Bioorganic and Medicinal Chemistry Letters p. 2319 - 2323 (2001)
Update date:2022-07-30
Topics:
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.
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.
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(1951)