Literature DB >> 23568546

A facile hydroxyindole carboxylic acid based focused library approach for potent and selective inhibitors of Mycobacterium protein tyrosine phosphatase B.

Li-Fan Zeng1, Jie Xu, Yantao He, Rongjun He, Li Wu, Andrea M Gunawan, Zhong-Yin Zhang.   

Abstract

Focused on Mtb: A facile hydroxyindole carboxylic acid based focused amide library was designed to target both the PTP active site and a unique nearby pocket for enhanced affinity and selectivity. HTS of the library led to the identification of a highly potent and selective inhibitor, 11 a, of mPTPB, an essential virulence factor for Mycobacterium tuberculosis. Compound 11 a shows high cellular activity and is capable of reversing the altered immune responses induced by mPTPB in macrophages.
Copyright © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

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Year:  2013        PMID： 23568546      PMCID： PMC3755370          DOI： 10.1002/cmdc.201300115

Source DB:  PubMed          Journal:  ChemMedChem        ISSN： 1860-7179            Impact factor:   3.466


  24 in total

Review 1.  Protein tyrosine phosphatases: structure and function, substrate specificity, and inhibitor development.

Authors:  Zhong-Yin Zhang
Journal:  Annu Rev Pharmacol Toxicol       Date:  2002       Impact factor: 13.820

Review 2.  Protein tyrosine phosphatases: prospects for therapeutics.

Authors:  Z Y Zhang
Journal:  Curr Opin Chem Biol       Date:  2001-08       Impact factor: 8.822

3.  Fragment-based substrate activity screening method for the identification of potent inhibitors of the Mycobacterium tuberculosis phosphatase PtpB.

Authors:  Matthew B Soellner; Katherine A Rawls; Christoph Grundner; Tom Alber; Jonathan A Ellman
Journal:  J Am Chem Soc       Date:  2007-07-18       Impact factor: 15.419

4.  High-throughput discovery of Mycobacterium tuberculosis protein tyrosine phosphatase B (MptpB) inhibitors using click chemistry.

Authors:  Lay Pheng Tan; Hao Wu; Peng-Yu Yang; Karunakaran A Kalesh; Xiaohua Zhang; Mingyu Hu; Rajavel Srinivasan; Shao Q Yao
Journal:  Org Lett       Date:  2009-11-19       Impact factor: 6.005

5.  Structure-based discovery of small molecule inhibitors targeted to protein tyrosine phosphatase 1B.

Authors:  M Sarmiento; L Wu; Y F Keng; L Song; Z Luo; Z Huang; G Z Wu; A K Yuan; Z Y Zhang
Journal:  J Med Chem       Date:  2000-01-27       Impact factor: 7.446

6.  Identification of a second aryl phosphate-binding site in protein-tyrosine phosphatase 1B: a paradigm for inhibitor design.

Authors:  Y A Puius; Y Zhao; M Sullivan; D S Lawrence; S C Almo; Z Y Zhang
Journal:  Proc Natl Acad Sci U S A       Date:  1997-12-09       Impact factor: 11.205

Review 7.  Protein-tyrosine phosphatases and cancer.

Authors:  Arne Ostman; Carina Hellberg; Frank D Böhmer
Journal:  Nat Rev Cancer       Date:  2006-04       Impact factor: 60.716

8.  Deciphering the biology of Mycobacterium tuberculosis from the complete genome sequence.

Authors:  S T Cole; R Brosch; J Parkhill; T Garnier; C Churcher; D Harris; S V Gordon; K Eiglmeier; S Gas; C E Barry; F Tekaia; K Badcock; D Basham; D Brown; T Chillingworth; R Connor; R Davies; K Devlin; T Feltwell; S Gentles; N Hamlin; S Holroyd; T Hornsby; K Jagels; A Krogh; J McLean; S Moule; L Murphy; K Oliver; J Osborne; M A Quail; M A Rajandream; J Rogers; S Rutter; K Seeger; J Skelton; R Squares; S Squares; J E Sulston; K Taylor; S Whitehead; B G Barrell
Journal:  Nature       Date:  1998-06-11       Impact factor: 49.962

9.  Inhibition of MptpB phosphatase from Mycobacterium tuberculosis impairs mycobacterial survival in macrophages.

Authors:  Nicola J Beresford; Debbie Mulhearn; Bruce Szczepankiewicz; Gang Liu; Michael E Johnson; Anthony Fordham-Skelton; Cele Abad-Zapatero; Jennifer S Cavet; Lydia Tabernero
Journal:  J Antimicrob Chemother       Date:  2009-02-24       Impact factor: 5.790

10.  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
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  8 in total

1.  Mycobacterial Protein Tyrosine Phosphatases A and B Inhibitors Augment the Bactericidal Activity of the Standard Anti-tuberculosis Regimen.

Authors:  Noton K Dutta; Rongjun He; Michael L Pinn; Yantao He; Francis Burrows; Zhong-Yin Zhang; Petros C Karakousis
Journal:  ACS Infect Dis       Date:  2015-12-24       Impact factor: 5.084

2.  Cefsulodin Inspired Potent and Selective Inhibitors of mPTPB, a Virulent Phosphatase from Mycobacterium tuberculosis.

Authors:  Rongjun He; Zhi-Hong Yu; Ruo-Yu Zhang; Li Wu; Andrea M Gunawan; Zhong-Yin Zhang
Journal:  ACS Med Chem Lett       Date:  2015-11-03       Impact factor: 4.345

3.  Diversity-Oriented Synthesis for Novel, Selective and Drug-like Inhibitors for a Phosphatase from Mycobacterium Tuberculosis.

Authors:  Rongjun He; Yunpeng Bai; Zhi-Hong Yu; Li Wu; Andrea Michelle Gunawan; Zhong-Yin Zhang
Journal:  Medchemcomm       Date:  2014-10       Impact factor: 3.597

4.  Hydroxyindole carboxylic acid-based inhibitors for receptor-type protein tyrosine protein phosphatase beta.

Authors:  Li-Fan Zeng; Ruo-Yu Zhang; Yunpeng Bai; Li Wu; Andrea M Gunawan; Zhong-Yin Zhang
Journal:  Antioxid Redox Signal       Date:  2014-02-04       Impact factor: 8.401

5.  Highly Potent and Selective N-Aryl Oxamic Acid-Based Inhibitors for Mycobacterium tuberculosis Protein Tyrosine Phosphatase B.

Authors:  Kasi Viswanatharaju Ruddraraju; Devesh Aggarwal; Congwei Niu; Erica Anne Baker; Ruo-Yu Zhang; Li Wu; Zhong-Yin Zhang
Journal:  J Med Chem       Date:  2020-08-21       Impact factor: 7.446

6.  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

7.  Therapeutic potential of targeting the oncogenic SHP2 phosphatase.

Authors:  Li-Fan Zeng; Ruo-Yu Zhang; Zhi-Hong Yu; Sijiu Li; Li Wu; Andrea M Gunawan; Brandon S Lane; Raghuveer S Mali; Xingjun Li; Rebecca J Chan; Reuben Kapur; Clark D Wells; Zhong-Yin Zhang
Journal:  J Med Chem       Date:  2014-07-28       Impact factor: 7.446

8.  Druggability analysis and classification of protein tyrosine phosphatase active sites.

Authors:  Mohammad A Ghattas; Noor Raslan; Asil Sadeq; Mohammad Al Sorkhy; Noor Atatreh
Journal:  Drug Des Devel Ther       Date:  2016-09-30       Impact factor: 4.162
  8 in total

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