About: BET Inhibitor GSK525762     Goto   Sponge   NotDistinct   Permalink

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AttributesValues
rdf:type
rdfs:label
  • BET Inhibitor GSK525762
rdfs:subClassOf
Semantic_Type
  • Pharmacologic Substance
Preferred_Name
  • BET Inhibitor GSK525762
NCI_META_CUI
  • CL435787
PDQ_Open_Trial_Search_ID
  • 733416
PDQ_Closed_Trial_Search_ID
  • 733416
FULL_SYN
  • BET Inhibitor GSK525762PTNCI
  • GSK525762CNNCI
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 GSK525762 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 may lead to an inhibition of tumor cell growth. Characterized by a tandem repeat of bromodomain at the N-terminus, BET proteins, comprising of BRD2, BRD3, BRD4 and BRDT, are transcriptional regulators that play an important role during development and cellular growth.NCI
code
  • C101538
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