About: Sam68 Modulator CWP232291     Goto   Sponge   NotDistinct   Permalink

An Entity of Type : owl:Class, within Data Space : linked.opendata.cz:8890 associated with source document(s)

AttributesValues
rdf:type
rdfs:label
  • Sam68 Modulator CWP232291
rdfs:subClassOf
Semantic_Type
  • Pharmacologic Substance
Preferred_Name
  • Sam68 Modulator CWP232291
NCI_META_CUI
  • CL430318
PDQ_Open_Trial_Search_ID
  • 706549
PDQ_Closed_Trial_Search_ID
  • 706549
FULL_SYN
  • Sam68 Modulator CWP232291PTNCI
  • CWP232291CNNCI
DEFINITION
  • A small molecule and prodrug of CWP232204 targeting Src associated in mitosis, of 68 kDa (Sam68 or KHDRBS1), with potential antineoplastic activity. CWP232291 is converted in serum into its active form CWP232204 which binds to Sam68, thereby resulting in the induction of apoptosis in selective cancer cells. Due to the multimodular structure of Sam68, the apoptosis mediated by CWP232204-Sam68 interaction can attribute from 1) activation of transcription factor NF-kB induced by tumor necrosis factor alpha signaling, 2) alternative splicing of BCL-2 apoptosis gene, driving the balance towards pro-apoptotic as opposed to anti-apoptotic isoforms, 3) down-regulation of the anti-apoptotic protein survivin via Wnt signaling. Sam68, a KH domain RNA-binding protein belonging to the signal transduction and activation of RNA (STAR) family, plays a key role in various cellular processes including cell cycle progression and apoptosis; it is upregulated in many types of cancer cells and its expression is associated with increased cell proliferation and survival.NCI
code
  • C97663
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