期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 18, 期 2, 页码 679-681出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2007.11.056
关键词
tyrosine phosphatase; phosphotyrosine analogs; phosphonomethylphenylalanine; enzyme inhibition
资金
- NINDS NIH HHS [R21 NS056945, R21 NS056945-01] Funding Source: Medline
Phosphonomethyl phenylalanine (Pmp), a nonhydrolyzable mimic of phosphotyrosine, is an important building block in the development of peptide-based PTP inhibitors. We have designed a novel, efficient synthesis of N-Bz-Pmp(t-Bu)(2)-OH. A Pmp-containing peptide based on a known biological substrate of the tyrosine phosphatase CD45 (Ac-TEGQ-Pmp-QPQP-NH2) inhibits CD45 with an IC50 value of approximately 100 mu M with virtually no inhibition of TCPTP up to concentrations of 120 mu M. (c) 2007 Elsevier Ltd. All rights reserved.
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