Document Detail


Discovery of a novel competitive inhibitor of PTP1B by high-throughput screening.
MedLine Citation:
PMID:  18215359     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
AIM: The aim of the present study was to discover novel protein tyrosine phosphatase 1B (PTP1B) inhibitors. We expressed and purified the human PTP1B catalytic domain and set up a molecular level high-throughput screening (HTS) assay to screen a set of 48,000 pure compounds. RESULTS: HTS was finished with an averaged Zo factor of 0.63, and LGH00081, a competitive inhibitor of PTP1B with novel structure and relatively good selectivity for receptor-type protein tyrosine phosphatases, was identified. CONCLUSION: We established a molecular level assay which is useful for the screening of PTP1B inhibitors with therapeutic potential. The novel competitive PTP1B inhibitor LGH00081 offers a good start for structure modification and cellular functional activity study.
Authors:
Lei Shi; Hai-ping Yu; Yue-yang Zhou; Jun-qin Du; Qiang Shen; Jing-ya Li; Jia Li
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Acta pharmacologica Sinica     Volume:  29     ISSN:  1671-4083     ISO Abbreviation:  Acta Pharmacol. Sin.     Publication Date:  2008 Feb 
Date Detail:
Created Date:  2008-01-24     Completed Date:  2009-05-04     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  100956087     Medline TA:  Acta Pharmacol Sin     Country:  China    
Other Details:
Languages:  eng     Pagination:  278-84     Citation Subset:  IM    
Affiliation:
National Center for Drug Screening, Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Shanghai 201203, China.
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MeSH Terms
Descriptor/Qualifier:
Animals
CHO Cells
Catalysis
Cricetinae
Cricetulus
Drug Evaluation, Preclinical
Enzyme Inhibitors / chemical synthesis*,  pharmacology*
Humans
Phosphorylation
Protein Tyrosine Phosphatase, Non-Receptor Type 1 / antagonists & inhibitors*,  chemistry,  genetics
Tyrosine / metabolism
Chemical
Reg. No./Substance:
0/Enzyme Inhibitors; 55520-40-6/Tyrosine; EC 3.1.3.48/PTPN1 protein, human; EC 3.1.3.48/Protein Tyrosine Phosphatase, Non-Receptor Type 1

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