293330-11-7Relevant academic research and scientific papers
Structure activity relationships of αv integrin antagonists for pulmonary fibrosis by variation in aryl substituents
Adams, James,Anderson, Edward C.,Blackham, Emma E.,Chiu, Yin Wa Ryan,Clarke, Thomas,Eccles, Natasha,Gill, Luke A.,Haye, Joshua J.,Haywood, Harvey T.,Hoenig, Christian R.,Kausas, Marius,Le, Joelle,Russell, Hannah L.,Smedley, Christopher,Tipping, William J.,Tongue, Tom,Wood, Charlotte C.,Yeung, Jason,Rowedder, James E.,Fray, M. Jonathan,McInally, Thomas,Macdonald, Simon J. F.
supporting information, p. 1207 - 1212 (2015/04/27)
Antagonism of αvβ6 is emerging as a potential treatment of idiopathic pulmonary fibrosis based on strong target validation. Starting from an αvβ3 antagonist lead and through simple variation in the nature and position of the aryl substituent, the discovery of compounds with improved αvβ6 activity is described. The compounds also have physicochemical properties commensurate with oral bioavailability and are high quality starting points for a drug discovery program. Compounds 33S and 43E1 are pan αv antagonists having ca. 100 nM potency against αvβ3, αvβ5, αvβ6, and αvβ8 in cell adhesion assays. Detailed structure activity relationships with these integrins are described which also reveal substituents providing partial selectivity (defined as at least a 0.7 log difference in pIC50 values between the integrins in question) for αvβ3 and αvβ5.
R-Isomers of Arg-Gly-Asp (RGD) mimics as potent αvβ3 inhibitors
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.
, p. 3783 - 3800 (2008/02/11)
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
