Discovery of orally active nonpeptide vitronectin receptor antagonists based on a 2-benzazepine Gly-Asp mimetic

…, DP Alberts, PK Bhatnagar, WE Bondinell…

Index: Miller, William H.; Alberts, Doreen P.; Bhatnagar, Pradip K.; Bondinell, William E.; Callahan, James F.; Calvo, Raul R.; Cousins, Russell D.; Erhard, Karl F.; Heerding, Dirk A.; Keenan, Richard M.; Kwon, Chet; Manley, Peter J.; Newlander, Kenneth A.; Ross, Stephen T.; Samanen, James M.; Uzinskas, Irene N.; Venslavsky, Joseph W.; Yuan, Catherine C. -K; Haltiwanger, R. Curtis; Gowen, Maxine; Hwang, Shing-Mei; James, Ian E.; Lark, Michael W.; Rieman, David J.; Stroup, George B.; Azzarano, Leonard M.; Salyers, Kevin L.; Smith, Brian R.; Ward, Keith W.; Johanson, Kyung O.; Huffman, William F. Journal of Medicinal Chemistry, 2000 , vol. 43, # 1 p. 22 - 26

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Citation Number: 119

Abstract

Introduction. The vitronectin receptor, also known as Rvβ3, is a member of the integrin family of heterodimeric transmembrane glycoprotein complexes that function in cellular adhesion events and signal transduction processes. 1 Integrin Rvβ3 is expressed on almost all cells originating from the mesenchyme and has been shown to mediate several biologically relevant processes, including adhesion of osteoclasts to the bone matrix, 2-5 migration of ...