Vaccinium

by | Mar 20, 2018 | Vaccinium

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Methylpiperidinopyrazole (MPP) is a synthetic, nonsteroidal, and highly selective antagonist of ERα that is used in scientific research to study the function of this receptor.[1][2] It has 200-fold selectivity for ERα over ERβ and 1000-fold selectivity for blocking ERα-mediated gene transcription relative to that of ERβ.[3]

See also

References

  1. ^ Sun J, Huang YR, Harrington WR, Sheng S, Katzenellenbogen JA, Katzenellenbogen BS (March 2002). "Antagonists selective for estrogen receptor alpha". Endocrinology. 143 (3): 941–7. doi:10.1210/endo.143.3.8704. PMID 11861516.
  2. ^ Zhou HB, Carlson KE, Stossi F, Katzenellenbogen BS, Katzenellenbogen JA (January 2009). "Analogs of methyl-piperidinopyrazole (MPP): antiestrogens with estrogen receptor alpha selective activity". Bioorganic & Medicinal Chemistry Letters. 19 (1): 108–10. doi:10.1016/j.bmcl.2008.11.006. PMC 2711511. PMID 19014882.
  3. ^ Ottow E, Weinmann H (8 September 2008). Nuclear Receptors as Drug Targets. John Wiley & Sons. pp. 50–. ISBN 978-3-527-62330-3.
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