Literature DB >> 27134695

mTOR Inhibitors at a Glance.

Yin Zheng1, Yu Jiang2.   

Abstract

Mechanistic target of rapamycin (mTOR) is a conserved threonine and serine protein kinase that was identified more than two decades ago as the target of immunosuppressive drug rapamycin. Since then considerable amount of information has been learned about the function of this kinase. It is now well-established that mTOR plays a pivotal role in governing cell growth and proliferation, hence making mTOR a therapeutic target for disease conditions caused by deregulated cell proliferation, such as cancer. In the past decade, numerous mTOR inhibitors have been developed and many are currently in clinical trials for cancer treatment. This commentary is to provide a brief summary of these mTOR inhibitors.

Entities:  

Keywords:  Akt; Kinase inhibitors; Phosphatidylinositol-3-kinase; Rapamycin; mTOR

Year:  2015        PMID: 27134695      PMCID: PMC4849280     

Source DB:  PubMed          Journal:  Mol Cell Pharmacol        ISSN: 1938-1247


  48 in total

Review 1.  Modulation of the protein kinase activity of mTOR.

Authors:  J C Lawrence; T A Lin; L P McMahon; K M Choi
Journal:  Curr Top Microbiol Immunol       Date:  2004       Impact factor: 4.291

2.  Identification of GNE-477, a potent and efficacious dual PI3K/mTOR inhibitor.

Authors:  Timothy P Heffron; Megan Berry; Georgette Castanedo; Christine Chang; Irina Chuckowree; Jennafer Dotson; Adrian Folkes; Janet Gunzner; John D Lesnick; Cristina Lewis; Simon Mathieu; Jim Nonomiya; Alan Olivero; Jodie Pang; David Peterson; Laurent Salphati; Deepak Sampath; Steve Sideris; Daniel P Sutherlin; Vickie Tsui; Nan Chi Wan; Shumei Wang; Susan Wong; Bing-Yan Zhu
Journal:  Bioorg Med Chem Lett       Date:  2010-03-12       Impact factor: 2.823

3.  Characterization of the activity of the PI3K/mTOR inhibitor XL765 (SAR245409) in tumor models with diverse genetic alterations affecting the PI3K pathway.

Authors:  Peiwen Yu; A Douglas Laird; Xiangnan Du; Jianming Wu; Kwang-Ai Won; Kyoko Yamaguchi; Pin Pin Hsu; Fawn Qian; Christopher T Jaeger; Wentao Zhang; Chris A Buhr; Paula Shen; Wendy Abulafia; Jason Chen; Jenny Young; Arthur Plonowski; F Michael Yakes; Felix Chu; Michelle Lee; Frauke Bentzien; Sanh Tan Lam; Stephanie Dale; David J Matthews; Peter Lamb; Paul Foster
Journal:  Mol Cancer Ther       Date:  2014-03-14       Impact factor: 6.261

Review 4.  mTOR signaling and drug development in cancer.

Authors:  Janet Dancey
Journal:  Nat Rev Clin Oncol       Date:  2010-03-16       Impact factor: 66.675

5.  Dual mTORC1/mTORC2 inhibition diminishes Akt activation and induces Puma-dependent apoptosis in lymphoid malignancies.

Authors:  Mamta Gupta; Andrea E Wahner Hendrickson; Seong Seok Yun; Jing Jing Han; Paula A Schneider; Brian D Koh; Mary J Stenson; Linda E Wellik; Jennifer C Shing; Kevin L Peterson; Karen S Flatten; Allan D Hess; B Douglas Smith; Judith E Karp; Sharon Barr; Thomas E Witzig; Scott H Kaufmann
Journal:  Blood       Date:  2011-11-11       Impact factor: 22.113

Review 6.  Mechanisms of mTOR inhibitor resistance in cancer therapy.

Authors:  Jennifer S Carew; Kevin R Kelly; Steffan T Nawrocki
Journal:  Target Oncol       Date:  2011-03-09       Impact factor: 4.493

Review 7.  Rapamycins: mechanism of action and cellular resistance.

Authors:  Shile Huang; Mary-Ann Bjornsti; Peter J Houghton
Journal:  Cancer Biol Ther       Date:  2003 May-Jun       Impact factor: 4.742

Review 8.  Achieving cancer cell death with PI3K/mTOR-targeted therapies.

