LO-(2-malonyl) tyrosine: a new phosphotyrosyl mimetic for the preparation of Src homology 2 domain inhibitory peptides
…, SE Shoelson, G Wolf, S Giorgetti-Peraldi…
Index: Ye, Bin; Akamatsu, Miki; Shoelson, Steven E.; Wolf, Gert; Giorgetti-Peraldi, Sophie; et al. Journal of Medicinal Chemistry, 1995 , vol. 38, # 21 p. 4270 - 4275
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Citation Number: 85
Abstract
domain (Ac-N-(L-OMTI-VNIE-amide, 12, IC50= 120 pM), and the N-terminal SH-PTP2 SH2 domain (Ac-LN-(L-OMTI-IDLDLV-amide, 13, IC50= 22.0 pM), These results show that peptides 10, 11, 13, and 14 have reasonable affinity for their respective SH2 domains, with the IC50 value for the SH-PTP2 SH2 domain-directed peptide 13 being equivalent to that previously observed for the corresponding FzPmp-containing peptide. OMT may afford a ...
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