Preferred Label : HIF-2alpha Inhibitor AB521;
NCIt synonyms : HIF-2a Inhibitor AB521;
NCIt definition : An orally bioavailable allosteric inhibitor of hypoxia inducible factor (HIF)-2alpha,
with potential antineoplastic activity. Upon oral administration, HIF-2alpha inhibitor
AB521 targets and allosterically binds to a hydrophobic pocket on HIF-2alpha leading
to a confirmational change that prevents HIF-2alpha heterodimerization with HIF-1beta
and binding to the hypoxia response element (HRE) binding site on DNA. This results
in decreased transcription and expression of HIF-2alpha downstream target genes, many
of which regulate tumor cell growth and survival. Blocking HIF-2alpha reduces the
proliferation of HIF-2alpha-expressing tumor cells. HIF-2alpha, a heterodimeric transcription
factor overexpressed under hypoxic conditions in many cancer cell types, promotes
proliferation, progression and metastasis of tumors.;
Molecule name : AB 521; AB-521;
NCI Metathesaurus CUI : CL1912584;
Origin ID : C192674;
UMLS CUI : C5785369;
Semantic type(s)
- concept_is_in_subset
- has_target
