Literature DB >> 18539456

Discovery of potent and cell-active allosteric dual Akt 1 and 2 inhibitors.

Tony Siu1, Jun Liang, Jeannie Arruda, Yiwei Li, Raymond E Jones, Deborah Defeo-Jones, Stanley F Barnett, Ronald G Robinson.   

Abstract

This paper describes the improvement of cell potency in a class of allosteric Akt 1 and 2 inhibitors. Key discoveries include identifying the solvent exposed region of the molecule and appending basic amines to enhance the physiochemical properties of the molecules. Findings from the structure-activity relationships are discussed.

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Year:  2008        PMID： 18539456     DOI： 10.1016/j.bmcl.2008.05.085

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


  4 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.  A 2D-QSAR and Grid-Independent Molecular Descriptor (GRIND) Analysis of Quinoline-Type Inhibitors of Akt2: Exploration of the Binding Mode in the Pleckstrin Homology (PH) Domain.

Authors:  Noreen Akhtar; Ishrat Jabeen
Journal:  PLoS One       Date:  2016-12-30       Impact factor: 3.240

3.  Polypharmacology Within the Full Kinome: a Machine Learning Approach.

Authors:  Derek Jones; Jeevith Bopaiah; Fatemah Alghamedy; Nathan Jacobs; Heidi L Weiss; W A de Jong; Sally R Ellingson
Journal:  AMIA Jt Summits Transl Sci Proc       Date:  2018-05-18

4.  Pharmacophore modeling, virtual screening, and molecular docking studies for discovery of novel Akt2 inhibitors.

Authors:  Jia Fei; Lu Zhou; Tao Liu; Xiang-Yang Tang
Journal:  Int J Med Sci       Date:  2013-01-23       Impact factor: 3.738
  4 in total

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