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Bioorg Med Chem Lett. 2003 Jun 2;13(11):1887-90.

Potent, selective inhibitors of protein tyrosine phosphatase 1B.

Author information

1
Metabolic Disease Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064-6098, USA.

Abstract

We have previously reported a novel series of oxalyl-aryl-amino benzoic acid-based, catalytic site-directed, competitive, reversible protein tyrosine phosphatase 1B (PTP1B) inhibitors. With readily access to key intermediates, we utilized a solution phase parallel synthesis approach and rapidly identified a highly potent PTP1B inhibitor (19, K(i)=76 nM) with moderate selectivity (5-fold) over T-cell PTPase (TCPTP) through interacting with a second phosphotyrosine binding site (site 2) in the close proximity to the catalytic site.

PMID:
12749891
DOI:
10.1016/s0960-894x(03)00302-0
[Indexed for MEDLINE]

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