Preferred Label : DHODH Inhibitor JBZ-001;
NCIt synonyms : Dihydroorotate Dehydrogenase Inhibitor JBZ-001;
NCIt definition : An orally available inhibitor of dihydroorotate dehydrogenase (DHODH), with potential
antineoplastic, activity. Upon oral administration, DHODH inhibitor JBZ-001 specifically
targets, binds to and prevents the activation of DHODH, thereby preventing the fourth
enzymatic step in de novo pyrimidine synthesis. This causes metabolic stress and prevents
uridine monophosphate (UMP) formation, DNA synthesis, cell division and cellular proliferation,
promotes cell differentiation, causes cell cycle arrest and induces apoptosis in susceptible
tumor cells. Specifically, JBZ-001 induces the differentiation of immature myeloid
cells and driving them toward a more mature, functional state as seen in morphological
changes in acute myeloid leukemia (AML) cells. In addition, JBZ-001 induces the upregulation
of CD38 and CD47 on susceptible cancer cells, thereby improving efficacy of CD38-
and CD47-targeted therapies. DHODH, a mitochondrial enzyme, catalyzes the conversion
of dihydroorotate (DHO) to orotate in the endogenous synthesis of UMP.;
Molecule name : JBZ-001; JBZ 001; HOSU-53;
Origin ID : C213785;
concept_is_in_subset
- has_target
