Literature DB >> 26819669

Potent, Selective, and Orally Bioavailable Inhibitors of VPS34 Provide Chemical Tools to Modulate Autophagy in Vivo.

Ayako Honda1, Edmund Harrington1, Ivan Cornella-Taracido1, Pascal Furet2, Mark S Knapp3, Meir Glick1, Ellen Triantafellow1, William E Dowdle1, Dmitri Wiedershain1, Wieslawa Maniara1, Christine Moore1, Peter M Finan1, Lawrence G Hamann1, Brant Firestone1, Leon O Murphy1, Erin P Keaney1.   

Abstract

Autophagy is a dynamic process that regulates lysosomal-dependent degradation of cellular components. Until recently the study of autophagy has been hampered by the lack of reliable pharmacological tools, but selective inhibitors are now available to modulate the PI 3-kinase VPS34, which is required for autophagy. Here we describe the discovery of potent and selective VPS34 inhibitors, their pharmacokinetic (PK) properties, and ability to inhibit autophagy in cellular and mouse models.

Entities:  

Keywords:  VPS34; autophagy; phosphoinositide 3-kinase

Year:  2015        PMID： 26819669      PMCID： PMC4716600          DOI： 10.1021/acsmedchemlett.5b00335

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  13 in total

1.  WHAT IF: a molecular modeling and drug design program.

Authors:  G Vriend
Journal:  J Mol Graph       Date:  1990-03

2.  Mammalian Atg18 (WIPI2) localizes to omegasome-anchored phagophores and positively regulates LC3 lipidation.

Authors:  Hannah E J Polson; Jane de Lartigue; Daniel J Rigden; Marco Reedijk; Sylvie Urbé; Michael J Clague; Sharon A Tooze
Journal:  Autophagy       Date:  2010-05-16       Impact factor: 16.016

3.  Shaping development of autophagy inhibitors with the structure of the lipid kinase Vps34.

Authors:  Simon Miller; Brandon Tavshanjian; Arkadiusz Oleksy; Olga Perisic; Benjamin T Houseman; Kevan M Shokat; Roger L Williams
Journal:  Science       Date:  2010-03-26       Impact factor: 47.728

Review 4.  To be or not to be? How selective autophagy and cell death govern cell fate.

Authors:  Douglas R Green; Beth Levine
Journal:  Cell       Date:  2014-03-27       Impact factor: 41.582

Review 5.  PI3K and cancer: lessons, challenges and opportunities.

Authors:  David A Fruman; Christian Rommel
Journal:  Nat Rev Drug Discov       Date:  2014-02       Impact factor: 84.694

6.  Selective VPS34 inhibitor blocks autophagy and uncovers a role for NCOA4 in ferritin degradation and iron homeostasis in vivo.

Authors:  William E Dowdle; Beat Nyfeler; Jane Nagel; Robert A Elling; Shanming Liu; Ellen Triantafellow; Suchithra Menon; Zuncai Wang; Ayako Honda; Gwynn Pardee; John Cantwell; Catherine Luu; Ivan Cornella-Taracido; Edmund Harrington; Peter Fekkes; Hong Lei; Qing Fang; Mary Ellen Digan; Debra Burdick; Andrew F Powers; Stephen B Helliwell; Simon D'Aquin; Julie Bastien; Henry Wang; Dmitri Wiederschain; Jenny Kuerth; Philip Bergman; David Schwalb; Jason Thomas; Savuth Ugwonali; Fred Harbinski; John Tallarico; Christopher J Wilson; Vic E Myer; Jeffery A Porter; Dirksen E Bussiere; Peter M Finan; Mark A Labow; Xiaohong Mao; Lawrence G Hamann; Brendan D Manning; Reginald A Valdez; Thomas Nicholson; Markus Schirle; Mark S Knapp; Erin P Keaney; Leon O Murphy
Journal:  Nat Cell Biol       Date:  2014-10-19       Impact factor: 28.824

7.  Dual role of 3-methyladenine in modulation of autophagy via different temporal patterns of inhibition on class I and III phosphoinositide 3-kinase.

Authors:  You-Tong Wu; Hui-Ling Tan; Guanghou Shui; Chantal Bauvy; Qing Huang; Markus R Wenk; Choon-Nam Ong; Patrice Codogno; Han-Ming Shen
Journal:  J Biol Chem       Date:  2010-02-01       Impact factor: 5.157

Review 8.  Class IA phosphatidylinositol 3-kinase: from their biologic implication in human cancers to drug discovery.

