Literature DB >> 15686884

Discovery of 2,3,5-trisubstituted pyridine derivatives as potent Akt1 and Akt2 dual inhibitors.

Zhijian Zhao1, William H Leister, Ronald G Robinson, Stanley F Barnett, Deborah Defeo-Jones, Raymond E Jones, George D Hartman, Joel R Huff, Hans E Huber, Mark E Duggan, Craig W Lindsley.   

Abstract

This letter describes the discovery of a novel series of dual Akt1/Akt2 kinase inhibitors, based on a 2,3,5-trisubstituted pyridine scaffold. Compounds from this series, which contain a 5-tetrazolyl moiety, exhibit more potent inhibition of Akt2 than Akt1.

Entities:  

Mesh：

Substances：

Year:  2005        PMID： 15686884     DOI： 10.1016/j.bmcl.2004.12.062

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


  42 in total

Review 1.  Inhibition of Akt with small molecules and biologics: historical perspective and current status of the patent landscape.

Authors:  Margrith E Mattmann; Sydney L Stoops; Craig W Lindsley
Journal:  Expert Opin Ther Pat       Date:  2011-06-02       Impact factor: 6.674

2.  CARMA1 is required for Akt-mediated NF-kappaB activation in T cells.

Authors:  Preeti Narayan; Brittany Holt; Richard Tosti; Lawrence P Kane
Journal:  Mol Cell Biol       Date:  2006-03       Impact factor: 4.272

3.  3-D structure and dynamics of protein kinase B-new mechanism for the allosteric regulation of an AGC kinase.

Authors:  Véronique Calleja; Michel Laguerre; Banafshé Larijani
Journal:  J Chem Biol       Date:  2009-02-20

4.  Inhibition of Akt signaling in hepatoma cells induces apoptotic cell death independent of Akt activation status.

Authors:  Francesca Buontempo; Tulin Ersahin; Silvia Missiroli; Serif Senturk; Daniela Etro; Mehmet Ozturk; Silvano Capitani; Rengul Cetin-Atalay; Maria Luca Neri
Journal:  Invest New Drugs       Date:  2010-07-14       Impact factor: 3.850

5.  Label-free detection of G protein-SNARE interactions and screening for small molecule modulators.

Authors:  Christopher A Wells; Katherine M Betke; Craig W Lindsley; Heidi E Hamm
Journal:  ACS Chem Neurosci       Date:  2012-01-18       Impact factor: 4.418

6.  Transforming growth factor-β (TGF-β)-induced up-regulation of TGF-β receptors at the cell surface amplifies the TGF-β response.

Authors:  Dana Duan; Rik Derynck
Journal:  J Biol Chem       Date:  2019-04-04       Impact factor: 5.157

7.  BDNF and exercise enhance neuronal DNA repair by stimulating CREB-mediated production of apurinic/apyrimidinic endonuclease 1.

Authors:  Vilhelm A Bohr; Mark P Mattson; Jenq-Lin Yang; Yu-Ting Lin; Pei-Chin Chuang
Journal:  Neuromolecular Med       Date:  2013-10-10       Impact factor: 3.843

8.  Crystal structure of human AKT1 with an allosteric inhibitor reveals a new mode of kinase inhibition.

Authors:  Wen-I Wu; Walter C Voegtli; Hillary L Sturgis; Faith P Dizon; Guy P A Vigers; Barbara J Brandhuber
Journal:  PLoS One       Date:  2010-09-23       Impact factor: 3.240

9.  Elucidation of binding mode and three dimensional quantitative structure-activity relationship studies of a novel series of protein kinase B/Akt inhibitors.

Authors:  M Muddassar; F A Pasha; M M Neaz; Y Saleem; S J Cho
Journal:  J Mol Model       Date:  2008-11-29       Impact factor: 1.810

10.  Activation of the PI3 kinase pathway by retinoic acid mediates sodium/iodide symporter induction and iodide transport in MCF-7 breast cancer cells.

Authors:  Emi Ohashi; Takahiko Kogai; Hiroyuki Kagechika; Gregory A Brent
Journal:  Cancer Res       Date:  2009-04-07       Impact factor: 12.701
View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.