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Patent Searching and Data


Title:
METHOD FOR SCREENING INHIBITORS OF RAS
Document Type and Number:
WIPO Patent Application WO/2017/070256
Kind Code:
A8
Abstract:
Provided herein are compositions, reactions mixtures, mutant Ras proteins, kits, substrates, and systems for selecting a Ras antagonist, as well as methods of using the same. The present disclosure provides a method of selecting a Ras antagonist. In some embodiments, the method comprises a mutant Ras, wherein the mutant Ras comprises a cysteine mutation; a competition probe, and a test compound;, and detecting binding between the mutant Ras and the competition probe; comparing the binding between the mutant Ras and the competition probe in the absence of the test compound; wherein a decrease in binding between the mutant Ras and the competition probe is indicative of Ras antagonist activity of the test compound. In some embodiments, the cysteine mutation is E62C; E72C; A100C; E73C; D92C; H102C; Q130C; E103C; A103C; E1 10C; H95C; Q95C; L95C; R105C; Q133C; K106C; D106C; E106C; or E1 13C relative to SEQ ' ID NO: 1.

Inventors:
PATRICELLI MATTHEW P (US)
PETERS ULF (US)
LI LIANSHENG (US)
REN PINGDA (US)
LIU YI (US)
Application Number:
US2016/057774
Publication Date:
June 08, 2017
Filing Date:
October 19, 2016
Export Citation:
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Assignee:
ARAXES PHARMA LLC (US)
International Classes:
A61K31/496; A61K31/517; C07D239/74; C07D239/94; C07D239/95; C07D241/04
Attorney, Agent or Firm:
WONG, Karen et al. (650 Page Mill RoadPalo Alto, CA, US)
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