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DHODH is an enzyme cells need to make pyrimidines, the building blocks of DNA and RNA. Blocking it pushed immature leukaemia cells to mature in mouse studies, and a DHODH inhibitor is in an early trial in solid tumours and lymphoma.
DHODH (chromosome 16q22.2) converts dihydroorotate to orotate, a step required for the cell's own (de novo) synthesis of UMP and so of pyrimidine nucleotides (UniProt Q02127). A 2016 Cell study screening for compounds that overcome the differentiation block of acute myeloid leukaemia found that inhibiting DHODH let leukaemia cells mature in human and mouse models, and that DHODH inhibitors reduced leukaemic burden and leukaemia-initiating cells and improved survival in mice (Sykes et al., doi:10.1016/j.cell.2016.08.057). In OnCo, JBZ-001 is an oral DHODH inhibitor in a phase 1 trial in advanced solid tumours and non-Hodgkin lymphoma.
In plain words · DHODH is an enzyme cells need to make pyrimidines, the building blocks of DNA and RNA. Blocking it pushed immature leukaemia cells to mature in mouse studies, and a DHODH inhibitor is in an early trial in solid tumours and lymphoma.
DHODH is an enzyme cells need to make pyrimidines, the building blocks of DNA and RNA. Blocking it pushed immature leukaemia cells to mature in mouse studies, and a DHODH inhibitor is in an early trial in solid tumours and lymphoma.
Enzyme that uses a quinone as electron acceptor to make orotate, required for UMP biosynthesis by the de novo pathway (UniProt Q02127).
1 product aims at DHODH: small molecules. Inhibitors are shaped to fit the enzyme's active site so the reaction the cancer relies on stops.
Enzyme that uses a quinone as electron acceptor to make orotate, required for UMP biosynthesis by the de novo pathway (UniProt Q02127).
JBZ-001 is an experimental oral small-molecule inhibitor from Jabez Biosciences, in phase 1 trials for advanced solid tumours and non-Hodgkin lymphoma.
Query for this target: (TITLE:"DHODH" OR ABSTRACT:"DHODH" OR TITLE:"dihydroorotate dehydrogenase" OR ABSTRACT:"dihydroorotate dehydrogenase") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about DHODH, not a curated reading list.
Shares Acute myeloid leukaemia and the tag pipeline-gap-target.
Shares Acute myeloid leukaemia and the tag pipeline-gap-target.
Shares Acute myeloid leukaemia and the tag pipeline-gap-target.
Shares JBZ-001, Non-Hodgkin lymphoma (all types).
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