Literature DB >> 15664853

Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme selective inhibitors.

Craig W Lindsley1, Zhijian Zhao, 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.   

Abstract

This letter describes the development of two series of potent and selective allosteric Akt kinase inhibitors that display an unprecedented level of selectivity for either Akt1, Akt2 or both Akt1/Akt2. An iterative analog library synthesis approach quickly provided a highly selective Akt1/Akt2 inhibitor that induces apoptosis in tumor cells and inhibits Akt phosphorylation in vivo.

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Year:  2005        PMID： 15664853     DOI： 10.1016/j.bmcl.2004.11.011

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


  137 in total

1.  Discovery of novel allosteric modulators of metabotropic glutamate receptor subtype 5 reveals chemical and functional diversity and in vivo activity in rat behavioral models of anxiolytic and antipsychotic activity.

Authors:  Alice L Rodriguez; Mark D Grier; Carrie K Jones; Elizabeth J Herman; Alexander S Kane; Randy L Smith; Richard Williams; Ya Zhou; Joy E Marlo; Emily L Days; Tasha N Blatt; Satyawan Jadhav; Usha N Menon; Paige N Vinson; Jerri M Rook; Shaun R Stauffer; Colleen M Niswender; Craig W Lindsley; C David Weaver; P Jeffrey Conn
Journal:  Mol Pharmacol       Date:  2010-10-05       Impact factor: 4.436

Review 2.  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

3.  Insulin reveals Akt signaling as a novel regulator of norepinephrine transporter trafficking and norepinephrine homeostasis.

Authors:  Sabrina D Robertson; Heinrich J G Matthies; W Anthony Owens; Vidiya Sathananthan; Nicole S Bibus Christianson; J Phillip Kennedy; Craig W Lindsley; Lynette C Daws; Aurelio Galli
Journal:  J Neurosci       Date:  2010-08-25       Impact factor: 6.167

4.  Akt-dependent and isoform-specific regulation of dopamine transporter cell surface expression.

Authors:  Nicole K Speed; Heinrich J G Matthies; J Phillip Kennedy; Roxanne A Vaughan; Jonathan A Javitch; Scott J Russo; Craig W Lindsley; Kevin Niswender; Aurelio Galli
Journal:  ACS Chem Neurosci       Date:  2010-05-25       Impact factor: 4.418

5.  Pathogenesis of selective insulin resistance in isolated hepatocytes.

Authors:  Joshua R Cook; Fanny Langlet; Yoshiaki Kido; Domenico Accili
Journal:  J Biol Chem       Date:  2015-04-14       Impact factor: 5.157

6.  EGFR signals to mTOR through PKC and independently of Akt in glioma.

Authors:  Qi-Wen Fan; Christine Cheng; Zachary A Knight; Daphne Haas-Kogan; David Stokoe; C David James; Frank McCormick; Kevan M Shokat; William A Weiss
Journal:  Sci Signal       Date:  2009-01-27       Impact factor: 8.192

Review 7.  The PIK3CA gene as a mutated target for cancer therapy.

Authors:  John P Gustin; David P Cosgrove; Ben Ho Park
Journal:  Curr Cancer Drug Targets       Date:  2008-12       Impact factor: 3.428

8.  mTORC1 Inhibition Induces Resistance to Methotrexate and 6-Mercaptopurine in Ph+ and Ph-like B-ALL.

Authors:  Thanh-Trang T Vo; J Scott Lee; Duc Nguyen; Brandon Lui; William Pandori; Andrew Khaw; Sharmila Mallya; Mengrou Lu; Markus Müschen; Marina Konopleva; David A Fruman
Journal:  Mol Cancer Ther       Date:  2017-05-31       Impact factor: 6.261

9.  Neuronal ablation of p-Akt at Ser473 leads to altered 5-HT1A/2A receptor function.

Authors:  Jeremy M Veenstra-Vanderweele; Aurelio Galli; Christine Saunders; Michael Siuta; Sabrina D Robertson; Adeola R Davis; Jennifer Sauer; Heinrich J G Matthies; Paul J Gresch; David Airey; Craig W Lindsley; John A Schetz; Kevin D Niswender
Journal:  Neurochem Int       Date:  2013-09-30       Impact factor: 3.921

10.  Design and synthesis of isoform-selective phospholipase D (PLD) inhibitors. Part II. Identification of the 1,3,8-triazaspiro[4,5]decan-4-one privileged structure that engenders PLD2 selectivity.

Authors:  Robert Lavieri; Sarah A Scott; Jana A Lewis; Paige E Selvy; Michelle D Armstrong; H Alex Brown; Craig W Lindsley
Journal:  Bioorg Med Chem Lett       Date:  2009-03-06       Impact factor: 2.823
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