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

AttributesValues
rdf:type
rdfs:label
  • Lucanthone
rdfs:subClassOf
Has_Salt_Form
Concept_In_Subset
Semantic_Type
  • Pharmacologic Substance
Preferred_Name
  • Lucanthone
UMLS_CUI
  • C0024071
CAS_Registry
  • 479-50-5
FDA_UNII_Code
  • FC6D57000M
Contributing_Source
  • FDA
PDQ_Open_Trial_Search_ID
  • 733411
PDQ_Closed_Trial_Search_ID
  • 733411
Chemical_Formula
  • C20H24N2OS
CHEBI_ID
  • CHEBI:51052
FULL_SYN
  • LUCANTHONEPTFDAFC6D57000M
  • LucanthonePTNCI
DEFINITION
  • An orally available thioxanthone-based DNA intercalator and inhibitor of the DNA repair enzyme apurinic-apyrimidinic endonuclease 1 (APEX1 or APE1), with anti-schistosomal and potential antineoplastic activity. Lucanthone intercalates DNA and interferes with the activity of topoisomerases I and II during replication and transcription, thereby inhibiting the synthesis of macromolecules. In addition, this agent specifically inhibits the endonuclease activity of APE1, without affecting its redox activity, resulting in un-repaired DNA strand breaks which may induce apoptosis. Therefore, lucanthone may sensitize tumor cells to radiation and chemotherapy. Furthermore, lucanthone inhibits autophagy through the disruption of lysosomal function. The multifunctional nuclease APE1 is a key component for DNA repair; its expression is often correlated with tumor cell resistance to radio- and chemotherapy.NCI
code
  • C83925
sameAs
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