About: ERa36 Modulator Icaritin     Goto   Sponge   NotDistinct   Permalink

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AttributesValues
rdf:type
rdfs:label
  • ERa36 Modulator Icaritin
rdfs:subClassOf
Semantic_Type
  • Pharmacologic Substance
Preferred_Name
  • ERa36 Modulator Icaritin
PubMedID_Primary_Reference
  • 17382317
UMLS_CUI
  • C1567768
CAS_Registry
  • 118525-40-9
PDQ_Open_Trial_Search_ID
  • 694226
PDQ_Closed_Trial_Search_ID
  • 694226
FULL_SYN
  • ERa36 Modulator IcaritinPTNCI
  • 4H-1-Benzopyran-4-one, 3,5,7-trihydroxy-2-(4-methoxyphenyl)-8-(3-methyl-2-butenyl)-SNNCI
DEFINITION
  • A metabolite of icariin, a principal flavonoid glycoside in Herba Epimedii (a traditional Chinese medicine herb used in treating osteoporosis) with potential antineoplastic activity. ERa36 modulator icaritin selectively binds to a novel variant of estrogen receptor alpha, a36, and mediates a membrane-initiated "nongenomic" signaling pathway, which is linked to activate signaling pathways like the MAPK/ERK and the PI3K/Akt pathways. This agent induces cell cycle arrest at G1, or G2/M arrest depending upon the dose. Consistently with G1 arrest, icaritin increases protein expressions of pRb, p27(Kip1) and p16(Ink4a), while decreasing phosphorylated pRb, Cyclin D1 and CDK4. 40% of ER-negative breast cancer tumors express high levels of ERa36, and this subset of patients is less likely to benefit from tamoxifen treatment compared with those with ERa66-positive/ERa36-negative tumors.NCI
code
  • C95720
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