Preferred Label : Karonudib;
NCIt synonyms : Karolinska NUDT1 Inhibitor TH1579; Karolinska MTH1 Inhibitor TH1579;
NCIt definition : An orally available inhibitor of Karolinska nudt1 (MTH1; MutT homologue 1; NUDT1),
with potential antineoplastic activity. Upon administration, karonudib targets and
binds to the active site of MTH1, thereby preventing the activity of MTH1. This leads
to the incorporation of oxidized deoxynucleoside triphosphates (dNTPs) into the DNA
of cancer cells, which causes DNA damage, introduces double strand breaks (DSBs),
and induces apoptosis in cancer cells. MTH1, a member of the Nudix phosphohydrolase
superfamily hydrolyzes oxidized purine nucleoside triphosphates, including 8-oxo-dGTP
and 2-OH-dATP, converts them into their corresponding monophosphate forms, and prevents
their incorporation into DNA, which allows MTH1-expressing cells to evade cell death.
Compared to normal, healthy cells, cancer cells overexpress MTH1, which leads to dysregulation
of the cellular redox system and increased reactive oxygen species (ROS) production,
which together prevents the incorporation of damaged and oxidized nucleotides into
DNA.;
Molecule name : TH1579;
NCI Metathesaurus CUI : CL550808;
Origin ID : C148140;
UMLS CUI : C4724843;
Currated CISMeF NLP mapping
- Semantic type(s)
- UMLS correspondences (same concept)
- concept_is_in_subset
