Characterization of a Steroid Receptor Coactivator Small Molecule Stimulator that Overstimulates Cancer Cells and Leads to Cell Stress and Death

By integrating growth pathways on which cancer cells rely, steroid receptor coactivators (SRC-1, SRC-2, and SRC-3) represent emerging targets in cancer therapeutics. High-throughput screening for SRC small molecule inhibitors (SMIs) uncovered MCB-613 as a potent SRC small molecule “stimulator” (SMS)...

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Bibliographic Details
Published in:	Cancer cell 2015-08, Vol.28 (2), p.240-252
Main Authors:	Wang, Lei, Yu, Yang, Chow, Dar-Chone, Yan, Fei, Hsu, Chih-Chao, Stossi, Fabio, Mancini, Michael A., Palzkill, Timothy, Liao, Lan, Zhou, Suoling, Xu, Jianming, Lonard, David M., O’Malley, Bert W.
Format:	Article
Language:	English
Subjects:	Cell Line, Tumor Cell Survival - drug effects Cyclohexanones - chemistry Cyclohexanones - metabolism Cyclohexanones - pharmacology Drug Screening Assays, Antitumor - methods Endoplasmic Reticulum Stress - drug effects HEK293 Cells HeLa Cells Humans Immunoblotting MCF-7 Cells Molecular Structure Mutation Neoplasms - genetics Neoplasms - metabolism Neoplasms - prevention & control Nuclear Receptor Coactivator 1 - genetics Nuclear Receptor Coactivator 1 - metabolism Nuclear Receptor Coactivator 2 - genetics Nuclear Receptor Coactivator 2 - metabolism Nuclear Receptor Coactivator 3 - genetics Nuclear Receptor Coactivator 3 - metabolism Oxidative Stress - drug effects Protein Binding - drug effects Pyridines - chemistry Pyridines - metabolism Pyridines - pharmacology Reactive Oxygen Species - metabolism Reverse Transcriptase Polymerase Chain Reaction RNA Interference Small Molecule Libraries - chemistry Small Molecule Libraries - metabolism Small Molecule Libraries - pharmacology Tumor Burden - drug effects Xenograft Model Antitumor Assays
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