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[Postponed due to COVID-19] No More Undruggables: Unconventional Approaches for Drug Discovery and Design - prodrugs, PROTACS, fragment-based design, directed evolution and beyond

Speakers: Carolyn Bertozzi (Stanford), Michelle Arkin (UCSF), Adrian Gill (Revolution Medicines), Michael Keiser (UCSF), Mark Smith (Stanford), Maureen Hillenmeyer (Hexagon Bio), Ian Seiple (UCSF), Daniel Erlanson (Frontier Medicines), Chaitan Khosla (Stanford)
Organizers: Toni Kline, PhD
Date: 2020-05-22
Time: 8:30-17:00 Pacific Time
Registration fee: (USD): Regular: $195; Academic: $125; Students & Unemployed: $35
Location: SF Bay Area: Foster City Crowne Plaza
Major Sponsor:
Vendor show vendors registered to date: (2)Applied StemCell; WuXi Apptec
Registration deadline:2020-05-20  (it will close sooner if the seating cap is reached)

About the Topic

Proteins function in a physiological environment of access barriers, regulators, facilitators, and partners. In many therapeutic ecologies, single drug-single target does not apply. To target these dynamics new modalities of both drug and drug discovery are being explored. This Symposium will highlight some emerging ones.  

Part A. Beyond Target Binding

Classic drug-target interactions are typically viewed as a non-covalent association of the small molecule drug with a single protein receptor, active, or allosteric site; this binding blocks protein reaction with the native agonist or substrate, and the offending signal is quenched.  The limitations of this vision become clear when in vitro results do not translate into in vivo efficacy.

Engineering the small molecule to accommodate and exploit the complexities of ADME-- and systems biology-- is now being accomplished in a number of creative ways: Much as we once naively talked about “junk DNA” and “undruggable” targets, we now have the insight and tools to understand the therapeutic potential embedded in complex biological systems.

Part B. Towards the rest of that chemical space.

Library (high-throughput or more modest) screening, and modifications of known drugs have been engines of the discovery process for a century. Along with combinatorial chemistry and computer assisted drug discovery (CADD), these methods have brought thousands of molecules to the clinic. But a certain ”drug-like” sameness often appears across therapeutic groups.  Perhaps for good reason (ADME, PK properties are optimized according to established conventions), but this sameness is at the expense of exploring truly novel chemical space. Happily, the discovery process is not static, and technologies are emerging to identify less obvious and less familiar-looking molecules.  In the oncology and antibiotic spaces, drugs arising from these methods might encounter less resistance.


Topics & Speakers:

  • LYTACs/PROTACsCarolyn Bertozzi, PhD, Professor of Chemical & Systems Biology and Radiology, Stanford University
  • Protein-protein interactionsMichelle Arkin, PhD, Co-director, Small Molecule Discovery Center (SMDC), Professor, Pharmaceutical Chemistry, UCSF    
  • Allosteric inhibitorsAdrian Gill, PhD, VP Medicinal Chemistry and CMC, REVOLUTION Medicines
  • Systems pharmacology and forward polypharmacologyMichael Keiser, PhD, Professor, Institute for Neurodegenerative Diseases, UCSF
  • Discovery at the academia/biotech borderline: Mark Smith, PhD, Head, ChEM-H Medicinal Chemistry Knowledge Center, Stanford University
  • AI meets fermentation: Maureen Hillenmeyer, PhD, CEO, Hexagon Bio      
  • Access to complex natural products: Ian Seiple, PhD, Professor in Residence, Cardiovascular Research Institute, UCSF
  • Fragment based drug discoveryDaniel Erlanson, PhD, VP of Chemistry, Frontier Medicines
  • Directed evolution: Chaitan Khosla, PhD, Professor of Chemical Engineering and Chemistry, Stanford University

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