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- B6454c26f79b4c1bf9d109529b940efd7 NCIT_P378 "NCI" @default.
- B6454c26f79b4c1bf9d109529b940efd7 type Axiom @default.
- B6454c26f79b4c1bf9d109529b940efd7 annotatedProperty IAO_0000115 @default.
- B6454c26f79b4c1bf9d109529b940efd7 annotatedSource NCIT_C180865 @default.
- B6454c26f79b4c1bf9d109529b940efd7 annotatedTarget "A conjugate composed of a pH low insertion peptide (pHLIP) linked to the camptothecin analog exatecan, with potential antineoplastic activity. Upon administration of pHLIP-exatecan conjugate CBX-12, the pHLIP moiety specifically targets and gets inserted into the cellular membrane of tumor cells in environments with low extracellular pH. Then the exatecan moiety is released intracellularly via glutathione reduction of the linker. Exatecan inhibits DNA topoisomerase I activity, thereby inhibiting DNA replication and resulting in cell cycle arrest and tumor cell apoptosis. Tumor cell environments are more acidic than normal, healthy tissue environments. The pHLIP forms an alpha helix and becomes inserted across the cell membrane specifically at the low extracellular pH found within tumors." @default.