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Fragment screening and assembly: a highly efficient approach to a selective and cell active protein tyrosine phosphatase 1B inhibitor.

Abstract：

:Using an NMR-based fragment screening and X-ray crystal structure-based assembly, starting with millimolar ligands for both the catalytic site and the second phosphotyrosine binding site, we have identified a small-molecule inhibitor of protein tyrosine phosphatase 1B with low micromolar inhibition constant, high selectivity (30-fold) over the highly homologous T-cell protein tyrosine phosphatase, and good cellular activity in COS-7 cells.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Liu G,Xin Z,Pei Z,Hajduk PJ,Abad-Zapatero C,Hutchins CW,Zhao H,Lubben TH,Ballaron SJ,Haasch DL,Kaszubska W,Rondinone CM,Trevillyan JM,Jirousek MR

doi

10.1021/jm034122o

keywords:

subject

Has Abstract

pub_date

2003-09-25 00:00:00

pages

4232-5

issue

20

eissn

0022-2623

issn

1520-4804

journal_volume

46

pub_type

杂志文章

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