovering RNA-targeted Small Molecules (IL10)
Dr Elena MENICHELLI (ARRAKIS THERAPEUTICS, Waltham, United States) |
Exploring the Undiscovered Country of RNA as a Drug target — Finding Bioactive Ligands against XIST RNA with Affinity-selection MS Screening (IL09)
Dr Elliott B. NICKBARG (MERCK & CO., INC., Boston, United States) Read more
Elliott Nickbarg PhD is a Principal Scientist in the Quantitative Biosciences Department at Merck Research Laboratories in Boston MA. He received a bachelor’s of science degree from the University of Chicago, a doctorate in Chemistry from Harvard University and did postdoctoral work at the University of Pennsylvania.
Since then, he has worked at both small biotechnology and large phamaceutical organizations, starting with Genetics Institute, Inc. of Cambridge MA (later part of Wyeth Pharmaceuticals) working on development and applications of proteomics technology. He later joined Neogenesis Pharmaceuticals and helped develop affinity-selection mass spectrometry and its applications and has continued to apply mass spectrometry analysis for protein, RNA and small molecules, As part of these varied efforts, he has a total of almost three decades of experience in both small and large molecule drug discovery. Close window
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