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DDR2 is a receptor that senses collagen; mutations in it occur in a small share of squamous lung cancers, and dasatinib inhibits it.
Discoidin domain receptor 2 is a receptor tyrosine kinase activated by fibrillar collagen rather than by a growth factor. DDR2 mutations were found in around 4 percent of squamous non-small cell lung cancers, and the leukaemia drug dasatinib inhibits DDR2 strongly, which prompted trials in DDR2-mutant lung cancer; responses were seen but the approach did not reach approval.
In plain words · DDR2 is a receptor that senses collagen; mutations in it occur in a small share of squamous lung cancers, and dasatinib inhibits it.
DDR2 is a receptor that senses collagen; mutations in it occur in a small share of squamous lung cancers, and dasatinib inhibits it.
Collagen binding through the discoidin domain triggers slow, sustained kinase activation, regulating cell adhesion, migration and matrix remodelling.
1 product aims at DDR2 receptor kinase: small molecules. Kinases are switched on by binding ATP inside the cell, so most drugs are small molecules shaped to plug that ATP pocket.
Broadly expressed or essential: HPA finds the RNA at low tissue specificity; the 1 medicine aimed at it (Dasatinib) act on the wild-type protein, so normal tissue is exposed and the therapeutic window comes from the tumour's faster division or its dependence on the protein. HPA DDR2: RNA low tissue specificity; no normal tissue stained high. Distribution: 1 cancer family in the corpus carries a prevalence row, label threshold or catalogue link for it (Lung cancer (all types)); Open Targets associates it with 1 specific cancer type at or above 0.5 (colorectal cancer). (Rule 7 of scripts/fetch-target-specificity.ts.)
Sources: Human Protein Atlas DDR2 tissue; Open Targets ENSG00000162733 associations
First described 1993. Earliest sequence paper UniProt cites for the protein: Karn et al, Oncogene, 1993, "Structure, expression and chromosomal mapping of TKT from man and mouse: a new subclass of receptor tyrosine kinases with a factor VIII-like domain". Source.
Collagen binding through the discoidin domain triggers slow, sustained kinase activation, regulating cell adhesion, migration and matrix remodelling.
RNA: low tissue specificity, detected in many normal tissues.
No normal tissue stained high.
No cancer sample stained medium or high.
HPA DDR2 tissue · HPA DDR2 pathology · HPA protein class: CD markers, FDA approved drug targets
Human Protein Atlas version 25.1, antibody staining at reliability approved, enhanced or supported; used under CC BY-SA 3.0. Staining counts are patients per level in the atlas cohort, not population prevalence.
| Cancer | Prevalence | Measure | Note | Source |
|---|---|---|---|---|
| Non-small-cell lung cancer | 3.8% | DDR2 kinase mutation, Sanger sequencing of squamous cell lung cancers and cell lines | Squamous histology only; mutant cell lines and one patient responded to dasatinib | doi.org |
Approximate, population-level figures; the measure column says what was counted. Ranges show the midpoint as a bar.
Dasatinib is a second-generation BCR::ABL1 pill that, combined with the immunotherapy blinatumomab, can put Ph-positive ALL into deep remission with no chemotherapy at all.
Query for this target: (TITLE:"DDR2 receptor kinase" OR ABSTRACT:"DDR2 receptor kinase" OR TITLE:"DDR2" OR ABSTRACT:"DDR2") 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 DDR2 receptor kinase, not a curated reading list.