Method of cell surface activation and inhibition

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

C - Chemistry, Metallurgy

12

N

C12N 9/64 (2006.01) C12Q 1/37 (2006.01)

Patent

CA 2266410

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 Asp656, but which can also include other residues in the Ge1A-CTD domain with which Asp656 forms a contiguous surface, namely Gly651, Phe650, and Tyr636. 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.

L'invention concerne des procédés d'activation et d'inhibition de surface cellulaire faisant intervenir l'interaction d'un inhibiteur de métalloprotéase matricielle appelée TIMP-2, avec l'enzyme gélatinase-A (GelA). Un élément particulièrement important dans les procédés de l'invention est la découverte d'un site de liaison unique de TIMP-2 sur la surface du domaine C-terminal (GelA-CTD) de l'enzyme, lequel a été déterminé comme étant Asp<656>, mais présente également d'autres restes dans le domaine GelA-CTD avec lesquels Asp<656> forme une surface contiguë, c'est-à-dire Gly<651>, Phe<650>, et Tyr<636>. L'identification de ce site de liaison constitue une cible utile pour le criblage d'inhibiteurs de MMP et dans le pronostic et le traitement de maladies dans lesquelles des MMP sont impliquées. Des composés inhibiteurs potentiels de MMP peuvent être structurés afin d'inhiber de manière compétitive l'activation d'une surface cellulaire.

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