Novel and Selective Inactivators for Matrix Metalloproteases Involved in Breast Cancer Metastasis
Annual rept. 13 Jun 1998-12 Jun 1999
WAYNE STATE UNIV DETROIT MI
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Matrix metalloproteases MMPs are endopeptidases with a diverse set of physiological and pathological functions. Two of these proteases, MMP-2 and MMP-9, also known as gelatinases A and B, respectively, have been implicated in breast tumor metastasis. This research endeavors to prepare the first mechanism-based inactivators for these enzymes, molecules which are expected to show high selectivity in inactivation of the targeted enzymes. Toward this goal, several such putative inactivators were designed and synthesized in the Mobashery laboratory in the past year. Initial characterization with the enzyme indicated that one of these molecules showed the desired inactivating trait, but it exhibited relatively low affinities for the gelatinases. Work in on-going in the design of derivatives of higher affinity.
- Medicine and Medical Research