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• W2029202752 endingPage "370" @default.
• W2029202752 startingPage "361" @default.
• W2029202752 abstract "Introduction: S2R (sigma-2 receptor)/Pgrmc1 (progesterone receptor membrane component 1) is a cytochrome-related protein that binds directly to heme and various pharmacological compounds. S2RPgrmc1 also associates with cytochrome P450 proteins, the EGFR receptor tyrosine kinase and the RNA-binding protein PAIR-BP1. S2RPgrmc1 is induced in multiple types of cancer, where it regulates tumor growth and is implicated in progesterone signaling. S2RPgrmc1 also increases cholesterol synthesis in non-cancerous cells and may have a role in modulating drug metabolizing P450 proteins. Areas covered: This review covers the independent identification of S2R and Pgrmc1 and their induction in cancers, as well as the role of S2RPgrmc1 in increasing cholesterol metabolism and P450 activity. This article was formed through a PubMed literature search using, but not limited to, the terms sigma-2 receptor, Pgrmc1, Dap1, cholesterol and aromatase. Expert opinion: Multiple laboratories have shown that S2RPgrmc1 associates with various P450 proteins and increases cholesterol synthesis via Cyp51. However, the lipogenic role of S2RPgrmc1 is tissue-specific. Furthermore, the role of S2RPgrmc1 in regulating P450 proteins other than Cyp51 appears to be highly selective, with modest inhibitory activity for Cyp3A4 in vitro and a complex regulatory pattern for Cyp21. Cyp19/aromatase is a therapeutic target in breast cancer, and S2RPgrmc1 activated Cyp19 significantly in vitro but modestly in biochemical assays. In summary, S2RPgrmc1 is a promising therapeutic target for cancer and possibly cholesterol synthesis but research to date has not identified a major role in P450-mediated drug metabolism." @default.
• W2029202752 created "2016-06-24" @default.
• W2029202752 creator A5025745759 @default.
• W2029202752 creator A5039960048 @default.
• W2029202752 creator A5062386707 @default.
• W2029202752 date "2012-02-01" @default.
• W2029202752 modified "2023-10-04" @default.
• W2029202752 title "S2R^Pgrmc1: the cytochrome-related sigma-2 receptor that regulates lipid and drug metabolism and hormone signaling" @default.
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• W2029202752 doi "https://doi.org/10.1517/17425255.2012.658367" @default.
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• W2029202752 hasPublicationYear "2012" @default.
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