Department of Molecular and Cellular Biology, Baylor College of Medicine, Houston, TX 77030, USA.
Department of Molecular and Cellular Biology, Baylor College of Medicine, Houston, TX 77030, USA.
Biochem Pharmacol. 2017 Sep 15;140:1-7. doi: 10.1016/j.bcp.2017.04.005. Epub 2017 Apr 6.
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.
甾体激素受体共激活因子（SRCs）是核激素受体功能的重要调节剂。SRC 共激活由激素刺激核受体和其他转录因子介导的转录，并在人体生理学和健康中具有重要功能。SRC 在许多癌症中过度表达，如乳腺癌、前列腺癌、子宫内膜癌和胰腺癌，它们促进肿瘤生长、侵袭、转移和化疗耐药。由于 SRC 在癌症中的多种作用，它们是开发能够干扰其功能的小分子药物的有前途的靶点。例如，用小分子抑制剂和激动剂扰乱 SRC 功能已被证明可有效减少体内肿瘤生长。这些早期研究表明，针对 SRC 可能对癌症治疗有效，应该更加努力地挖掘开发针对这些共激活因子的药物的潜力。
