Tamoxifen Isomers and Metabolites Exhibit Distinct Affinity and Activity at Cannabinoid Receptors: Potential Scaffold for Drug Development

Tamoxifen (Tam) is a selective estrogen receptor (ER) modulator (SERM) that is an essential drug to treat ER-positive breast cancer. Aside from known actions at ERs, recent studies have suggested that some SERMs like Tam also exhibit novel activity at cannabinoid subtype 1 and 2 receptors (CB1R and...

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Veröffentlicht in:	PloS one 2016-12, Vol.11 (12), p.e0167240
Hauptverfasser:	Ford, Benjamin M, Franks, Lirit N, Radominska-Pandya, Anna, Prather, Paul L
Format:	Artikel
Sprache:	eng
Schlagworte:	Adenylyl Cyclases - metabolism Affinity Animals Binding, Competitive Biology and Life Sciences Breast cancer Breast Neoplasms - drug therapy Breast Neoplasms - metabolism Cannabinoid CB1 receptors Cannabinoid CB2 receptors Cannabinoid Receptor Agonists - metabolism Cannabinoid Receptor Agonists - pharmacology Cannabinoid Receptor Antagonists - metabolism Cannabinoid Receptor Antagonists - pharmacology Cell growth Cell receptors CHO Cells Colforsin - metabolism Colforsin - pharmacology Cricetinae Cricetulus Cyclic AMP - metabolism Cyclohexanols - metabolism Cyclohexanols - pharmacology Cytochrome Cytochrome P450 Development and progression Drug development Drug metabolism Drug therapy Drugs Estrogen receptors Estrogens FDA approval Female Genetic aspects GTP-Binding Proteins - metabolism Guanosine 5'-O-(3-Thiotriphosphate) - metabolism Health aspects Humans Indoles - metabolism Indoles - pharmacology Inverse agonists Isomerism Isomers Medical treatment Medicine Medicine and Health Sciences Metabolites Osteoporosis Patient outcomes Pharmacology Physical Sciences Proteins Receptor, Cannabinoid, CB1 - agonists Receptor, Cannabinoid, CB1 - antagonists & inhibitors Receptor, Cannabinoid, CB1 - metabolism Receptor, Cannabinoid, CB2 - agonists Receptor, Cannabinoid, CB2 - antagonists & inhibitors Receptor, Cannabinoid, CB2 - metabolism Receptors Research and Analysis Methods Selective estrogen receptor modulators Selective Estrogen Receptor Modulators - chemistry Selective Estrogen Receptor Modulators - metabolism Selective Estrogen Receptor Modulators - pharmacology Studies Tamoxifen Tamoxifen - analogs & derivatives Tamoxifen - chemistry Tamoxifen - metabolism Tamoxifen - pharmacology Toxicology
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