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US 9,810,690 B2Granted
Method for screening inhibitors of Ras
AssigneeAraxes Pharma LLC
InventorsMatthew P. Patricelli, Ulf Peters, Liansheng Li, Pingda Ren, Yi Liu
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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.
Claims30
A method of selecting a Ras antagonist, the method comprising:
- (a) combining in a reaction mixture a mutant Ras, a competition probe, and a test compound;
- and
- (b) detecting a decrease in binding between the mutant Ras and the competition probe as compared to binding of the competition probe to the mutant Ras in an absence of the test compound;
- wherein:
- i. the mutant Ras comprises a truncated or full-length sequence according to SEQ ID NO:
- 1, SEQ ID NO:
- 2, SEQ ID NO:
- 3, or SEQ ID NO:
- 4, that is mutated to have up to 20 mutations including mutation of SEQ ID NO:
- 1, SEQ ID NO:
- 2, SEQ ID NO:
- 3, or SEQ ID NO:
- 4 at amino acid residue 62, 92, or 95 to cysteine;
- ii. the competition probe is capable of binding and covalently modifying the mutant Ras;
- and
- iii. the decrease in binding between the mutant Ras and the competition probe is indicative of Ras antagonist activity of the test compound.
13 more elements
A mutant Ras comprising a truncated or full-length sequence according to SEQ ID NO:
- 1, SEQ ID NO:
- 2, SEQ ID NO:
- 3, or SEQ ID NO:
- 4, that is mutated to have up to 20 mutations including mutation of SEQ ID NO:
- 1, SEQ ID NO:
- 2, SEQ ID NO:
- 3, or SEQ ID NO:
- 4 at amino acid residue 62, 92, or 95 to cysteine, wherein said mutant Ras exhibits the ability to react with a competition probe capable of binding and covalently modifying said mutant Ras.
5 more elements
Dependencies are inferred from the claim text.