Preferred Label : ENPP1 Inhibitor SR-8541A;
NCIt definition : An orally bioavailable selective small molecule inhibitor of ectonucleotide pyrophosphatase/phosphodiesterase
1 (ENPP1), with potential immunomodulating and antineoplastic activities. Upon oral
administration, ENPP1 inhibitor SR-8541A selectivelly targets and binds to ENPP1,
thereby inhibiting the activity of ENPP1. This inhibits ENPP1-mediated 2'-3'-cyclic
guanosine monophosphate-adenosine monophosphate (cGAMP) and adenosine triphosphate
(ATP) hydrolysis and stabilizes extracellular endogenous cGAMP and ATP. This leads
to the extracellular accumulation of cGAMP and ATP, and inhibits the production and
accumulation of immunosuppressive adenosine in the tumor microenvironment (TME). This
allows for the activation of stimulator of interferon genes (STING), and the induction
of anticancer immune responses. ENPP1, overexpressed in a number of tumor types, mediates
nucleotide recycling by breaking down ATP to AMP, which is then converted to adenosine.
It suppresses anti-tumor immune responses and increases metastasis.;
Molecule name : SR 8541A; SR-8541A;
NCI Metathesaurus CUI : CL1921227;
Origin ID : C202239;
UMLS CUI : C5907960;
Semantic type(s)
- concept_is_in_subset
- has_target
