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Overview
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Background
PPT, abbreviated from propyl pyrazole triol, is a potent, selective agonist of estrogen receptor α (ERα), with a reported 410-fold selectivity for ERα over ERβ. ERα is one of two main types of estrogen receptor, a nuclear receptor that is activated by the sex hormone estrogen and involved in normal developmental, physiological, and reproductive processes in vertebrates. Compared with ERβ, ERα is encoded by a distinct gene, and differs in its relative and absolute tissue distribution. Since PPT exhibits subtype-selective property for estrogen receptors, it may serve as a useful tool for exploring how estrogens work through different ER subtypes.
1. Sotoca AM, van den Berg H, Vervoort J, et al. Influence of cellular ERα/ERβ ratio on the ERα-agonist induced proliferation of human T47D breast cancer cells. Toxicological Sciences, 2008, 105(2): 303-311.
2. Stauffer SR, Coletta CJ, Tedesco R, et al. Pyrazole ligands: structure-affinity/activity relationships and estrogen receptor-alpha-selective agonists. Journal of Medicinal Chemistry, 2000, 43(26): 4934-4947.
3. Harris HA, Katzenellenbogen JA, Katzenellenbogen BS. Characterization of the biological roles of the estrogen receptors, ERα and ERβ, in estrogen target tissues in vivo through the use of an ERα-selective ligand. Endocrinology, 2002, 143(11): 4172-4177.
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