Matrix metalloproteinase inhibitors: a structure-activity study

…, F Lapierre, W Liang, W Ye, CW Lange…

Index: Levy, Daniel E.; Lapierre, France; Liang, Weisheng; Ye, Wenqing; Lange, Christopher W.; Li, Xiaoyuan; Grobelny, Damian; Casabonne, Marie; Tyrrell, David; Holme, Kevin; Nadzan, Alex; Galardy, Richard E. Journal of Medicinal Chemistry, 1998 ,  vol. 41,  # 2  p. 199 - 223

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Citation Number: 186

Abstract

Modifications around the dipeptide-mimetic core of a hydroxamic acid based matrix metalloproteinase inhibitor were studied. These variations incorporated a variety of natural, unnatural, and synthetic amino acids in addition to modifications of the P1'and P3'substituents. The results of this study indicate the following structural requirements:(1) Two key hydrogen bonds must be present between the enzyme and potent substrates.(2) ...