GART (trifunctional purine synthesis enzyme)
GART is one of the enzymes that builds purines from scratch; pemetrexed blocks it alongside thymidylate synthase, which is why the drug starves fast-growing lung and mesothelioma cells.
Overview
The trifunctional protein GART carries three activities of de novo purine synthesis, including glycinamide ribonucleotide formyltransferase, a folate-dependent step. Pemetrexed, once polyglutamated inside cells, inhibits thymidylate synthase most strongly but also GART and dihydrofolate reductase, giving it a multi-targeted antifolate action in non-small cell lung cancer and mesothelioma.
- Target · the protein and the cell it sits on
- Drug · antibody, small molecule, cell or radioligand
- Effect · signal, damage or kill
In plain words · GART is one of the enzymes that builds purines from scratch; pemetrexed blocks it alongside thymidylate synthase, which is why the drug starves fast-growing lung and mesothelioma cells.
- 1 · What it is
GART is one of the enzymes that builds purines from scratch; pemetrexed blocks it alongside thymidylate synthase, which is why the drug starves fast-growing lung and mesothelioma cells.
- 2 · What goes wrong in cancer
A cytosolic enzyme of the purine pathway whose activity rises with proliferation; inhibition depletes purine nucleotides needed for DNA and RNA.
- 3 · How drugs use it
No product in this corpus aims at GART (trifunctional purine synthesis enzyme) yet. Inhibitors are shaped to fit the enzyme's active site so the reaction the cancer relies on stops.
External identifiers
Biology
A cytosolic enzyme of the purine pathway whose activity rises with proliferation; inhibition depletes purine nucleotides needed for DNA and RNA.
- Proliferating cells generally
- Lung adenocarcinoma and mesothelioma treated with pemetrexed
Latest papers
topQuery for this target: (TITLE:"GART" OR ABSTRACT:"GART" OR TITLE:"trifunctional purine synthesis enzyme" OR ABSTRACT:"trifunctional purine synthesis enzyme") 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 GART (trifunctional purine synthesis enzyme), not a curated reading list.
Similar pages
not linked directly; found by shared links- TreatmentLeucovorin (folinic acid)
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- CompanyOrion, Orion Pharma
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