268741-89-5Relevant academic research and scientific papers
Bicyclic signal transduction inhibitors, compositions containing them and uses thereof
-
, (2008/06/13)
This invention concerns compounds for inhibiting intracellular signal transduction, especially intracellular signal transduction mediated by one or more molecular interactions involving a phosphotyrosine-containing protein. This invention also relates to
A novel phosphotyrosine mimetic 4′-carboxymethyloxy-3′-phosphonophenylalanine (Cpp): Exploitation in the design of nonpeptide inhibitors of pp60Src SH2 domain
Kawahata, Noriyuki,Yang, Michael G.,Luke, George P.,Shakespeare, William C.,Sundaramoorthi, Raji,Wang, Yihan,Johnson, Daniel,Merry, Taylor,Violette, Shelia,Guan, Wei,Bartlett, Catherine,Smith, Jeremy,Hatada, Marcos,Lu, Xiaode,Dalgarno, David C.,Eyermann, Charles J.,Bohacek, Regine S.,Sawyer, Tomi K.
, p. 2319 - 2323 (2007/10/03)
The novel phosphotyrosine (pTyr) mimetic 4′-carboxymethyloxy-3′-phosphonophenylalanine (Cpp) has been designed and incorporated into a series of nonpeptide inhibitors of the SH2 domain of pp60c-Src (Src) tyrosine kinase. A 2.2 A X-ray crystal structure of 1a bound to a mutant form of Lck SH2 domain provides insight regarding the structure-activity relationships and supports the design concept of this new pTyr mimetic.
