Literature DB >> 21428919

Benefits of mTOR kinase targeting in oncology: pre-clinical evidence with AZD8055.

Gayle Marshall1, Zoe Howard, Jonathan Dry, Sarah Fenton, Dan Heathcote, Neil Gray, Heather Keen, Armelle Logie, Sarah Holt, Paul Smith, Sylvie M Guichard.   

Abstract

AZD8055 is a small-molecule inhibitor of mTOR (mammalian target of rapamycin) kinase activity. The present review highlights molecular and phenotypic differences between AZD8055 and allosteric inhibitors of mTOR such as rapamycin. Biomarkers, some of which are applicable to clinical studies, as well as biological effects such as autophagy, growth inhibition and cell death are compared between AZD8055 and rapamycin. Potential ways to develop rational combinations with mTOR kinase inhibitors are also discussed. Overall, AZD8055 may provide a better therapeutic strategy than rapamycin and analogues.

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Year:  2011        PMID: 21428919     DOI: 10.1042/BST0390456

Source DB:  PubMed          Journal:  Biochem Soc Trans        ISSN: 0300-5127            Impact factor:   5.407


  16 in total

Review 1.  Rapamycin passes the torch: a new generation of mTOR inhibitors.

Authors:  Don Benjamin; Marco Colombi; Christoph Moroni; Michael N Hall
Journal:  Nat Rev Drug Discov       Date:  2011-10-31       Impact factor: 84.694

2.  A low dose of AZD8055 enhances radiosensitivity of nasopharyngeal carcinoma cells by activating autophagy and apoptosis.

Authors:  Lihong Chang; Zizhen Huang; Shuaixiang Li; Zhouzhou Yao; Hongwei Bao; Zhiyuan Wang; Xia Li; Xiaohong Chen; Jiancong Huang; Gehua Zhang
Journal:  Am J Cancer Res       Date:  2019-09-01       Impact factor: 6.166

Review 3.  Mechanisms of autophagy and relevant small-molecule compounds for targeted cancer therapy.

Authors:  Jin Zhang; Guan Wang; Yuxin Zhou; Yi Chen; Liang Ouyang; Bo Liu
Journal:  Cell Mol Life Sci       Date:  2018-02-07       Impact factor: 9.261

4.  Examining changes in [18 F]FDG and [18 F]FLT uptake in U87-MG glioma xenografts as early response biomarkers to treatment with the dual mTOR1/2 inhibitor AZD8055.

Authors:  Heather G Keen; Sally-Ann Ricketts; Juliana Maynard; Armelle Logie; Rajesh Odedra; Aoife M Shannon; Stephen R Wedge; Sylvie M Guichard
Journal:  Mol Imaging Biol       Date:  2014-06       Impact factor: 3.488

Review 5.  The mTOR signaling pathway in the brain: focus on epilepsy and epileptogenesis.

Authors:  Emilio Russo; Rita Citraro; Andrew Constanti; Giovambattista De Sarro
Journal:  Mol Neurobiol       Date:  2012-07-24       Impact factor: 5.682

Review 6.  Targeting RTK-PI3K-mTOR Axis in Gliomas: An Update.

Authors:  Mayra Colardo; Marco Segatto; Sabrina Di Bartolomeo
Journal:  Int J Mol Sci       Date:  2021-05-05       Impact factor: 5.923

7.  Potent dual inhibitors of TORC1 and TORC2 complexes (KU-0063794 and KU-0068650) demonstrate in vitro and ex vivo anti-keloid scar activity.

Authors:  Farhatullah Syed; Hitesh J Sanganee; Subir Singh; Ashwani Bahl; Ardeshir Bayat
Journal:  J Invest Dermatol       Date:  2013-01-10       Impact factor: 8.551

8.  AZD8055 enhances in vivo efficacy of afatinib in chordomas.

Authors:  Tianna Zhao; I-Mei Siu; Tara Williamson; Haoyu Zhang; Chenchen Ji; Peter C Burger; Nick Connis; Jacob Ruzevick; Menghang Xia; Lucia Cottone; Adrienne M Flanagan; Christine L Hann; Gary L Gallia
Journal:  J Pathol       Date:  2021-07-28       Impact factor: 9.883

Review 9.  Ras/Raf/MEK/ERK and PI3K/PTEN/Akt/mTOR cascade inhibitors: how mutations can result in therapy resistance and how to overcome resistance.

Authors:  James A McCubrey; Linda S Steelman; William H Chappell; Stephen L Abrams; Richard A Franklin; Giuseppe Montalto; Melchiorre Cervello; Massimo Libra; Saverio Candido; Grazia Malaponte; Maria C Mazzarino; Paolo Fagone; Ferdinando Nicoletti; Jörg Bäsecke; Sanja Mijatovic; Danijela Maksimovic-Ivanic; Michele Milella; Agostino Tafuri; Francesca Chiarini; Camilla Evangelisti; Lucio Cocco; Alberto M Martelli
Journal:  Oncotarget       Date:  2012-10

10.  Targeting the Mammalian Target of Rapamycin (mTOR) in Cancer Therapy: Lessons from Past and Future Perspectives.

Authors:  Marc Dufour; Anne Dormond-Meuwly; Nicolas Demartines; Olivier Dormond
Journal:  Cancers (Basel)       Date:  2011-05-24       Impact factor: 6.639

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