Literature DB >> 17407812

PTP1B inhibitor Ertiprotafib is also a potent inhibitor of IkappaB kinase beta (IKK-beta).

Suja Shrestha1, Bharat Raj Bhattarai, Heeyeong Cho, Joong-Kwon Choi, Hyeongjin Cho.   

Abstract

Ertiprotafib was developed as an inhibitor of PTP1B for the treatment of type 2 diabetes. It normalized the plasma glucose and insulin levels in diabetic animal models, and progressed to a phase II clinical trial. Multiple in vivo targets of Ertiprotafib, in addition to PTP1B inhibition, have been suggested. In this study, Ertiprotafib was also shown to be a potent inhibitor of IkappaB kinase beta (IKK-beta), with an IC(50) of 400nM.

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Year:  2007        PMID： 17407812     DOI： 10.1016/j.bmcl.2007.03.001

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


  8 in total

Review 1.  Phosphotyrosine isosteres: past, present and future.

Authors:  Robert A Cerulli; Joshua A Kritzer
Journal:  Org Biomol Chem       Date:  2019-11-28       Impact factor: 3.876

Review 2.  Human Protein Tyrosine Phosphatase 1B (PTP1B): From Structure to Clinical Inhibitor Perspectives.

Authors:  Rongxing Liu; Cécile Mathieu; Jérémy Berthelet; Wenchao Zhang; Jean-Marie Dupret; Fernando Rodrigues Lima
Journal:  Int J Mol Sci       Date:  2022-06-24       Impact factor: 6.208

Review 3.  Targeting hepatic glucose metabolism in the treatment of type 2 diabetes.

Authors:  Amy K Rines; Kfir Sharabi; Clint D J Tavares; Pere Puigserver
Journal:  Nat Rev Drug Discov       Date:  2016-08-12       Impact factor: 84.694

Review 4.  Protein tyrosine phosphatases: promising targets in pancreatic ductal adenocarcinoma.

Authors:  Mariana Tannús Ruckert; Pamela Viani de Andrade; Verena Silva Santos; Vanessa Silva Silveira
Journal:  Cell Mol Life Sci       Date:  2019-04-13       Impact factor: 9.207

5.  Identification of distant drug off-targets by direct superposition of binding pocket surfaces.

Authors:  Marcel Schumann; Roger S Armen
Journal:  PLoS One       Date:  2013-12-31       Impact factor: 3.240

6.  Inhibitory Kappa B Kinase α (IKKα) Inhibitors That Recapitulate Their Selectivity in Cells against Isoform-Related Biomarkers.

Authors:  Nahoum G Anthony; Jessica Baiget; Giacomo Berretta; Marie Boyd; David Breen; Joanne Edwards; Carly Gamble; Alexander I Gray; Alan L Harvey; Sophia Hatziieremia; Ka Ho Ho; Judith K Huggan; Stuart Lang; Sabin Llona-Minguez; Jia Lin Luo; Kathryn McIntosh; Andrew Paul; Robin J Plevin; Murray N Robertson; Rebecca Scott; Colin J Suckling; Oliver B Sutcliffe; Louise C Young; Simon P Mackay
Journal:  J Med Chem       Date:  2017-08-15       Impact factor: 7.446

7.  The protein tyrosine phosphatase PTP1B is a negative regulator of CD40 and BAFF-R signaling and controls B cell autoimmunity.

Authors:  David Medgyesi; Elias Hobeika; Robert Biesen; Florian Kollert; Adriano Taddeo; Reinhard E Voll; Falk Hiepe; Michael Reth
Journal:  J Exp Med       Date:  2014-03-03       Impact factor: 14.307

8.  A novel role for protein tyrosine phosphatase 1B as a positive regulator of neuroinflammation.

Authors:  Gyun Jee Song; Myungsu Jung; Jong-Heon Kim; Hana Park; Md Habibur Rahman; Sheng Zhang; Zhong-Yin Zhang; Dong Ho Park; Hyun Kook; In-Kyu Lee; Kyoungho Suk
Journal:  J Neuroinflammation       Date:  2016-04-19       Impact factor: 8.322
  8 in total

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