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- Bce8bfb0608534b0ce02082e2dfc8f77c NCIT_P378 "NCI" @default.
- Bce8bfb0608534b0ce02082e2dfc8f77c type Axiom @default.
- Bce8bfb0608534b0ce02082e2dfc8f77c annotatedProperty IAO_0000115 @default.
- Bce8bfb0608534b0ce02082e2dfc8f77c annotatedSource NCIT_C180865 @default.
- Bce8bfb0608534b0ce02082e2dfc8f77c 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.