Literature DB >> 27539118

Allosteric Modulation of Phosphatase Activity May Redefine Therapeutic Value.

Joseph M Salamoun1, Peter Wipf1.   

Abstract

Despite their extensive involvement in signaling pathways and disease pathologies, targeting protein phosphatases remains an underexplored opportunity in drug discovery. Selective intracellular regulation of phosphatases with small molecule inhibitors has been an unmet challenge. However, recent progress in the development of allosteric modulators encourages renewed efforts to exploit their potential as therapeutic targets.

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Year:  2016        PMID: 27539118     DOI: 10.1021/acs.jmedchem.6b01210

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  3 in total

1.  Selective inhibition of leukemia-associated SHP2E69K mutant by the allosteric SHP2 inhibitor SHP099.

Authors:  X Sun; Y Ren; S Gunawan; P Teng; Z Chen; H R Lawrence; J Cai; N J Lawrence; J Wu
Journal:  Leukemia       Date:  2018-01-30       Impact factor: 11.528

2.  A screen of FDA-approved drugs identifies inhibitors of protein tyrosine phosphatase 4A3 (PTP4A3 or PRL-3).

Authors:  Dylan R Rivas; Mark Vincent C Dela Cerna; Caroline N Smith; Shilpa Sampathi; Blaine G Patty; Donghan Lee; Jessica S Blackburn
Journal:  Sci Rep       Date:  2021-05-13       Impact factor: 4.379

3.  A New Paradigm for KIM-PTP Drug Discovery: Identification of Allosteric Sites with Potential for Selective Inhibition Using Virtual Screening and LEI Analysis.

Authors:  James Adams; Benjamin P Thornton; Lydia Tabernero
Journal:  Int J Mol Sci       Date:  2021-11-11       Impact factor: 5.923

  3 in total

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