Preferred Label : BET-bromodomain Inhibitor ODM-207;
NCIt synonyms : Bromodomain and Extraterminal Domain Protein Inhibitor ODM-207; BET Inhibitor ODM-207;
NCIt related terms : ODM-207;
NCIt definition : An orally bioavailable inhibitor of the Bromodomain and Extra-Terminal (BET) family
of proteins, with potential antineoplastic activity. Upon oral administration, the
BET inhibitor ODM-207 binds to the acetylated lysine recognition motifs in the bromodomains
of BET proteins, thereby preventing the interaction between the BET proteins and acetylated
histones. This disrupts chromatin remodeling and gene expression of oncogenic drivers
that are important for cell proliferation and survival. Prevention of the expression
of certain growth-promoting genes may lead to an inhibition of proliferation in BET-overexpressing
tumor cells. BET proteins, comprised of BRD2, BRD3, BRD4 and BRDT, are transcriptional
regulators that bind to acetylated lysine residues in histones and play an important
role during development and cellular growth. In tumor cells, BET proteins play a key
role in the regulation of oncogene transcription and tumor cell proliferation.;
UNII : BL5NEF7JDK;
CAS number : 1801503-93-4;
Molecule name : ODM 207; ODM-207;
NCI Metathesaurus CUI : CL550806;
Origin ID : C148138;
UMLS CUI : C4724841;
Semantic type(s)
- UMLS correspondences (same concept)
- ODM-207 [MeSH Supplementary Concept]
- concept_is_in_subset
