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OwnerAnne-Claude Dublanchet, Charles Andrianjara +9inventors
InventorsAnne-Claude Dublanchet, Charles Andrianjara, Roger Wrigglesworth, Claude Bertrand, Pierre Ducrot, Renaud Morales, Venkataraman Thanabal, Alexander G. Pavlovsky, Margaret M. O'Gara, Jennifer M. Thorn, Delphine Compere
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The invention relates to compounds that are selective inhibitors of matrix metalloproteinases, to pharmaceutical compositions containing them and to their use in the prevention and/or treatment of MMP-associated diseases. The invention also relates to methods for identification of lead compounds that are selective inhibitors of matrix metalloproteinases. The compounds have the properties that they: (a) bind allosterically to a matrix metalloproteinase or small group of metallic metalloproteinases; (b) bind into at least the S1′ pocket, at least the S1″ pocket (as defined) or at least the S1′ pocket and the S1″ pocket of said matrix metalloproteinase; and (c) exhibit selectivity for a matrix metalloproteinase or group of matrix metalloproteinases other than MMP-13.
A compound that is a matrix metalloproteinase inhibitor, and that:
A method for identifying a matrix metalloproteinase inhibitor whose potency is relatively insensitive to concentration of substrate, said method comprising comparing the IC50 of a test compound using a full-length MMP or a catalytic domain thereof in the presence and in the absence of a ligand that chelates readily to zinc but is a sufficiently small molecule that it does not substantially interfere with the binding of the inhibitor to its intended location adjacent to the catalytic domain.
Dependencies are inferred from the claim text.