Method of cell surface activation and inhibition

Details Method of cell surface activation and inhibition Method of cell surface activation and inhibition

1997-09-05

2000-02-08

Tsang, Cecilia J.

Chemistry: natural resins or derivatives; peptides or proteins;

Peptides of 3 to 100 amino acid residues

15 to 23 amino acid residues in defined sequence

530324, 530325, 514 13, A61K 3816

Patent

active

060229489

ABSTRACT:
Disclosed are methods of cell surface activation and inhibition that involve the interaction of an inhibitor of matrix metalloprotease known as TIMP-2, with the enzyme, gelatinase-A (GelA). Critical to the methods of the invention is the discovery of a unique TIMP-2 binding site on the surface of the C-terminal domain (GelA-CTD) of the enzyme, which has been determined to be Asp.sup.656, but which can also included other residues in the GelA-CTD domain with which Asp.sup.656 forms a contiguous surface, namely Gly.sup.651, Phe.sup.650, and Tyr.sup.636 Identification of this binding site provides a useful target for the screening of MMP inhibitors and for prognosis and treatment of diseases in which MMPs are implicated. Compounds which are candidate MMP inhibitors can be structured to competitively inhibit cell surface activation.

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