Methods for identifying allosteric sites
First Claim
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1. A method of identifying an allosteric site comprising:
- a) providing a target comprising a first binding site, a second binding site, and a chemically reactive group at or near the second binding site;
b) contacting the target with a compound that is capable of forming a covalent bond with the chemically reactive group;
c) forming a covalent bond between the target and the compound thereby forming a target-compound conjugate;
d) determining whether the target-compound conjugate possesses a change in the primary binding site as compared with the target.
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Abstract
The present invention relates to exosites and methods for identifying exosites in protein targets. The present invention also relates to methods for identifying allosteric sites and identifying compounds that bind therein.
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Citations
20 Claims
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1. A method of identifying an allosteric site comprising:
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a) providing a target comprising a first binding site, a second binding site, and a chemically reactive group at or near the second binding site;
b) contacting the target with a compound that is capable of forming a covalent bond with the chemically reactive group;
c) forming a covalent bond between the target and the compound thereby forming a target-compound conjugate;
d) determining whether the target-compound conjugate possesses a change in the primary binding site as compared with the target. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14)
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15. A method of identifying an allosteric inhibitor comprising:
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a) performing a first tethering experiment and b) performing a second tethering experiment wherein both tethering experiments comprise;
i) providing a target comprising a first binding site, a second binding site, and a chemically reactive group at or near the second binding site;
ii) contacting the target with a compound that is capable of forming a covalent bond with the chemically reactive group;
iii) forming covalent bond between the target and the compound thereby forming a target-compound conjugate; and
iv) identifying the target-compound conjugate wherein the first tethering experiment is performed in the presence of a ligand that binds to the first binding site and the second tethering experiment is performed in the absence of the ligand that binds to the first binding site. - View Dependent Claims (16, 17, 18)
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19. A method of identifying an allosteric inhibitor comprising:
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a) providing a target that is capable of allosteric regulation and a mutant thereof that is not capable of allosteric regulation;
b) contacting the target with a compound;
c) contacting the mutant with the compound; and
d) comparing the activity of the compound against the target with the activity of the compound against mutant.
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20. An allosteric inhibitor of a caspase.
Specification