Literature DB >> 18434147

Discovery of a novel submicromolar inhibitor of the lymphoid specific tyrosine phosphatase.

Yuli Xie1, Yidong Liu, Gangli Gong, Alison Rinderspacher, Shi-Xian Deng, Deborah H Smith, Udo Toebben, Effie Tzilianos, Lars Branden, Dusica Vidović, Caty Chung, Stephan Schürer, Lutz Tautz, Donald W Landry.   

Abstract

We report here a class of thiazolidine-2,4-diones and 2-thioxothiazolidin-4-ones as potent inhibitors of the lymphoid specific tyrosine phosphatase (Lyp) identified from high throughput screens. Chemical modification by incorporating the known phosphotyrosine (pTyr) mimics led to the discovery of a salicylate-based inhibitor with submicromolar potency.

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Year:  2008        PMID: 18434147      PMCID: PMC2701911          DOI: 10.1016/j.bmcl.2008.03.079

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


  5 in total

Review 1.  A decade of fragment-based drug design: strategic advances and lessons learned.

Authors:  Philip J Hajduk; Jonathan Greer
Journal:  Nat Rev Drug Discov       Date:  2007-02-09       Impact factor: 84.694

2.  A functional variant of lymphoid tyrosine phosphatase is associated with type I diabetes.

Authors:  Nunzio Bottini; Lucia Musumeci; Andres Alonso; Souad Rahmouni; Konstantina Nika; Masoud Rostamkhani; James MacMurray; Gian Franco Meloni; Paola Lucarelli; Maurizio Pellecchia; George S Eisenbarth; David Comings; Tomas Mustelin
Journal:  Nat Genet       Date:  2004-03-07       Impact factor: 38.330

Review 3.  Phosphotyrosyl mimetics in the development of signal transduction inhibitors.

Authors:  Terrence R Burke; Kyeong Lee
Journal:  Acc Chem Res       Date:  2003-06       Impact factor: 22.384

4.  Structure, inhibitor, and regulatory mechanism of Lyp, a lymphoid-specific tyrosine phosphatase implicated in autoimmune diseases.

Authors:  Xiao Yu; Jin-Peng Sun; Yantao He; Xiaoling Guo; Sijiu Liu; Bo Zhou; Andy Hudmon; Zhong-Yin Zhang
Journal:  Proc Natl Acad Sci U S A       Date:  2007-12-03       Impact factor: 11.205

5.  Autoimmune-associated lymphoid tyrosine phosphatase is a gain-of-function variant.

Authors:  Torkel Vang; Mauro Congia; Maria Doloretta Macis; Lucia Musumeci; Valeria Orrú; Patrizia Zavattari; Konstantina Nika; Lutz Tautz; Kjetil Taskén; Francesco Cucca; Tomas Mustelin; Nunzio Bottini
Journal:  Nat Genet       Date:  2005-11-06       Impact factor: 38.330

  5 in total
  17 in total

1.  Substrate selection influences molecular recognition in a screen for lymphoid tyrosine phosphatase inhibitors.

Authors:  Rhushikesh A Kulkarni; Nadeem A Vellore; Matthew R Bliss; Stephanie M Stanford; Matthew D Falk; Nunzio Bottini; Riccardo Baron; Amy M Barrios
Journal:  Chembiochem       Date:  2013-08-16       Impact factor: 3.164

2.  Role of the C1858T polymorphism of protein tyrosine phosphatase non-receptor type 22 (PTPN22) in children and adolescents with type 1 diabetes.

Authors:  A Blasetti; C Di Giulio; S Tumini; M Provenzano; D Rapino; L Comegna; G Prezioso; R Chiuri; S Franchini; F Chiarelli; L Stuppia
Journal:  Pharmacogenomics J       Date:  2016-02-23       Impact factor: 3.550

3.  Covalent inhibition of the lymphoid tyrosine phosphatase.

Authors:  Vanessa F Ahmed; Nunzio Bottini; Amy M Barrios
Journal:  ChemMedChem       Date:  2014-01-08       Impact factor: 3.466

Review 4.  Lymphoid tyrosine phosphatase and autoimmunity: human genetics rediscovers tyrosine phosphatases.

Authors:  Stephanie M Stanford; Tomas M Mustelin; Nunzio Bottini
Journal:  Semin Immunopathol       Date:  2010-03-04       Impact factor: 9.623

5.  Target-specific control of lymphoid-specific protein tyrosine phosphatase (Lyp) activity.

Authors:  Zandra E Walton; Anthony C Bishop
Journal:  Bioorg Med Chem       Date:  2010-06-12       Impact factor: 3.641

6.  Discovery of a novel series of inhibitors of lymphoid tyrosine phosphatase with activity in human T cells.

Authors:  Stephanie M Stanford; Divya Krishnamurthy; Matthew D Falk; Rossella Messina; Bikash Debnath; Sheng Li; Tong Liu; Roza Kazemi; Russell Dahl; Yantao He; Xiao Yu; Andrew C Chan; Zhong-Yin Zhang; Amy M Barrios; Virgil L Woods; Nouri Neamati; Nunzio Bottini
Journal:  J Med Chem       Date:  2011-02-22       Impact factor: 7.446

7.  Association of PTPN22 gene (rs2488457) polymorphism with ulcerative colitis and high levels of PTPN22 mRNA in ulcerative colitis.

Authors:  Zhitao Chen; Heng Zhang; Bing Xia; Ping Wang; Ting Jiang; Min Song; Jie Wu
Journal:  Int J Colorectal Dis       Date:  2013-03-03       Impact factor: 2.571

8.  A potent and selective small-molecule inhibitor for the lymphoid-specific tyrosine phosphatase (LYP), a target associated with autoimmune diseases.

Authors:  Yantao He; Sijiu Liu; Ambili Menon; Stephanie Stanford; Emmanuel Oppong; Andrea M Gunawan; Li Wu; Dennis J Wu; Amy M Barrios; Nunzio Bottini; Andrew C B Cato; Zhong-Yin Zhang
Journal:  J Med Chem       Date:  2013-06-06       Impact factor: 7.446

9.  Identifying potent, selective protein tyrosine phosphatase inhibitors from a library of Au(I) complexes.

Authors:  Mark R Karver; Divya Krishnamurthy; Rhushikesh A Kulkarni; Nunzio Bottini; Amy M Barrios
Journal:  J Med Chem       Date:  2009-11-12       Impact factor: 7.446

10.  Inhibition of the lymphoid tyrosine phosphatase: the effect of zinc(II) ions and chelating ligand fragments on enzymatic activity.

Authors:  Megan K Thorson; David T Puerta; Seth M Cohen; Amy M Barrios
Journal:  Bioorg Med Chem Lett       Date:  2014-06-16       Impact factor: 2.823

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