Preferred Label : Subasumstat;
NCIt definition : A small molecule inhibitor of sumoylation, with potential immune-activating and antineoplastic
activities. Upon intravenous administration, subasumstat targets and covalently binds
to the small ubiquitin-like modifier (SUMO; small ubiquitin-related modifier) protein,
forming an adduct with SUMO protein (subasumstat-SUMO adduct). This prevents the transfer
of SUMO from the SUMO-activating enzyme (SAE) to SUMO-conjugating enzyme UBC9. This
prevents SUMO conjugation to lysine residues on target proteins and abrogates many
sumoylated protein-mediated cellular processes that play key roles in tumor cells,
including proliferation, DNA repair, metastasis and survival. In addition, by preventing
sumoylation, subasumstat is able to increase the production of type 1 interferon (IFN),
thereby increasing type 1 IFN-mediated signaling, activating innate effector cells
and enhancing the antitumor innate immune responses. This may further increase tumor
cell killing. Sumoylation, a post-translational modification that attaches the SUMO
protein to target proteins, plays a key role in regulating their activity, function,
subcellular localization and stability. Sumoylation also plays a key role in inhibiting
innate immune responses, specifically by inhibiting the pattern recognition receptor
(PRR) pathway and preventing type 1 IFN expression. Abnormal sumoylation of target
proteins is associated with many cancers.;
UNII : XQ43H3V6M1;
InChIKey : LXRZVMYMQHNYJB-UNXOBOICSA-N;
CAS number : 1858276-04-6;
Molecule name : TAK-981; TAK 981;
NCI Metathesaurus CUI : CL562995;
Origin ID : C156270;
UMLS CUI : C5432271;
Semantic type(s)
- concept_is_in_subset
