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Formylchromone derivatives as irreversible and selective inhibitors of human protein tyrosine phosphatase 1B. Kinetic and modeling studies.

Abstract：

:A series of formylchromone derivatives were synthesized as PTP1B inhibitors and some of them were potent against PTP1B with IC50 values as low as 1.0 microM. They exhibited remarkable selectivity for PTP1B over other human PTPases. Kinetic studies revealed that formylchromone derivatives are irreversible and active site-directed inhibitors. Molecular modeling study identified the orientation of the inhibitor bound at the active site of PTP1B.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Shim YS,Kim KC,Lee KA,Shrestha S,Lee KH,Kim CK,Cho H

doi

10.1016/j.bmc.2004.11.006

subject

Has Abstract

pub_date

2005-02-15 00:00:00

pages

1325-32

issue

4

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(04)00884-3

journal_volume

13

pub_type

杂志文章

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