R-isomers of Arg-Gly-Asp (RGD) mimics as potent α v β 3 inhibitors

SR Nagarajan, B Devadas, JW Malecha, HF Lu…

Index: Nagarajan, Srinivasan R.; Devadas, Balekudru; Malecha, James W.; Lu, Hwang-Fun; Ruminski, Peter G.; Rico, Joseph G.; Rogers, Thomas E.; Marrufo, Laura D.; Collins, Joe T.; Kleine, H. Peter; Lantz, Melissa K.; Zhu, Jun; Green, Nawasa F.; Russell, Mark A.; Landis, Bryan H.; Miller, Lawrence M.; Meyer, Debra M.; Duffin, Tiffany D.; Engleman, V. Wayne; Finn, Mary B.; Freeman, Sandra K.; Griggs, David W.; Williams, Melanie L.; Nickols, Maureen A.; Pegg, Jodi A.; Shannon, Kristen E.; Steininger, Christina; Westlin, Marisa M.; Nickols, G. Alan; Keene, Jeffery L. Bioorganic and Medicinal Chemistry, 2007 , vol. 15, # 11 p. 3783 - 3800

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Citation Number: 23

Abstract

The integrin αvβ3, vitronectin receptor, is expressed in a number of cell types and has been shown to mediate adhesion of osteoclasts to bone matrix, vascular smooth muscle cell migration, and angiogenesis. We recently disclosed the discovery of a tripeptide Arg-Gly- Asp (RGD) mimic, which has been shown to be a potent inhibitor of the integrin αvβ3 and has excellent anti-angiogenic properties including its suppression of tumor growth in ...