About: Ruthenium-based Transferrin Targeting Agent NKP-1339     Goto   Sponge   NotDistinct   Permalink

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AttributesValues
rdf:type
rdfs:label
  • Ruthenium-based Transferrin Targeting Agent NKP-1339
rdfs:subClassOf
Semantic_Type
  • Pharmacologic Substance
Preferred_Name
  • Ruthenium-based Transferrin Targeting Agent NKP-1339
NCI_META_CUI
  • CL430556
PDQ_Open_Trial_Search_ID
  • 709242
PDQ_Closed_Trial_Search_ID
  • 709242
FULL_SYN
  • Ruthenium-based Transferrin Targeting Agent NKP-1339PTNCI
  • NKP-1339CNNCI
DEFINITION
  • A ruthenium-containing cancer agent targeting transferrin with potential antineoplastic activity. Upon intravenous administration, NKP-1339 (Ru3+) binds to transferrin (Tf) and is taken up via Tf receptors (TfR), which are overexpressed on cancer cells. Once inside the cell, NKP-1339 is released from Tf and is reduced, within the acidic environment of the endosomes, to its active form NKP-119 (Ru2+). In turn, the active form induces a redox reaction, thereby leading to the formation of reactive oxygen species (ROS) which inhibits GRP78 and SOD, endoplasmic reticulum-stress modulating molecules as well as BAG4 and ERK, program cell death regulating molecules. This eventually induces caspase-dependent apoptosis.NCI
code
  • C97948
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