CD39 (ENTPD1)
CD39 is the first of two enzymes that turn the ATP spilt by dying tumour cells into adenosine, which sedates T cells. Blocking it keeps the ATP alarm ringing; one antibody has completed phase 2 in pancreatic cancer.
Overview
ENTPD1 (chromosome 10q24.1) catalyses the hydrolysis of nucleoside triphosphates and diphosphates, sequentially removing phosphate groups to leave nucleoside monophosphates; it is expressed primarily on activated lymphoid cells and in endothelium, and highly in placenta, lung, skeletal muscle and kidney (UniProt P49961). CD39 and CD73 together catabolise extracellular ATP into adenosine, and both, with adenosine receptors, have emerged as therapeutic targets (Allard et al. 2019, Immunol Rev). TTX-030, an anti-CD39 antibody, completed a phase 2 study with chemotherapy, with or without budigalimab, in first-line metastatic pancreatic cancer (NCT06119217).
- Target · the protein and the cell it sits on
- Drug · antibody, small molecule, cell or radioligand
- Effect · signal, damage or kill
In plain words · CD39 is the first of two enzymes that turn the ATP spilt by dying tumour cells into adenosine, which sedates T cells. Blocking it keeps the ATP alarm ringing; one antibody has completed phase 2 in pancreatic cancer.
- 1 · What it is
CD39 is the first of two enzymes that turn the ATP spilt by dying tumour cells into adenosine, which sedates T cells. Blocking it keeps the ATP alarm ringing; one antibody has completed phase 2 in pancreatic cancer.
- 2 · What goes wrong in cancer
The upstream ectonucleotidase of the adenosine axis; CD73 (NT5E) finishes the conversion.
- 3 · How drugs use it
No product in this corpus aims at CD39 (ENTPD1) yet. Inhibitors are shaped to fit the enzyme's active site so the reaction the cancer relies on stops.
External identifiers
Sources: HGNC HGNC:3363 (approved symbol, name, aliases and cross-references); UniProt P49961 (protein name, function and tissue specificity)
Biology
The upstream ectonucleotidase of the adenosine axis; CD73 (NT5E) finishes the conversion.
- Activated lymphoid cells, endothelium (UniProt P49961)
- Pancreatic cancer trial of TTX-030 (NCT06119217)
Notes
top- Prevalence not recorded: HGNC and UniProt carry no positivity rates.
Latest papers
topQuery for this target: (TITLE:"CD39" OR ABSTRACT:"CD39" OR TITLE:"ENTPD1" OR ABSTRACT:"ENTPD1" OR TITLE:"NTPDase-1" OR ABSTRACT:"NTPDase-1" OR TITLE:"ectonucleoside triphosphate diphosphohydrolase 1" OR ABSTRACT:"ectonucleoside triphosphate diphosphohydrolase 1") 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 CD39 (ENTPD1), not a curated reading list.
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