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Steroid receptor coactivators present a unique opportunity for drug development in hormone-dependent cancers
Aarti D Rohira1, David M Lonard1
1Department of Molecular and Cellular Biology, Baylor College of Medicine, Houston, TX 77030, USA.
Abstract:
Steroid receptor coactivators (SRCs) are essential regulators of nuclear hormone receptor function. SRCs coactivate transcription mediated by hormone stimulation of nuclear receptors and other transcription factors and have essential functions in human physiology and health. The SRCs are over expressed in a number of cancers such as breast, prostate, endometrial and pancreatic cancers where they promote tumor growth, invasion, metastasis and chemo-resistance. With their multiple roles in cancer, the SRCs are promising targets for the development of small molecule agents that can interfere with their function. For instance, perturbing SRC function with small molecule inhibitors and stimulators has been shown to be effective in reducing tumor growth in vivo. These early studies demonstrate that targeting the SRCs might prove effective for cancer treatment and more effort should be made to realize the untapped potential of developing drugs designed to target these coactivators.
Insights
Steroid receptor coactivators (SRCs) are crucial for hormone signaling and are overexpressed in many cancers. Targeting SRCs with small molecules shows promise for effective cancer treatment by inhibiting tumor growth and resistance.
Area of Science:
- Molecular Biology
- Cancer Biology
- Endocrinology
Background:
- Steroid receptor coactivators (SRCs) are key regulators of nuclear hormone receptor activity.
- SRCs play vital roles in human physiology and are implicated in various cancers.
- Overexpression of SRCs contributes to tumor progression, invasion, metastasis, and chemoresistance.
Purpose of the Study:
- To highlight the significance of SRCs as therapeutic targets in oncology.
- To review the potential of small molecule agents in modulating SRC function for cancer treatment.
Main Methods:
- Literature review of SRC function in cancer.
- Analysis of studies investigating small molecule inhibitors and stimulators of SRCs.
- Evaluation of in vivo data on SRC-targeted therapies.
Main Results:
- SRCs are overexpressed in breast, prostate, endometrial, and pancreatic cancers.
- Perturbation of SRC function with small molecules has demonstrated efficacy in reducing tumor growth in vivo.
- Targeting SRCs offers a promising strategy for cancer therapy.
Conclusions:
- SRCs are critical mediators of cancer development and progression.
- Small molecule-based strategies targeting SRCs represent a promising avenue for novel cancer therapeutics.
- Further research into SRC-targeted drug development is warranted to exploit their full therapeutic potential.