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- NCIT_C90554 IAO_0000115 "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, mipsagargin 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. Mipsagargin 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." @default.
- NCIT_C90554 NCIT_A32 NCIT_C1909 @default.
- NCIT_C90554 NCIT_A7 NCIT_C17796 @default.
- NCIT_C90554 NCIT_NHC0 "C90554" @default.
- NCIT_C90554 NCIT_P106 "Pharmacologic Substance" @default.
- NCIT_C90554 NCIT_P107 "Mipsagargin" @default.
- NCIT_C90554 NCIT_P108 "Mipsagargin" @default.
- NCIT_C90554 NCIT_P208 "CL416238" @default.
- NCIT_C90554 NCIT_P210 "1245732-48-2" @default.
- NCIT_C90554 NCIT_P319 "Q032I35QMX" @default.
- NCIT_C90554 NCIT_P322 "CTRP" @default.
- NCIT_C90554 NCIT_P322 "FDA" @default.
- NCIT_C90554 NCIT_P322 "GDC" @default.
- NCIT_C90554 NCIT_P329 "666090" @default.
- NCIT_C90554 NCIT_P330 "666090" @default.
- NCIT_C90554 NCIT_P375 "Mipsagargin" @default.
- NCIT_C90554 NCIT_P399 "666090" @default.
- NCIT_C90554 normalizedInformationContent "100" @default.
- NCIT_C90554 referenceCount "1" @default.
- NCIT_C90554 hasExactSynonym "G-202" @default.
- NCIT_C90554 hasExactSynonym "MIPSAGARGIN" @default.
- NCIT_C90554 hasExactSynonym "Mipsagargin" @default.
- NCIT_C90554 inSubset NCIT_C116977 @default.
- NCIT_C90554 inSubset NCIT_C116978 @default.
- NCIT_C90554 inSubset NCIT_C128784 @default.
- NCIT_C90554 inSubset NCIT_C157711 @default.
- NCIT_C90554 inSubset NCIT_C157712 @default.
- NCIT_C90554 inSubset NCIT_C176424 @default.
- NCIT_C90554 inSubset NCIT_C177537 @default.
- NCIT_C90554 inSubset NCIT_C63923 @default.
- NCIT_C90554 type Class @default.
- NCIT_C90554 isDefinedBy ncit.owl @default.
- NCIT_C90554 label "Mipsagargin" @default.
- NCIT_C90554 subClassOf NCIT_C163758 @default.
- NCIT_C90554 subClassOf NCIT_C176017 @default.
- NCIT_C90554 subClassOf NCIT_C1908 @default.
- NCIT_C90554 subClassOf NCIT_C1909 @default.
- NCIT_C90554 subClassOf NCIT_C274 @default.
- NCIT_C90554 subClassOf NCIT_C90554 @default.