About: Thapsigargin Prodrug G-202     Goto   Sponge   NotDistinct   Permalink

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AttributesValues
rdf:type
rdfs:label
  • Thapsigargin Prodrug G-202
rdfs:subClassOf
Semantic_Type
  • Pharmacologic Substance
Preferred_Name
  • Thapsigargin Prodrug G-202
NCI_META_CUI
  • CL416238
PDQ_Open_Trial_Search_ID
  • 666090
PDQ_Closed_Trial_Search_ID
  • 666090
FULL_SYN
  • Thapsigargin Prodrug G-202PTNCI
  • G-202CNNCI
DEFINITION
  • A soluble, thapsigargin prodrug containing the cytotoxic analog of thapsigargin, 8-O-(12Aminododecanoyl)-8-O debutanoylthapsigargin (12-ADT) linked, via a carboxyl group, to the targeting peptide containing aspartic acid with potential antineoplastic activity. Upon intravenous administration, the non-toxic prodrug targets prostate specific membrane antigen (PSMA), a type II membrane carboxypeptidase, which is overexpressed in prostate cancer cells and in the neovasculature of most solid tumors but not in normal blood vessels. G-202 is subsequently converted, through hydrolysis, into the active cytotoxic analog of thapsigargin 12-ADT-Asp. 12-ADT binds to and blocks the Sarcoplasmic/Endoplasmic Reticulum Calcium ATPase (SERCA) pump, thereby increasing the concentration of cytosolic calcium which leads to an induction of apoptosis. By preventing nutrient supply to tumor cells, G-202 may be able to inhibit tumor growth. Compared to thapsigargin alone, thapsigargin prodrug G-202 is able to achieve higher concentrations of the active agents at the tumor site while avoiding systemic toxicity.NCI
code
  • C90554
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