Literature DB >> 12372498

alpha-bromoacetophenone derivatives as neutral protein tyrosine phosphatase inhibitors: structure-Activity relationship.

Gulnur Arabaci1, Tian Yi, Hua Fu, Mary E Porter, Kirk D Beebe, Dehua Pei.   

Abstract

A series of alpha-haloacetophenone derivatives was tested for inhibition of protein tyrosine phosphatases SHP-1 and PTP1B. The results show that the bromides are much more potent than the corresponding chlorides, whereas the phenyl ring is remarkably tolerant to modifications. Derivatization of the phenyl ring with a tripeptide Gly-Glu-Glu resulted in a potent, selective inhibitor against PTP1B.

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Year:  2002        PMID: 12372498     DOI: 10.1016/s0960-894x(02)00681-9

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  5 in total

1.  Cannabinoid CB1 receptors transactivate multiple receptor tyrosine kinases and regulate serine/threonine kinases to activate ERK in neuronal cells.

Authors:  George D Dalton; Allyn C Howlett
Journal:  Br J Pharmacol       Date:  2012-04       Impact factor: 8.739

Review 2.  Covalent inhibition of protein tyrosine phosphatases.

Authors:  Kasi Viswanatharaju Ruddraraju; Zhong-Yin Zhang
Journal:  Mol Biosyst       Date:  2017-06-27

3.  Endoplasmic reticulum stress causes insulin resistance by inhibiting delivery of newly synthesized insulin receptors to the cell surface.

Authors:  Max Brown; Samantha Dainty; Natalie Strudwick; Adina D Mihai; Jamie N Watson; Robina Dendooven; Adrienne W Paton; James C Paton; Martin Schröder
Journal:  Mol Biol Cell       Date:  2020-09-02       Impact factor: 4.138

4.  Proteome-Wide Profiling of the Covalent-Druggable Cysteines with a Structure-Based Deep Graph Learning Network.

Authors:  Hongyan Du; Dejun Jiang; Junbo Gao; Xujun Zhang; Lingxiao Jiang; Yundian Zeng; Zhenxing Wu; Chao Shen; Lei Xu; Dongsheng Cao; Tingjun Hou; Peichen Pan
Journal:  Research (Wash D C)       Date:  2022-07-21

Review 5.  Revisiting the roles of VHR/DUSP3 phosphatase in human diseases.

Authors:  Lilian Cristina Russo; Jéssica Oliveira Farias; Pault Yeison Minaya Ferruzo; Lucas Falcão Monteiro; Fábio Luís Forti
Journal:  Clinics (Sao Paulo)       Date:  2018-09-06       Impact factor: 2.365

  5 in total

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