Specific blockade of Rictor-mTOR association inhibits mTORC2 activity and is cytotoxic in glioblastoma

A small molecule which specifically blocks the interaction of Rictor and mTOR was identified utilizing a high-throughput yeast two-hybrid screen and evaluated as a potential inhibitor of mTORC2 activity in glioblastoma multiforme (GBM). In vitro, CID613034 inhibited mTORC2 kinase activity at submicr...

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Veröffentlicht in:	PloS one 2017-04, Vol.12 (4), p.e0176599
Hauptverfasser:	Benavides-Serrato, Angelica, Lee, Jihye, Holmes, Brent, Landon, Kenna A, Bashir, Tariq, Jung, Michael E, Lichtenstein, Alan, Gera, Joseph
Format:	Artikel
Sprache:	eng
Schlagworte:	1-Phosphatidylinositol 3-kinase Acetylation Actin Activation Adipocytes AKT protein Animals Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Antineoplastic Agents - therapeutic use Apoptosis Assembly Binding Binding proteins Bioactive Biochemistry Biology Biology and Life Sciences Biotechnology Brain cancer Brain tumors Cancer Carrier Proteins - metabolism Cell cycle Cell death Cell Line, Tumor Cell size Cell survival Chemistry Cullin Cytoskeleton Cytotoxicity Destruction Drug resistance Drug therapy Drugs Engineering and Technology Enzyme inhibitors Gene Expression Regulation, Neoplastic - drug effects Genetic engineering Genetics Glioblastoma - drug therapy Glioblastoma - pathology Glioblastomas Glucose Growth factors Health care Humans Inhibition Inhibitors Kinases Light emitting diodes Mechanistic Target of Rapamycin Complex 2 Medical prognosis Medicine Medicine and Health Sciences Mice Molecular biology Multiprotein Complexes - antagonists & inhibitors Multiprotein Complexes - metabolism Mutation Negative feedback Neoplasms Nervous system Phosphorylation Physical Sciences Polarization Properties Protein Binding - drug effects R&D Rapamycin-Insensitive Companion of mTOR Protein Research & development Research and Analysis Methods Screens Sensitivity Signal transduction Signal Transduction - drug effects Small Molecule Libraries - chemistry Small Molecule Libraries - pharmacology Small Molecule Libraries - therapeutic use Structure-Activity Relationship Surgery Survival TOR Serine-Threonine Kinases - antagonists & inhibitors TOR Serine-Threonine Kinases - metabolism Toxicity Transformation Tumor cells Tumors Veterans Xenograft Model Antitumor Assays Xenografts Yeasts
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