Chemical biology and proteomic strategies are rapidly emerging as cost effective yet powerful preclinical approaches for the discovery and identification of novel drugs and targets. Advances in the development and combination of high-quality chemical tools, bioorthogonal techniques, disease-relevant phenotypic systems, chemoinformatics, proteomics and quantitative mass spectrometry, now provide robust and high-throughput workflows for interrogating drug-target-phenotype relationships. These efforts are poised to significantly enrich preclinical discovery programs and are illuminating a new paradigm for the development of novel drugs modulating novel targets.
Cambridge Healthtech Institute’s back-to-back Chemical Biology and Proteomics for Target Validation meetings will once again gather an interdisciplinary collection of leaders to discuss these emerging tools and strategies to de-risk novel discovery initiatives
Preliminary Agenda
Protein Folding: A Powerful Driver of Phenotypic Novelty
Susan Lindquist, Ph.D., Professor, Biology, MIT; Investigator, Howard Hughes Medical Institute
FITGE-Based Target Identification for the Connection of Rational Drug Discovery with Phenotypic Screening
Seung Bum Park, Ph.D., Professor, Chemistry, Seoul National University
Sulfonyl Fluoride Chemistry for Target Validation, Identification and Other Applications in Chemical Biology
Lyn Jones, Ph.D., Head, Chemistry, Chemical Biology & Rare Diseases, Pfizer
Chemical Probe Libraries to Explore and Validate Novel Biology
Iván Cornella-Taracido, Ph.D., Senior Principal Scientist, Discovery Chemistry, Merck
PROTAC and HyT Technologies for Protein Degradation
Andy Crew, Ph.D., Vice President, Chemistry, Arvinas
Targeting the Stress Chaperome in Disease, Diagnosis and Treatment
Gabriela Chiosis, Ph.D., Associate Member and Lab Head, Molecular Pharmacology and Chemistry, Sloan Kettering Institute; Associate Attending, Department of Medicine, Memorial Sloan Kettering Cancer Center
Chemical Modulation of Chromatin Structure
Jun Qi, Ph.D., Senior Research Scientist, Bradner Lab, Department of Medical Oncology, Dana-Farber Cancer Institute
Small Molecules to Engineer and Explore Human Immunity
David A. Spiegel, Ph.D., M.D., Professor, Department of Chemistry, Yale University
Spliceosome Modulation for the Treatment of Mutant SF3B1 Cancers
Gregg F. Keaney, Ph.D., Senior Scientific Investigator, Medicinal Chemistry, H3 Biomedicine
Discovering and Validating Drug Targets Using Synthetic Binding Proteins
Shohei Koide, Professor, Ph.D., Biochemistry and Molecular Biology, The University of Chicago
Not All mGluR PAMs are Created Equal: Designing the Right Allosteric Ligand for Your Clinical Indication
Dario Doller, Ph.D., Director, Discovery Chemistry & DMPK, Global Head of Chemical Biology, Lundbeck Research USA
Novel Probes for E3 Ligases: pH Cleavable Photocrosslinkers to Map E2/E3 Ligase PPI Interface and UbiFlu Novel Fluorescent Probes
Alexander Statsyuk, Ph.D., Assistant Professor, Department of Chemistry, Northwestern University
Preliminary Agenda
BioPlex 1.0: An Orfeome-Based, Mass Spectrometry-Driven, Human Protein Interaction Network
Steven P. Gygi, Ph.D., Professor, Cell Biology, Harvard Medical School
Mass Spectrometry-Based Proteomics in Preclinical Drug Discovery
Bernhard Kuster, Ph.D., Professor, Co-Founder, Chair, Proteomics and Bioanalytics, Technische Universität München
Proteomics as a Contributing Technology in Drug Discovery
Kieran Geoghegan, Ph.D., Research Fellow, Pfizer Inc.
Tracking Cancer Drugs in Living Cells by Thermal Profiling of the Proteome
Marcus Bantscheff, Ph.D., Head, Technology, Cellzome GmbH, Molecular Discovery Research, GlaxoSmithKline
Proteomics-Based Methods for In-Depth Analysis of Key Molecular Events in Tumorigenesis
Jarrod Marto, Ph.D., Department of Biological Chemistry and Molecular Pharmacology, Dana-Farber
Chemical Proteomic Strategies to Investigate Reactive Cysteines
Eranthie Weerapana, Ph.D., Assistant Professor, Chemistry, Boston College
Serendipitous Discovery of the Selective Inhibitor of the Ubiquitin System Using Chemoproteomic Approaches
Alexander Statsyuk, Ph.D., Assistant Professor, Chemistry, Northwestern University
Towards Comprehensive Coverage of Drug Target Space in Chemical Proteomics
Markus Schirle, Ph.D., Senior Investigator I, Novartis Institutes for BioMedical Research, Inc.
Case Strudies in Target Identification and Mechanism of Action in Drug Discovery
Monica Schenone, Ph.D., Technical and Scientific Leader, Biochemical Target ID, Proteomics Platform, Broad Institute
Small Molecule Profiling by Protein Stability-Based Interaction Proteomics (ProSIP)
Kilian Huber, Ph.D., Senior Fellow, Giulio Superti-Furga Laboratory, CeMM Research Center for Molecular Medicine of the Austrian Academy of Sciences
Utilizing Chemogenomics to Chemoproteomics to Identify and Validate New Targets in Drug Discovery
Erik Hett, Ph.D., Principal Scientist, Chemical Biology, Medicinal Chemistry, Pfizer
Tandem Photoaffinity Labeling - Bioorthogonal Conjugation in Medicinal Chemistry
David Lapinsky, Ph.D., Associate Professor, Medicinal Chemistry, Division of Pharmaceutical Sciences, Duquesne University
A Modular and Traceless Chemical Method to Locate and Track Endogenous Protein Targets in Live Cells
James Chambers, Ph.D., Assistant Professor, Chemistry, University of Massachusetts, Amherst
Chemoproteomics with Clickable Photoaffinity Probes for Neuroscience Target ID and Validation
Doug Johnson, Ph.D., Associate Research Fellow, Neuroscience, Medicinal Chemistry, Pfizer
Pharma Sources Insight January 2025
