A highly efficient route to enantiomerically pure L-N-Bz-Pmp(t-Bu)(2)-OH and incorporation into a peptide-based protein tyrosine phosphatase inhibitor

Article de journal

Auteurs / Editeurs

Barrios, António

Domaines de Recherche

Health sciences (Medical and Health sciences)

Neuroscience

Détails sur la publication

Liste des auteurs: Hubbard CE, Barrios AM

Editeur: Elsevier

Année de publication: 2008

Numéro du volume: 18

Numéro de publication: 2

Page d'accueil: 679

Dernière page: 681

Nombre de pages: 3

ISSN: 0960-894X

Languages: Anglais-Royaume-Uni (EN-GB)

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Résumé

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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