Literature DB >> 16303309

Bicyclic and tricyclic thiophenes as protein tyrosine phosphatase 1B inhibitors.

A F Moretto1, S J Kirincich, W X Xu, M J Smith, Z-K Wan, D P Wilson, B C Follows, E Binnun, D Joseph-McCarthy, K Foreman, D V Erbe, Y L Zhang, S K Tam, S Y Tam, J Lee.   

Abstract

A novel pyridothiophene inhibitor of PTP1B was discovered by rational screening of phosphotyrosine mimics at high micromolar concentrations. The potency of this lead compound has been improved significantly by medicinal chemistry guided by X-ray crystallography and molecular modeling. Excellent consistency has been observed between structure-activity relationships and structural information from PTP1B-inhibitor complexes.

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Year:  2005        PMID: 16303309     DOI: 10.1016/j.bmc.2005.11.005

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  13 in total

Review 1.  Phosphotyrosine isosteres: past, present and future.

Authors:  Robert A Cerulli; Joshua A Kritzer
Journal:  Org Biomol Chem       Date:  2019-11-28       Impact factor: 3.876

2.  Synthesis, electrochemical, and optical properties of new fluorescent, substituted thieno[3,2-b][1]benzothiophenes.

Authors:  Cheikh Lô; Jean-Jacques Aaron; Václav Kozmík; Jirí Svoboda; Jean-Claude Brochon; Li Na
Journal:  J Fluoresc       Date:  2010-04-13       Impact factor: 2.217

3.  Ligand-Binding-Site Refinement to Generate Reliable Holo Protein Structure Conformations from Apo Structures.

Authors:  Hugo Guterres; Sang-Jun Park; Wei Jiang; Wonpil Im
Journal:  J Chem Inf Model       Date:  2020-12-18       Impact factor: 4.956

4.  Impaired acid catalysis by mutation of a protein loop hinge residue in a YopH mutant revealed by crystal structures.

Authors:  Tiago A S Brandão; Howard Robinson; Sean J Johnson; Alvan C Hengge
Journal:  J Am Chem Soc       Date:  2009-01-21       Impact factor: 15.419

5.  Knowledge-based characterization of similarity relationships in the human protein-tyrosine phosphatase family for rational inhibitor design.

Authors:  Dusica Vidović; Stephan C Schürer
Journal:  J Med Chem       Date:  2009-11-12       Impact factor: 7.446

6.  Substrate-based fragment identification for the development of selective, nonpeptidic inhibitors of striatal-enriched protein tyrosine phosphatase.

Authors:  Tyler D Baguley; Hai-Chao Xu; Manavi Chatterjee; Angus C Nairn; Paul J Lombroso; Jonathan A Ellman
Journal:  J Med Chem       Date:  2013-10-01       Impact factor: 7.446

7.  Analysis of structural water and CH···π interactions in HIV-1 protease and PTP1B complexes using a hydrogen bond prediction tool, HBPredicT.

Authors:  Joshy P Yesudas; Fareed Bhasha Sayyed; Cherumuttathu H Suresh
Journal:  J Mol Model       Date:  2010-05-19       Impact factor: 1.810

8.  Computational Insight into Protein Tyrosine Phosphatase 1B Inhibition: A Case Study of the Combined Ligand- and Structure-Based Approach.

Authors:  Xiangyu Zhang; Hailun Jiang; Wei Li; Jian Wang; Maosheng Cheng
Journal:  Comput Math Methods Med       Date:  2017-12-26       Impact factor: 2.238

Review 9.  Thiazolidinediones: An In-Depth Study of Their Synthesis and Application to Medicinal Chemistry in the Treatment of Diabetes Mellitus.

Authors:  Nathan Long; Adam Le Gresley; Stephen P Wren
Journal:  ChemMedChem       Date:  2021-05-04       Impact factor: 3.466

10.  QSAR Study on a Series of Protein Tyrosine Phosphatase 1B Inhibitors.

Authors:  Rajendra S Mehta; Hetal R Prajapati; Dinesh V Thakkar; Pathik S Brahmkshatriya
Journal:  Int J Biomed Sci       Date:  2008-12
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