Literature DB >> 20731359

A focused library of protein tyrosine phosphatase inhibitors.

Anthony B Comeau1, David A Critton, Rebecca Page, Christopher T Seto.   

Abstract

Protein tyrosine phosphatases such as PTP1B and YopH are potential targets for the development of therapeutic agents against a variety of pathological conditions including diabetes, obesity, and infection by the bacterium Yersinia pestis. A focused library of bidentate α-ketoacid-based inhibitors has been screened against several tyrosine phosphatases. Compound 2a has IC(50) values of 43 and 220 nM against YopH and PTP1B, respectively, and shows a 30-fold selectivity for PTP1B over the closely related phosphatase TCPTP.

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Year:  2010        PMID： 20731359     DOI： 10.1021/jm100528p

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


  6 in total

1.  Utilization of nitrophenylphosphates and oxime-based ligation for the development of nanomolar affinity inhibitors of the Yersinia pestis outer protein H (YopH) phosphatase.

Authors:  Medhanit Bahta; George T Lountos; Beverly Dyas; Sung-Eun Kim; Robert G Ulrich; David S Waugh; Terrence R Burke
Journal:  J Med Chem       Date:  2011-03-28       Impact factor: 7.446

2.  Inhibitors of the Yersinia protein tyrosine phosphatase through high throughput and virtual screening approaches.

Authors:  Xin Hu; Milos Vujanac; Noel Southall; C Erec Stebbins
Journal:  Bioorg Med Chem Lett       Date:  2012-12-20       Impact factor: 2.823

3.  A HaloTag-based small molecule microarray screening methodology with increased sensitivity and multiplex capabilities.

Authors:  Devin J Noblin; Charlotte M Page; Hyun Seop Tae; Peter C Gareiss; John S Schneekloth; Craig M Crews
Journal:  ACS Chem Biol       Date:  2012-10-11       Impact factor: 5.100

4.  Biotinylated phosphoproteins from kinase-catalyzed biotinylation are stable to phosphatases: implications for phosphoproteomics.

Authors:  Chamara Senevirathne; Mary Kay H Pflum
Journal:  Chembiochem       Date:  2013-01-17       Impact factor: 3.164

5.  Effects of a natural PTP1B inhibitor from Rhodomela confervoides on the amelioration of fatty acid-induced insulin resistance in hepatocytes and hyperglycaemia in STZ-induced diabetic rats.

Authors:  Shuju Guo; Lijun Wang; Dong Chen; Bo Jiang
Journal:  RSC Adv       Date:  2020-01-21       Impact factor: 4.036

Review 6.  Terminal Phenoxy Group as a Privileged Moiety of the Drug Scaffold-A Short Review of Most Recent Studies 2013-2022.

Authors:  Paweł Kozyra; Monika Pitucha
Journal:  Int J Mol Sci       Date:  2022-08-09       Impact factor: 6.208
  6 in total

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