Literature DB >> 23726034

Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation.

Pascal Furet1, Vito Guagnano, Robin A Fairhurst, Patricia Imbach-Weese, Ian Bruce, Mark Knapp, Christine Fritsch, Francesca Blasco, Joachim Blanz, Reiner Aichholz, Jacques Hamon, Doriano Fabbro, Giorgio Caravatti.   

Abstract

Phosphatidylinositol-3-kinase α (PI3Kα) is a therapeutic target of high interest in anticancer drug research. On the basis of a binding model rationalizing the high selectivity and potency of a particular series of 2-aminothiazole compounds in inhibiting PI3Kα, a medicinal chemistry program has led to the discovery of the clinical candidate NVP-BYL719.
Copyright © 2013 Elsevier Ltd. All rights reserved.

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Year:  2013        PMID: 23726034     DOI: 10.1016/j.bmcl.2013.05.007

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


  118 in total

1.  Dual Inhibition of PI3K/Akt and mTOR by the Dietary Antioxidant, Delphinidin, Ameliorates Psoriatic Features In Vitro and in an Imiquimod-Induced Psoriasis-Like Disease in Mice.

Authors:  Jean Christopher Chamcheu; Vaqar M Adhami; Stephane Esnault; Mario Sechi; Imtiaz A Siddiqui; Kenneth A Satyshur; Deeba N Syed; Shah-Jahan M Dodwad; Maria-Ines Chaves-Rodriquez; B Jack Longley; Gary S Wood; Hasan Mukhtar
Journal:  Antioxid Redox Signal       Date:  2016-10-04       Impact factor: 8.401

2.  AXL mediates resistance to PI3Kα inhibition by activating the EGFR/PKC/mTOR axis in head and neck and esophageal squamous cell carcinomas.

Authors:  Moshe Elkabets; Evangelos Pazarentzos; Dejan Juric; Qing Sheng; Raphael A Pelossof; Samuel Brook; Ana Oaknin Benzaken; Jordi Rodon; Natasha Morse; Jenny Jiacheng Yan; Manway Liu; Rita Das; Yan Chen; Angela Tam; Huiqin Wang; Jinsheng Liang; Joseph M Gurski; Darcy A Kerr; Rafael Rosell; Cristina Teixidó; Alan Huang; Ronald A Ghossein; Neal Rosen; Trever G Bivona; Maurizio Scaltriti; José Baselga
Journal:  Cancer Cell       Date:  2015-04-13       Impact factor: 31.743

3.  PI3K isoform-selective inhibition in neuron-specific PTEN-deficient mice rescues molecular defects and reduces epilepsy-associated phenotypes.

Authors:  Angela R White; Durgesh Tiwari; Molly C MacLeod; Steve C Danzer; Christina Gross
Journal:  Neurobiol Dis       Date:  2020-07-24       Impact factor: 5.996

4.  Characterization of a novel p110β-specific inhibitor BL140 that overcomes MDV3100-resistance in castration-resistant prostate cancer cells.

Authors:  Chenchen He; Shaofeng Duan; Liang Dong; Yifen Wang; Qingting Hu; Chunjing Liu; Marcus L Forrest; Jeffrey M Holzbeierlein; Suxia Han; Benyi Li
Journal:  Prostate       Date:  2017-06-20       Impact factor: 4.104

5.  Therapeutic targeting of cancers with loss of PTEN function.

Authors:  Lloye M Dillon; Todd W Miller
Journal:  Curr Drug Targets       Date:  2014-01       Impact factor: 3.465

6.  Addition of the p110α inhibitor BYL719 overcomes targeted therapy resistance in cells from Her2-positive-PTEN-loss breast cancer.

Authors:  Chen Zhang; Bingfei Xu; Pian Liu
Journal:  Tumour Biol       Date:  2016-09-17

7.  INPP4B and PTEN Loss Leads to PI-3,4-P2 Accumulation and Inhibition of PI3K in TNBC.

Authors:  Darien E Reed; Kevan M Shokat
Journal:  Mol Cancer Res       Date:  2017-02-14       Impact factor: 5.852

8.  Prediction of Tissue-to-Plasma Ratios of Basic Compounds in Mice.

Authors:  Prashant B Nigade; Jayasagar Gundu; K Sreedhara Pai; Kumar V S Nemmani
Journal:  Eur J Drug Metab Pharmacokinet       Date:  2017-10       Impact factor: 2.441

9.  Hematopoiesis and RAS-driven myeloid leukemia differentially require PI3K isoform p110α.

Authors:  Kira Gritsman; Haluk Yuzugullu; Thanh Von; Howard Yan; Linda Clayton; Christine Fritsch; Sauveur-Michel Maira; Gregory Hollingworth; Christine Choi; Tulasi Khandan; Mahnaz Paktinat; Rachel O Okabe; Thomas M Roberts; Jean J Zhao
Journal:  J Clin Invest       Date:  2014-02-24       Impact factor: 14.808

10.  A PI3K p110α-selective inhibitor enhances the efficacy of anti-HER2/neu antibody therapy against breast cancer in mice.

Authors:  Jae-Hyeog Choi; Ki Hyang Kim; Kug-Hwan Roh; Hana Jung; Anbok Lee; Ji-Young Lee; Joo Yeon Song; Seung Jae Park; Ilhwan Kim; Won-Sik Lee; Su-Kil Seo; Il-Whan Choi; Yang-Xin Fu; Sung Su Yea; SaeGwang Park
Journal:  Oncoimmunology       Date:  2018-01-16       Impact factor: 8.110

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