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Updated: Apr 5, 2026

Identification of Mediators of T-cell Receptor Signaling via the Screening of Chemical Inhibitor Libraries
08:49

Identification of Mediators of T-cell Receptor Signaling via the Screening of Chemical Inhibitor Libraries

Published on: January 22, 2019

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Characterization of a Steroid Receptor Coactivator Small Molecule Stimulator that Overstimulates Cancer Cells and

Lei Wang1, Yang Yu1, Dar-Chone Chow2

  • 1Department of Molecular and Cellular Biology, Baylor College of Medicine, Houston, TX 77030, USA.

Cancer Cell
|August 13, 2015
PubMed

Insights

Steroid receptor coactivators (SRCs) are key for cancer growth. A new compound, MCB-613, over-stimulates SRCs, causing cancer cell death via excessive stress and reactive oxygen species (ROS).

Area of Science:

  • Oncology
  • Molecular Biology
  • Biochemistry

Background:

  • Steroid receptor coactivators (SRCs) are crucial for cancer cell growth and proliferation.
  • SRCs are emerging as significant therapeutic targets in cancer treatment.

Purpose of the Study:

  • To investigate the potential of targeting SRCs in cancer therapy.
  • To identify and characterize small molecules that modulate SRC activity.

Main Methods:

  • High-throughput screening was employed to identify SRC modulators.
  • MCB-613 was identified as a potent SRC small molecule stimulator (SMS).
  • The effects of MCB-613 on SRC transcriptional activity, coactivator interactions, ER stress, and ROS generation were analyzed.

Main Results:

  • MCB-613 was found to super-stimulate SRC transcriptional activity.
  • MCB-613 enhanced SRC interactions with other coactivators.
  • MCB-613 induced significant ER stress and reactive oxygen species (ROS) generation.

Conclusions:

  • Over-stimulating the SRC oncogenic program with MCB-613 selectively induces excessive stress in cancer cells.
  • Targeting SRCs through over-stimulation presents a novel strategy for cancer cell killing.

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