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DTSTART:20210314T080000
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BEGIN:VEVENT
DTSTART;TZID=America/Chicago:20210423T100000
DTEND;TZID=America/Chicago:20210423T110000
DTSTAMP:20260521T183610
CREATED:20210304T184812Z
LAST-MODIFIED:20220405T131937Z
UID:24585-1619172000-1619175600@www.warf.org
SUMMARY:New Strategies to Drug Challenging Targets by Exploiting Covalent Targeting\, Beyond Rule of 5 Bitopic Ligands and Binary Pharmacology
DESCRIPTION:The GTP-ase K-Ras represents the most frequently altered oncogene in cancer patients. Directly targeting K-Ras is difficult due to its picomolar affinity for GTP/GDP and the absence of easily identifiable allosteric sites. \nKevan M. Shokat\, a professor of cellular and molecular pharmacology at UCSF\, a professor of chemistry at UC Berkeley and an investigator with the Howard Hughes Medical Institute\, will describe the discovery of small molecules that covalently bind to a common oncogenic mutant\, K-RasG12C. These compounds have served as a blueprint for the development of multiple K-RasG12C drugs currently undergoing clinical investigation. \nMany drug discovery efforts are hampered by the size limit of cell permeable ligands. Shokat will discuss an unusually large (>1700Da) bitopic ligand termed Rapa-Link which inhibits all drug resistant forms of the nutrient sensor kinase\, mTOR. The particular physicochemical properties of this molecule can be exploited to overcome a common challenge in drug discovery termed on target/off tissue toxicity by leveraging a new binary pharmacology platform. \nThis seminar is part of the Pharmaceutical Sciences Seminar Series/WARF Therapeutics Distinguished Lecture in Drug Discovery. To obtain the Webex link\, contact Debra King at Debra.King@wisc.edu.
URL:https://www.warf.org/event/new-strategies-to-drug-challenging-targets-by-exploiting-covalent-targeting-beyond-rule-of-5-bitopic-ligands-and-binary-pharmacology/
LOCATION:Virtual
CATEGORIES:Inventors, Entrepreneurs & Researchers,WARF Website
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END:VEVENT
END:VCALENDAR