Preferred Label : pH Low Insertion Peptide-exatecan Conjugate CBX-12;
NCIt synonyms : pHLIP-exatecan Conjugate CBX-12; Low pH Targeting Alphalex-exatecan Conjugate CBX-12; Alphalex Conjugate CBX-12; Alphalex-exatecan Conjugate CBX-12;
NCIt definition : 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.;
Molecule name : CBX-12; CBX 12;
NCI Metathesaurus CUI : CL1663446;
Origin ID : C180865;
UMLS CUI : C5556674;
Semantic type(s)
- concept_is_in_subset
- has_target
