Preferred Label : Paclitaxel-conjugated CXCR4 Peptide Antagonist MB1707;
NCIt synonyms : Peptide-drug Conjugate MB1707; PDC MB1707; Paclitaxel-conjugated CXC Chemokine Receptor 4 Antagonist MB1707;
NCIt definition : A peptide-drug conjugate (PDC) of paclitaxel with an inhibitor of CXC chemokine receptor
4 (CXCR4), with potential antineoplastic activity. Upon administration of paclitaxel-conjugated
CXCR4 peptide antagonist MB1707, the CXCR4 inhibitor moiety binds to the chemokine
receptor CXCR4 expressed on tumor cells, thereby preventing CXCR4 binding to its ligand,
stromal derived factor-1 (SDF-1), and subsequent receptor activation. This may result
in decreased tumor cell proliferation and migration. In addition, paclitaxel binds
to tubulin inside CXCR4-expressing tumor cells and inhibits the disassembly-assembly
dynamics of microtubules, resulting in cell cycle arrest and cell death. CXCR4, a
chemokine receptor belonging to the G protein-coupled receptor (GPCR) gene family,
plays an important role in chemotaxis and angiogenesis and is upregulated in several
tumor cell types. By targeting CXCR4-expressing tumor cells specifically, paclitaxel's
efficacy is increased while minimizing systemic toxiciy.;
Molecule name : MB-1707;
NCI Metathesaurus CUI : CL1798596;
Origin ID : C189826;
UMLS CUI : C5706558;
Semantic type(s)
- chemical_or_drug_has_mechanism_of_action
- concept_is_in_subset
- has_target
