Preferred Label : Selective Estrogen Receptor Covalent Antagonist H3B-6545;
NCIt synonyms : SERCA H3B-6545;
NCIt definition : An orally available, selective and covalent antagonist of estrogen receptor alpha
(ERalpha; ERa; ESR1; nuclear receptor subfamily 3, group A, member 1; NR3A1), with
potential antineoplastic activity. Upon oral administration, selective estrogen receptor
covalent antagonist (SERCA) H3B-6545 selectively and covalently binds to a cysteine
that is unique to ERalpha and is not present in other nuclear hormone receptors, thereby
inhibiting the activity of ERalpha. This inhibits the growth and survival of ERalpha-expressing
cancer cells. ERalpha, a nuclear hormone receptor, is often overexpressed and/or mutated
in a variety of cancer cell types. It plays a key role in tumor cell proliferation
and survival.;
Molecule name : H3B 6545; H3B-6545;
NCI Metathesaurus CUI : CL541412;
Origin ID : C142980;
UMLS CUI : C4684940;
Semantic type(s)
- UMLS correspondences (same concept)
- concept_is_in_subset
