title: Steroid receptor coactivators present a unique opportunity for drug development in hormone-dependent cancers.
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.
authors.affiliation: Department of Molecular and Cellular Biology, Baylor College of Medicine, Houston, TX 77030, USA.
authors.forename: Aarti D
authors.initials: AD
authors.lastname: Rohira
authors.affiliation: Department of Molecular and Cellular Biology, Baylor College of Medicine, Houston, TX 77030, USA. Electronic address: dlonard@bcm.edu.
authors.forename: David M
authors.initials: DM
authors.lastname: Lonard
mesh_terms: D000893:Anti-Inflammatory Agents / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D015195:Drug Design; D018432:Drug Resistance, Multiple; D019008:Drug Resistance, Neoplasm; D006801:Humans; D008024:Ligands; D058990:Molecular Targeted Therapy; D009363:Neoplasm Proteins / Q000037:antagonists & inhibitors / Q000737:chemistry / Q000378:metabolism; D009376:Neoplasms, Hormone-Dependent / Q000188:drug therapy* / Q000276:immunology / Q000378:metabolism; D056920:Nuclear Receptor Coactivator 1 / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000378:metabolism; D051958:Nuclear Receptor Coactivator 2 / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000378:metabolism; D056921:Nuclear Receptor Coactivator 3 / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000378:metabolism; D054730:Protein Interaction Domains and Motifs
chemical_list: D000893:Anti-Inflammatory Agents; D000894:Anti-Inflammatory Agents, Non-Steroidal; D000970:Antineoplastic Agents; D008024:Ligands; C498001:NCOA2 protein, human; D009363:Neoplasm Proteins; D051958:Nuclear Receptor Coactivator 2; C538859:NCOA1 protein, human; C538866:NCOA3 protein, human; D056920:Nuclear Receptor Coactivator 1; D056921:Nuclear Receptor Coactivator 3
keywords: Coregulator; Drug development; Hormone-dependent cancer; Steroid receptor coactivator; Transcription