Literature DB >> 19799530

ATP non-competitive Ser/Thr kinase inhibitors as potential anticancer agents.

Giorgio Cozza1, Andrea Bortolato, Ernesto Menta, Ennio Cavalletti, Silvano Spinelli, Stefano Moro.   

Abstract

Protein kinases are one of the largest known families of enzyme characterized by having a well conserved ATP binding pocket. Most of the synthetic kinase inhibitors are ATP-competitive, but display some potential problems, like selectivity, discrepancy between the in vitro and in vivo inhibition assays and an high risk of developing mutation inside the ATP-binding pocket. Recently some new inhibitors with a non-competitive mechanism of action were reported, with interesting results both in vitro and in vivo.

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Year:  2009        PMID: 19799530     DOI: 10.2174/187152009789056930

Source DB:  PubMed          Journal:  Anticancer Agents Med Chem        ISSN: 1871-5206            Impact factor:   2.505


  3 in total

1.  Suppression of cytokine signaling by SOCS3: characterization of the mode of inhibition and the basis of its specificity.

Authors:  Jeffrey J Babon; Nadia J Kershaw; James M Murphy; Leila N Varghese; Artem Laktyushin; Samuel N Young; Isabelle S Lucet; Raymond S Norton; Nicos A Nicola
Journal:  Immunity       Date:  2012-02-24       Impact factor: 31.745

Review 2.  Targeting protein phosphatase PP2A for cancer therapy: development of allosteric pharmaceutical agents.

Authors:  David L Brautigan; Caroline Farrington; Goutham Narla
Journal:  Clin Sci (Lond)       Date:  2021-07-16       Impact factor: 6.876

3.  Substituted 3-benzylcoumarins as allosteric MEK1 inhibitors: design, synthesis and biological evaluation as antiviral agents.

Authors:  Chao Wang; Hao Zhang; Fengrong Xu; Yan Niu; Yun Wu; Xin Wang; Yihong Peng; Jing Sun; Lei Liang; Ping Xu
Journal:  Molecules       Date:  2013-05-21       Impact factor: 4.411

  3 in total

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