Authors:  Sauveur-Michel Maira; Charles Voliva; Carlos Garcia-Echeverria
Journal:  Expert Opin Ther Targets       Date:  2008-02       Impact factor: 6.902

9.  Autophagy requires endoplasmic reticulum targeting of the PI3-kinase complex via Atg14L.

Authors:  Kohichi Matsunaga; Eiji Morita; Tatsuya Saitoh; Shizuo Akira; Nicholas T Ktistakis; Tetsuro Izumi; Takeshi Noda; Tamotsu Yoshimori
Journal:  J Cell Biol       Date:  2010-08-16       Impact factor: 10.539

Review 10.  Emerging regulation and functions of autophagy.

Authors:  Patricia Boya; Fulvio Reggiori; Patrice Codogno
Journal:  Nat Cell Biol       Date:  2013-07       Impact factor: 28.824
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  15 in total

1.  Targeting the Autophagy Specific Lipid Kinase VPS34 for Cancer Treatment: An Integrative Repurposing Strategy.

Authors:  Poornimaa Murali; Kanika Verma; Thanyada Rungrotmongkol; Perarasu Thangavelu; Ramanathan Karuppasamy
Journal:  Protein J       Date:  2021-01-05       Impact factor: 2.371

2.  N-(1-Benzyl-3,5-dimethyl-1H-pyrazol-4-yl)benzamides: Antiproliferative Activity and Effects on mTORC1 and Autophagy.

Authors:  Teng Ai; Rose Willett; Jessica Williams; Rui Ding; Daniel J Wilson; Jiashu Xie; Do-Hyung Kim; Rosa Puertollano; Liqiang Chen
Journal:  ACS Med Chem Lett       Date:  2016-11-28       Impact factor: 4.345

Review 3.  Cell Survival and Cell Death at the Intersection of Autophagy and Apoptosis: Implications for Current and Future Cancer Therapeutics.

Authors:  Nicole Bata; Nicholas D P Cosford
Journal:  ACS Pharmacol Transl Sci       Date:  2021-11-03

Review 4.  Autophagy in Cancer: Regulation by Small Molecules.

Authors:  Allison S Limpert; Lester J Lambert; Nicole A Bakas; Nicole Bata; Sonja N Brun; Reuben J Shaw; Nicholas D P Cosford
Journal:  Trends Pharmacol Sci       Date:  2018-12       Impact factor: 14.819

5.  Endosomal Phosphatidylinositol 3-Kinase Is Essential for Canonical GPCR Signaling.

Authors:  Yasunori Uchida; Florentine U Rutaganira; Damien Jullié; Kevan M Shokat; Mark von Zastrow
Journal:  Mol Pharmacol       Date:  2016-11-07       Impact factor: 4.436

6.  PIK3C3 Inhibition Promotes Sensitivity to Colon Cancer Therapy by Inhibiting Cancer Stem Cells.

Authors:  Balawant Kumar; Rizwan Ahmad; Swagat Sharma; Saiprasad Gowrikumar; Mark Primeaux; Sandeep Rana; Amarnath Natarajan; David Oupicky; Corey R Hopkins; Punita Dhawan; Amar B Singh
Journal:  Cancers (Basel)       Date:  2021-04-30       Impact factor: 6.639

Review 7.  Autophagy and inflammation.

Authors:  Mengjia Qian; Xiaocong Fang; Xiangdong Wang
Journal:  Clin Transl Med       Date:  2017-07-26

8.  Vps34 PI 3-kinase inactivation enhances insulin sensitivity through reprogramming of mitochondrial metabolism.

Authors:  Benoit Bilanges; Samira Alliouachene; Wayne Pearce; Daniele Morelli; Gyorgy Szabadkai; Yuen-Li Chung; Gaëtan Chicanne; Colin Valet; Julia M Hill; Peter J Voshol; Lucy Collinson; Christopher Peddie; Khaled Ali; Essam Ghazaly; Vinothini Rajeeve; Georgios Trichas; Shankar Srinivas; Claire Chaussade; Rachel S Salamon; Jonathan M Backer; Cheryl L Scudamore; Maria A Whitehead; Erin P Keaney; Leon O Murphy; Robert K Semple; Bernard Payrastre; Sharon A Tooze; Bart Vanhaesebroeck
Journal:  Nat Commun       Date:  2017-11-27       Impact factor: 14.919

Review 9.  Targeting Autophagy in the Tumor Microenvironment: New Challenges and Opportunities for Regulating Tumor Immunity.

Authors:  Bassam Janji; Guy Berchem; Salem Chouaib
Journal:  Front Immunol       Date:  2018-04-25       Impact factor: 7.561

Review 10.  VPS34 complexes from a structural perspective.

Authors:  Yohei Ohashi; Shirley Tremel; Roger L Williams
Journal:  J Lipid Res       Date:  2018-11-05       Impact factor: 5.922
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