Authors:  Sung Su Yea; David A Fruman
Journal:  Ann N Y Acad Sci       Date:  2013-03       Impact factor: 5.691

9.  An ATP-competitive mammalian target of rapamycin inhibitor reveals rapamycin-resistant functions of mTORC1.

Authors:  Carson C Thoreen; Seong A Kang; Jae Won Chang; Qingsong Liu; Jianming Zhang; Yi Gao; Laurie J Reichling; Taebo Sim; David M Sabatini; Nathanael S Gray
Journal:  J Biol Chem       Date:  2009-01-15       Impact factor: 5.157

Review 10.  Emerging common themes in regulation of PIKKs and PI3Ks.

Authors:  Harri Lempiäinen; Thanos D Halazonetis
Journal:  EMBO J       Date:  2009-09-24       Impact factor: 11.598

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  34 in total

1.  New Mechanisms of mTOR Pathway Activation in KIT-mutant Malignant GISTs.

Authors:  Jerzy Lasota; Artur Kowalik; Anna Felisiak-Golabek; Sebastian Zięba; Zeng-Feng Wang; Markku Miettinen
Journal:  Appl Immunohistochem Mol Morphol       Date:  2019-01

2.  MYCing and YAPing the escape of tumor cell growth arrest after chronic PI3K/mTOR inhibition.

Authors:  Georgios D Vavougios; Sotirios G Zarogiannis
Journal:  J Thorac Dis       Date:  2017-05       Impact factor: 2.895

Review 3.  mTOR in Lung Neoplasms.

Authors:  Ildiko Krencz; Anna Sebestyen; Andras Khoor
Journal:  Pathol Oncol Res       Date:  2020-02-03       Impact factor: 3.201

4.  Protein Methylation and Translation: Role of Lysine Modification on the Function of Yeast Elongation Factor 1A.

Authors:  Jonelle T White; Tieranee Cato; Neil Deramchi; Jason Gabunilas; Kevin R Roy; Charles Wang; Guillaume F Chanfreau; Steven G Clarke
Journal:  Biochemistry       Date:  2019-12-02       Impact factor: 3.162

5.  Combined mTORC1/mTORC2 inhibition blocks growth and induces catastrophic macropinocytosis in cancer cells.

Authors:  Ritesh K Srivastava; Changzhao Li; Jasim Khan; Nilam Sanjib Banerjee; Louise T Chow; Mohammad Athar
Journal:  Proc Natl Acad Sci U S A       Date:  2019-11-15       Impact factor: 11.205

6.  Modulator of the PI3K/Akt oncogenic pathway affects mTOR complex 2 in human adenocarcinoma cells.

Authors:  Blair P Curless; Nne E Uko; Diane F Matesic
Journal:  Invest New Drugs       Date:  2018-12-13       Impact factor: 3.850

7.  Profiling the Surfaceome Identifies Therapeutic Targets for Cells with Hyperactive mTORC1 Signaling.

Authors:  Junnian Wei; Kevin Leung; Charles Truillet; Davide Ruggero; James A Wells; Michael J Evans
Journal:  Mol Cell Proteomics       Date:  2019-12-02       Impact factor: 5.911

8.  Pharmacological Inhibition of mTOR Kinase Reverses Right Ventricle Remodeling and Improves Right Ventricle Structure and Function in Rats.

Authors:  Andressa Pena; Ahasanul Kobir; Dmitry Goncharov; Akiko Goda; Tatiana V Kudryashova; Arnab Ray; Rebecca Vanderpool; Jeffrey Baust; Baojun Chang; Ana L Mora; John Gorcsan; Elena A Goncharova
Journal:  Am J Respir Cell Mol Biol       Date:  2017-11       Impact factor: 6.914

Review 9.  An update: emerging drugs to treat squamous cell carcinomas of the head and neck.

Authors:  Yoon Se Lee; Daniel E Johnson; Jennifer R Grandis
Journal:  Expert Opin Emerg Drugs       Date:  2018-11-16       Impact factor: 4.191

10.  Connectivity Map Analysis of a Single-Cell RNA-Sequencing -Derived Transcriptional Signature of mTOR Signaling.

Authors:  Naim Al Mahi; Erik Y Zhang; Susan Sherman; Jane J Yu; Mario Medvedovic
Journal:  Int J Mol Sci       Date:  2021-04-22       Impact factor: 5.923

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