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Version: 17.12d (Release date: 2017-12-26)
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ERa36 Modulator Icaritin (Code C95720)

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Terms & Properties

Preferred Name: ERa36 Modulator Icaritin

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.

Label: ERa36 Modulator Icaritin

NCI Thesaurus Code: C95720 (Search for linked caDSR metadata)  (search value sets)

NCI Metathesaurus Link: C1567768  (see NCI Metathesaurus info)

Synonyms & Abbreviations: (see Synonym Details)
4H-1-Benzopyran-4-one, 3,5,7-trihydroxy-2-(4-methoxyphenyl)-8-(3-methyl-2-butenyl)-
ERa36 Modulator Icaritin

External Source Codes: 
CAS Registry Number 118525-40-9 (see NLM ChemIDplus info)
PDQ Closed Trial Search ID 694226
PDQ Open Trial Search ID 694226 (check for NCI PDQ open clinical trial info)
PubMedID Primary Reference 17382317 (see PubMed Primary Reference info)
UMLS CUI C1567768

Other Properties:
     Name Value (qualifiers indented underneath)
code C95720
Semantic_Type Pharmacologic Substance

Additional Concept Data: 
Defined Fully by Roles: No  


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