Discovery and SAR of novel, potent and selective protein tyrosine phosphatase 1B inhibitors

Zhonghua Pei; Xiaofeng Li; Gang Liu; Cele Abad-Zapatero; Tom Lubben; Tianyuan Zhang; Stephen J Ballaron; Charles W Hutchins; James M Trevillyan; Michael R Jirousek

doi:10.1016/s0960-894x(03)00725-x

Discovery and SAR of novel, potent and selective protein tyrosine phosphatase 1B inhibitors

Bioorg Med Chem Lett. 2003 Oct 6;13(19):3129-32. doi: 10.1016/s0960-894x(03)00725-x.

Authors

Zhonghua Pei¹, Xiaofeng Li, Gang Liu, Cele Abad-Zapatero, Tom Lubben, Tianyuan Zhang, Stephen J Ballaron, Charles W Hutchins, James M Trevillyan, Michael R Jirousek

Affiliation

¹ Metabolic Disease Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064-6098, USA. [email protected]

PMID: 12951078
DOI: 10.1016/s0960-894x(03)00725-x

Abstract

A salicylate second site binder was linked to three classes of phosphotyrosine mimetics to produce potent protein tyrosine phosphatase 1B (PTP1B) inhibitors which exhibit significant selectivity against other phosphatases including the most homologous member, TCPTP.

MeSH terms

Enzyme Inhibitors / chemistry*
Enzyme Inhibitors / pharmacology
Humans
Protein Tyrosine Phosphatase, Non-Receptor Type 1
Protein Tyrosine Phosphatases / antagonists & inhibitors*
Protein Tyrosine Phosphatases / chemistry*
Protein Tyrosine Phosphatases / metabolism
Structure-Activity Relationship

Substances

Enzyme Inhibitors
PTPN1 protein, human
Protein Tyrosine Phosphatase, Non-Receptor Type 1
Protein Tyrosine Phosphatases