Preferred Label : Birabresib;
NCIt synonyms : BRD 2/3/4 Inhibitor OTX015; 6H-Thieno(3,2-f)(1,2,4)triazolo(4,3-a)(1,4)diazepine-6-acetamide, 4-(4-Chlorophenyl)-N-(4-hydroxyphenyl)-2,3,9-trimethyl-,
(6S)-;
NCIt definition : A synthetic, small molecule inhibitor of the BET (Bromodomain and Extra-Terminal)
family of bromodomain-containing proteins 2, 3 and 4 with potential antineoplastic
activity. Upon administration, birabresib binds to the acetylated lysine recognition
motifs on the bromodomain of BET proteins, thereby preventing the interaction between
the BET proteins and acetylated histone peptides. This disrupts chromatin remodeling
and gene expression. Prevention of the expression of certain growth-promoting genes,
including c-Myc-dependent target genes, may lead to an inhibition of tumor cell growth.
Characterized by a tandem repeat of bromodomain at the N-terminus, the BET proteins
BRD2, BRD3, BRD4 are transcriptional regulators that play an important role in cellular
growth.;
UNII : X40LKS49S3;
InChIKey : GNMUEVRJHCWKTO-FQEVSTJZSA-N;
CAS number : 202590-98-5;
Molecule name : OTX015; MK-8628;
Origin ID : C103298;
UMLS CUI : C4552083;
Semantic type(s)
- concept_is_in_subset
- has_target
