Propylpyrazoletriol (PPT) is a synthetic, nonsteroidal agonist of ERα with 400-fold selectivity over ERβ[1] that is used widely in scientific research to study the function of ERα.[2][3][4] Though originally thought to be highly selective for ERα, PPT has subsequently been found to also act as an agonist of the GPER (GPR30).[5]

See also

References

  1. ^ Weatherman RV (8 September 2008). "Untangling the Estrogen Receptor Web: Tools to Selectively Study Estrogen‐Binding Receptors". In Ottow E, Weinmann H (eds.). Nuclear Receptors as Drug Targets. Methods and Principles in Medicinal Chemistry. John Wiley & Sons. pp. 47–64 (50). doi:10.1002/9783527623297.ch3. ISBN 978-3-527-62330-3.
  2. ^ Pfaus JG, Jones SL, Flanagan-Cato LM, Blaustein JD (15 November 2014). "Female sexual behavior: Hormonal Priming and Control". In Plant TM, Zeleznik AJ (eds.). Knobil and Neill's Physiology of Reproduction: Two-Volume Set. Vol. 2. Academic Press. pp. 2287-2370 (2311). ISBN 978-0-12-397769-4.
  3. ^ Aguirre C, Jayaraman A, Pike C, Baudry M (December 2010). "Progesterone inhibits estrogen-mediated neuroprotection against excitotoxicity by down-regulating estrogen receptor-β". Journal of Neurochemistry. 115 (5): 1277–87. doi:10.1111/j.1471-4159.2010.07038.x. PMC 3010223. PMID 20977477.
  4. ^ Mann MK (2008). Synthesis of Non-steroidal Estrogen Receptor Proteolysis Targeting Chimeric Molecules (PROTACS) (Ph.D. thesis). University of Illinois at Urbana-Champaign. pp. 11–.
  5. ^ Prossnitz ER, Barton M (May 2014). "Estrogen biology: new insights into GPER function and clinical opportunities". Molecular and Cellular Endocrinology. 389 (1–2): 71–83. doi:10.1016/j.mce.2014.02.002. PMC 4040308. PMID 24530924.