Preferred Label : Selective Human Estrogen-receptor Alpha Partial Agonist TTC-352;
NCIt synonyms : 3-(4-Fluorophenyl)-2-(4-hydroxyphenoxy)benzo[b]thiophen-6-ol; ShERPA TTC-352; ERa Partial Agonist TTC-352; SEM TTC-352; Selective Estrogen Mimic TTC-352; Selective Estrogen Modulator TTC-352;
NCIt related terms : TTC-352;
NCIt definition : A benzothiophene and orally bioavailable selective human estrogen receptor alpha (ERalpha;
ESR1; ERa) partial agonist (ShERPA), with potential antineoplastic activity. Upon
administration, TTC-352 mimics the naturally-occurring 17beta-estradiol (E2) and targets
and binds to ERa located in the nucleus. This causes translocation of ERa to extranuclear
sites. Nuclear export of ERa prevents normal ER-mediated signaling and inhibits proliferation
of ER-positive tumor cells. TTC-352 causes tumor regression of tamoxifen (TAM)-resistant
(TR) tumor cells which often overexpress protein kinase C alpha (PKCalpha; PKCa).
PKCa expression is associated with poor patient survival and breast cancer aggressiveness
and may predict tumor responses to E2, E2-like compounds and ShERPAs. Unlike E2 and
E2-like compounds, TTC-352 does not cause endometrial proliferation.;
UNII : 65ILH3Y0MI;
CAS number : 1607819-68-0;
Molecule name : TTC-352; TTC 352;
NCI Metathesaurus CUI : CL552181;
Origin ID : C150363;
UMLS CUI : C4725680;
Semantic type(s)
- concept_is_in_subset
- has_target
