Preferred Label : Nimesulide-Hyaluronic Acid Conjugate CA102N;
NCIt synonyms : Nim-HA Conjugate; Hyaluronic Acid Nimesulide-NH2 Bioconjugate; HA-Nim Conjugate CA102N; HA-Nimesulide;
NCIt definition : A covalently bound conjugate composed of the biological polymer sodium hyaluronate
(NaHA) and the hydrophobic, cyclooxygenase 2 (COX-2) inhibitor and cytotoxic agent
nimesulide (Nim), with potential antineoplastic activity. Upon intravenous administration
of Nim-HA conjugate CA102N, the HA moiety targets and binds to CD44. Following endocytosis
of CA102N and enzymatic degradation within the lysosomal compartment, Nim is released
inside CD44-expressing tumor cells, causing Nim-mediated induction of cell cycle arrest
tumor cell apoptosis and decreases tumor cell growth. In addition, Nim inhibits various
tumor cell signaling pathways thereby further inhibiting tumor cell proliferation.
CD44, a transmembrane glycoprotein and HA receptor expressed in healthy tissue, plays
a key role in cellular growth, survival, differentiation and motility. Overexpressed
in a variety of cancer cell types, CD44 plays a key role in tumor cell proliferation,
migration and survival. Conjugation of HA to Nim allows for increased solubility of
Nim and for targeted delivery of Nim to CD44-expressing tumor cells, thereby increasing
efficacy and safety of Nim.;
Molecule name : CA-102N; CA 102N;
NCI Metathesaurus CUI : CL936840;
Origin ID : C157231;
UMLS CUI : C4763495;
Semantic type(s)
- concept_is_in_subset
- has_target
