Preferred Label : ERa36 Modulator Icaritin;
NCIt synonyms : 4H-1-Benzopyran-4-one, 3,5,7-trihydroxy-2-(4-methoxyphenyl)-8-(3-methyl-2-butenyl)-;
NCIt 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.;
CAS number : 118525-40-9;
PubMed : 17382317;
Origin ID : C95720;
UMLS CUI : C1567768;
Semantic type(s)
- UMLS correspondences (same concept)
- concept_is_in_subset
