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[Free Online Symposium] No More Undruggables: Unconventional Approaches for Drug Discovery and Design – prodrugs, PROTACS, fragment-based design, directed evolution and beyond

CA

10/29/2020 - 10/30/2020

4:00pm - 12:00pm

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

Library 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, these methods have brought thousands of molecules to the clinic. But a certain ”drug-like” sameness often appears across therapeutic groups. This may be 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 in particular, drugs arising from these methods might encounter less resistance. Much as we once naively talked about “junk DNA” and “undruggable” targets, we now have the insight and tools to understand the therapeutic potential inherent in complex biological systems.

Thursday October 29, 4-7 PM (US Pacific Time)
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.

Friday October 30, 9AM – noon (US Pacific Time)
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.

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Online via Zoom