COMPOSITIONS AND METHODS FOR TREATING CANCER
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Accused Products
Abstract
Disclosed herein, inter alia, are compositions and methods for modulating Ras and treating cancer.
0 Citations
62 Claims
- 1. A compound having the formula:
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2-18. -18. (canceled)
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21-22. -22. (canceled)
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25-26. -26. (canceled)
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28-31. -31. (canceled)
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33-40. -40. (canceled)
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42-43. -43. (canceled)
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44. A method of identifying a covalent inhibitor of K-Ras protein comprising:
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contacting a K-Ras protein with a K-Ras inhibitor test compound; allowing said K-Ras inhibitor test compound to covalently inhibit said K-Ras protein; detecting the level of covalent inhibition of said K-Ras protein thereby identifying a covalent inhibitor of K-Ras protein.
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45-51. -51. (canceled)
- 52. A human K-Ras inhibitor, wherein said human K-Ras inhibitor is a Switch 2 Groove binding compound.
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59. A K-Ras protein covalently bound to a compound, wherein said compound is covalently bound to a cysteine residue of said K-Ras protein and said compound contacts at least one amino acid residue of said K-Ras protein selected from V7, V9, T58, A59, G60, Y64, R68, D69, Y71, M72, R73, F78, K88, E91, D92, H94, H95, Y96, R97, Q99, I100, R102, and V103.
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60. A method of modulating the activity of a K-Ras protein, said method comprising contacting said K-Ras protein with an effective amount of a human K-Ras modulator, wherein said human K-Ras modulator is a Switch 2 Groove binding compound.
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61. A method of inhibiting the activity of a K-Ras protein, said method comprising contacting said K-Ras protein with an effective amount of a human K-Ras inhibitor, wherein said human K-Ras inhibitor is a Switch 2 Groove binding compound.
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62. A method of treating cancer in a patient in need of such treatment, said method comprising administering a therapeutically effective amount of a compound to said patient, wherein said compound is a Switch 2 Groove binding compound.
Specification