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US 12,460,244 B2Granted
Inhibitors of RNA-guided nuclease activity and uses thereof
AssigneesThe Broad Institute, Inc., The Brigham and Women's Hospital, Inc.
InventorsAmit Choudhary, Kurt Cox
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Abstract
Compositions and methods are provided for the inhibition of the function of RNA guided endonucleases, including the identification and use of such inhibitors. Methods of identifying inhibitor compounds of RNA guided nucleases, assays for detecting nuclease activity and compounds for use therein are also provided.
Claims14
A method of inhibiting the nuclease activity of an RNA-guided endonuclease, the comprising contacting an RNA-guided endonuclease-guide complex with a compound of Formula I:
- wherein:
- R1 is hydrogen;
- R2 is selected from hydrogen,
- and aryl optionally substituted with one or more R10;
- R3 is hydrogen or C1-C3 alkyl;
- R4 is hydrogen or C1-C3 alkyl;
- R5 is C1-C3 alkyl or C3-C8 cycloalkyl each optionally substituted with one or more R11;
- each R10 is independently selected from halogen, C1-C3 alkyl, haloalkyl, and alkoxy;
- each R11 is independently selected from halogen, C1-C3 alkyl, haloalkyl, and alkoxy;
- and
- X is C1-C3 alkylalcohol.
8 more elements
Dependencies are inferred from the claim text.