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

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...

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Published inBiochemical Society transactions Vol. 39; no. 2; p. 456
Main Authors Marshall, Gayle, Howard, Zoe, Dry, Jonathan, Fenton, Sarah, Heathcote, Dan, Gray, Neil, Keen, Heather, Logie, Armelle, Holt, Sarah, Smith, Paul, Guichard, Sylvie M
Format Journal Article
LanguageEnglish
Published England 01.04.2011
Subjects
Animals
Antineoplastic Agents - therapeutic use
Drug Evaluation, Preclinical
Humans
Medical Oncology - methods
Molecular Targeted Therapy - methods
Morpholines - therapeutic use
Neoplasms - drug therapy
Protein Kinase Inhibitors - pharmacology
Protein Kinase Inhibitors - therapeutic use
Sirolimus - analogs & derivatives
Sirolimus - pharmacology
Sirolimus - therapeutic use
TOR Serine-Threonine Kinases - antagonists & inhibitors
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Summary: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.
ISSN:1470-8752
DOI:10.1042/BST0390456