Identification of novel molecular scaffolds for the design of MMP-13 inhibitors: a first round of lead optimization

V La Pietra, L Marinelli, S Cosconati, FS Di Leva…

Index: La Pietra, Valeria; Marinelli, Luciana; Cosconati, Sandro; Di Leva, Francesco Saverio; Nuti, Elisa; Santamaria, Salvatore; Pugliesi, Isabella; Morelli, Matteo; Casalini, Francesca; Rossello, Armando; La Motta, Concettina; Taliani, Sabrina; Visse, Robert; Nagase, Hideaki; Da Settimo, Federico; Novellino, Ettore European Journal of Medicinal Chemistry, 2012 , vol. 47, # 1 p. 143 - 152

Full Text: HTML

Citation Number: 13

Abstract

Osteoarthritis (OA) is the leading cause of joint pain and disability in middle-aged and elderly patients, and is characterized by progressive loss of articular cartilage. Among the various matrix metalloproteinases (MMPs), MMP-13 is specifically expressed in the cartilage of human OA patients and is not present in normal adult cartilage. Thus, MMP-13-selective inhibitors are promising candidates in osteoarthritis therapy. Recently, we designed an N- ...