Potent inhibition of insulin receptor dephosphorylation by a hexamer peptide containing the phosphotyrosyl mimetic F2Pmp.
摘要：
Phosphonomethyl phenylalanine (Pmp) is a non-hydrolyzable phosphotyrosyl (pTyr) mimetic, which has been incorporated into eleven-mer Pmp-containing that have previously been reported to competitively inhibit the and . We have recently shown that phosphonodifluoromethyl phenylalanine (F2Pmp) is superior to Pmp as a pTyr mimetic in domain-. Herein we find using the hexameric sequence Ac-D-A-D-E-X-L-, where X = (D/L)-Pmp or L-F2Pmp, that the half maximal inhibition values of these two against -mediated of autophosphorylated to be 200 microM and 100 nM, respectively. These data indicate that F2Pmp induces a three orders of magnitude enhancement in affinity relative to Pmp, resulting in an exceptionally potent -based inhibitor. We conclude that F2Pmp may be a generally useful tool in the preparation of selective, high affinity inhibitors.
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DOI：
10.1006/bbrc.1994.2435
被引量：
年份：
1994
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