SCREENING METHOD FOR GPCR LIGANDS
First Claim
1. A method of identifying a compound capable of binding to a target domain of a G-protein coupled receptor comprising the steps of:
- (a) providing a receptor comprising said target domain and a first group(b) bringing into contact said receptor of (a) with a test molecule comprising a(c) determining, subsequent to the binding of said first group to said second.
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Abstract
This invention relates to a method of identifying a compound capable of binding to a target domain of a G-protein coupled receptor comprising the steps of: (a) providing a receptor comprising said target domain and a first group linked to said target domain; (b) bringing into contact said receptor of (a) with a test molecule comprising a second group and said compound linked to each other, wherein said first group binds said second group; and (c) determining, subsequent to the binding of said first group to said second group, whether said compound binds to said target domain.
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Citations
45 Claims
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1. A method of identifying a compound capable of binding to a target domain of a G-protein coupled receptor comprising the steps of:
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(a) providing a receptor comprising said target domain and a first group (b) bringing into contact said receptor of (a) with a test molecule comprising a (c) determining, subsequent to the binding of said first group to said second. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 31, 34, 42, 43, 45)
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29. A kit comprising a library of test molecules, wherein each test molecule comprises:
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(i) a peptide comprising or consisting of the sequence of any one of SEQ ID NO;
1 to 3, or a sequence having at least 70% sequence identity to said sequence of any(iii) the linker is selected from the group consisting of alkyl with 1 to 30 carbon atoms, polyethylene glycol with 1 to 20 ethylene moieties, polyalanine with 1 to 20
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30. A kit comprising a library of test molecules, wherein each test molecule comprises:
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(i) a peptide consisting of the sequence of any one of secretin, VIP, PACAP, adrenomedullin, calcitonin, amylin or CGRP, wherein between 1 and 10 N-terminal amino acids are deleted from said peptide, or a sequence having at least 70% sequence identity to the truncated peptide, or an analog thereof, linked to (H) a member of a library of compounds;
wherein(iii) the linker is selected from the group consisting of alkyl with 1 to 30 carbon atoms, polyethylene glycol with 1 to 20 ethylene moieties, polyalanine with 1 to 20
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32. A compound comprising or consisting of.
(i) a peptide comprising or consisting of the sequence of any one of SEQ ID (ii) a first reactive group, wherein (iii) the linker is selected from the group consisting of alkyl with 1 to 30 carbon atoms, polyethylene glycol with 1 to 20 ethylene moieties, polyalanine with 1 to 20
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33. A compound comprising:
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(i) a peptide consisting of the sequence of any one of secretin, VIP, PACAP, adrenomedullin, calcitonin, amylin or CGRP, wherein between 1 and 10 N-terminal amino acids are deleted from said peptide, or a sequence having at least 70% sequence identity to the truncated peptide, or an analog thereof, linked to (ii) a first reactive group;
wherein(iii) the linker is selected from the group consisting of alkyl with 1 to 30 carbon atoms, polyethylene glycol with 1 to 20 ethylene moieties, polyalanine with 1 to 20 - View Dependent Claims (44)
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36. A chimeric G-protein coupled receptor comprising:
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(i) a class A or a class C G-protein coupled receptor or a fragment thereof (ii) the N-terminal domain of a class B G-protein coupled receptor or a fragment of - View Dependent Claims (37, 38, 39, 40, 41)
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Specification