Conformationally constrained phosphotyrosyl mimetics designed as monomeric Src homology 2 domain inhibitors

TR Burke Jr, JJ Barchi, C George, G Wolf…

Index: Burke Jr.; Barchi Jr.; George; Wolf; Shoelson; Yan Journal of Medicinal Chemistry, 1995 , vol. 38, # 8 p. 1386 - 1396

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Citation Number: 78

Abstract

Inhibitors of specific src homology 2 (SH2) domain binding interactions could potentially afford new therapeutic approaches toward a variety of diseases, including several cancers. To date SH2 domain inhibitors have been confined to small phosphotyrosyl (pTyr)- containing peptides that appear to bind along the surface of SH2 domains with specific recognition features protruding into the protein. Among these protrusions is the pTyr ...

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Indanylacetic acids as PPAR-δ activator insulin sensitizers

[Wickens, Philip; Zhang, Chengzhi; Ma, Xin; Zhao, Qian; Amatruda, John; Bullock, William; Burns, Michael; Cantin, Louis-David; Chuang, Chih-Yuan; Claus, Thomas; Dai, Miao; Dela Cruz, Fernando; Dickson, David; Ehrgott, Frederick J.; Fan, Dongping; Heald, Sarah; Hentemann, Martin; Iwuagwu, Christiana I.; Johnson, Jeffrey S.; Kumarasinghe, Ellalahewage; Ladner, David; Lavoie, Rico; Liang, Sidney; Livingston, James N.; Lowe, Derek; Magnuson, Steve; Mannelly, Gretchen; Mugge, Ingo; Ogutu, Herbert; Pleasic-Williams, Susan; Schoenleber, Robert W.; Shapiro, Jeff; Shelekhin, Tatiana; Sweet, Laurel; Town, Christopher; Tsutsumi, Manami Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 15 p. 4369 - 4373]