Preferred Label : BET Inhibitor JAB-8263;
NCIt definition : An orally bioavailable inhibitor of the bromodomain and extra-terminal (BET) family
of proteins, with potential antineoplastic and anti-fibrotic activities. Upon oral
administration, BET inhibitor JAB-8263 targets and binds to bromodomain-containing
proteins 2, 3, and 4 (BRD2, BRD3, and BRD4) as well as bromodomain testis-specific
protein (BRDT), thereby preventing the interaction between BET proteins and acetylated
histones. This disrupts chromatin remodeling and suppresses the expression of certain
oncogenes and profibrotic genes, including Myc and other transcriptional regulators.
Preventing the expression of certain growth-promoting genes may lead to an inhibition
of tumor cell growth and fibrosis. Characterized by a tandem repeat of bromodomains
at the N-terminus, BET proteins, comprised of BRD2, BRD3, BRD4 and BRDT, are transcriptional
regulators that play an important role during cellular development and growth.;
Molecule name : JAB8-263; JAB 8263;
NCI Metathesaurus CUI : CL1662149;
Origin ID : C179628;
UMLS CUI : C5555824;
Semantic type(s)
- concept_is_in_subset
- has_target
