NCIt synonyms : Bromodomain and Extra-Terminal Protein Inhibitor RO6870810;
NCIt related terms : RO-6870810;
NCIt definition : A small molecule inhibitor of the BET (Bromodomain and Extra-Terminal) family of bromodomain-containing
proteins with potential antineoplastic activity. Upon administration, the BET inhibitor
RO6870810 binds to the acetylated lysine recognition motifs found in the bromodomain
of BET proteins, which prevents the interaction between BET proteins and acetylated
histones. This interaction disrupts chromatin remodeling and gene expression. Prevention
of the expression of certain growth-promoting genes may lead to an inhibition of tumor
cell growth. 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.;
UNII : TA3QN7788D;
InChIKey : PKQXLRYFPSZKDU-QFIPXVFZSA-N;
CAS number : 1349719-98-7;
Molecule name : RO6870810; TEN-010; RG 6146; RG6146; TEN 010;