SESSION 3: HYBRID METHODS AND TECHNIQUE COMBINATIONS
Session Chair
Dr Holly SOUTTER
BROAD INSTITUTE, Cambridge, United States
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.
09:00 am
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
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.
09:30 am
Drug Discovery for the Oncogenic Protein KRAS on a Model Membrane (OC05)
Dr Fenneke KLEINJAN
UHN, Toronto, Canada
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.
09:45 am
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
10:05 am
Coffee Break & Exhibition on-site
10:35 am
Integration of Biophysics and Simulation to Drive Drug Discovery (IL06)
Dr Holly SOUTTER
BROAD INSTITUTE, Cambridge, United States
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.
11:05 am
Biophysical Characterization of Allosteric Cooperativity in PRMT5 (OC07)
Prof. Till MAURER
IDEAYA BIOSCIENCES, South San Francisco, United States
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
11:20 am
Exhibitor Short Presentation
Integrated Use of Biophysics to Improve Data and Decision Quality in Drug Discovery (ESP05)
Dr Stoyan MILEV
MALVERN PANALYTICAL INC., Westborough, United States
11:30 am
Identification and Characterization of Modulators of DEAH-Box Helicase DHX9 (OC08)
Dr Ann BORIACK-SJODIN
ACCENT THERAPEUTICS, Lexington, United States
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.
KEYNOTE LECTURE
11:45 am
How Ligand-Binding Biophysics can Advance a Small-Molecule Neuroscience Portfolio (KL02)
Dr Laura SILVIAN
BIOGEN, Cambridge, United States
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.
12:45 pm
Lunch, Networking & Exhibition on-site
01:45 pm
In-person delegates: Poster Session 1
Virtual delegates: Meet & Greet discussion with Exhibitors
SESSION 4: BIOPHYSICAL ASSAYS FOR PROTACS AND MOLECULAR GLUES
Session Chair
Dr Claudio CIFERRI
GENENTECH, South San Francisco, United States
02:30 pm
An Integrated Biophysical Approach to Discover Ligands for a Novel E3 Ligase (IL07)
Dr Nichole O'CONNELL
KYMERA THERAPEUTICS, Watertown, United States
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.
03:00 pm
Exhibitor Short Presentation
Cube Biotech Combines Seamless Gene-to-CryoEM Structure Service with its Detergent-Free Membrane Protein Stabilization Platform Technology Native Nanodiscs (ESP06)
Dr Barbara MAERTENS
CUBE BIOTECH, Monheim, Germany
03:10 pm
Targeted MDM2 Degradation Reveals a new Vulnerability for P53-Inactivated Triple Negative Breast Cancer (OC09)
Dr Joseph SALVINO
THE WISTAR INSTITUTE, Philadelphia, United States
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.
03:25 pm
Coffee Break & Exhibition on-site
03:55 pm
Capturing the Flexibility of CRBN Protacs with Cryo-EM (OC10)
Dr Daniel PETER
BOEHRINGER INGELHEIM, Vienna, Austria
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.
04:10 pm
Exhibitor Short Presentation
How Cryo-EM is Transforming Drug Discovery (ESP07)
Dr Zuben BROWN
THERMO FISHER SCIENTIFIC, Hillsboro, United States
04:20 pm
A Covalent BTK Ternary Complex Compatible with Targeted Protein Degradation (IL08)
Dr Matthew CALABRESE
PFIZER, Groton, United States
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.
04:50 pm
Round Table set-up
04:55 pm
Round Table Discussion:
Biophysics and Structural Biology Studies to Assist the Development of PROTACs, Molecular Glues and Beyond
Moderated by
Dr Katarzyna MARCINKIEWICZ
NATURE COMMUNICATIONS, New York, NY, United States
05:40 pm
In-person delegates: Poster Session 2
Virtual delegates: Meet & Greet discussion with Exhibitors
06:30 pm
End of the Day
07:00 pm
Conference Dinner on-site (subject to prior registration)