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US 10,788,496 B2Granted
MEK1 mutation conferring resistance to RAF and MEK inhibitors
AssigneeDana-Farber Cancer Institute, Inc.
InventorsLevi A. Garraway, Caroline Emery, Nikhil Wagle
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Abstract
Nucleic acids and proteins having a mutant MEK sequence, and methods concerning identification of patients having resistance to treatment with anti-cancer agents, specifically inhibitors of RAF or MEK are provided. Methods of treatment and for optimizing treatment for patients having a mutation in a MEK1 sequence are also provided.
Claims5
A method of identifying a compound effective for inhibiting a mutant MEK1 protein having a C121S amino acid substitution, the method comprising:
- a) providing a live cell expressing a mutant MEK1 protein having MEK1 activity comprising an amino acid substitution at position 121 of wild-type MEK1 protein shown in SEQ ID NO:
- 2 where the amino acid substitution is a C121S amino acid substitution, and a MEK substrate;
- b) contacting the cell with a test compound;
- and
- c) determining the effect of the compound on phosphorylation of the MEK substrate in the cell;
- wherein down-modulation of phosphorylation of the MEK substrate as compared to the mutant MEK1 protein not treated with the test compound identifies the test compound as a compound effective for inhibiting a mutant MEK1 protein having a C121S amino acid substitution.
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Dependencies are inferred from the claim text.