Protein / target
Discoidin domain-containing receptor 2
Protein at a glance
Biological role
Transmembrane receptor protein tyrosine kinase activity
Primary system
Musculoskeletal system
Strongest disease association
spondyloepimetaphyseal dysplasia-short limb-abnormal calcification syndrome
Therapeutic maturity
Clinically validated target
Druggability
Small molecule
Clinical development
1 approved
Derived from structured UniProt, Open Targets and literature data on this page.
Protein profile
Canonical identity and biological annotation from UniProt.
Function
Tyrosine kinase involved in the regulation of tissues remodeling (PubMed:30449416). It functions as a cell surface receptor for fibrillar collagen and regulates cell differentiation, remodeling of the extracellular matrix, cell migration and cell proliferation. Required for normal bone development. Regulates osteoblast differentiation and chondrocyte maturation via a signaling pathway that involves MAP kinases and leads to the activation of the transcription factor RUNX2. Regulates remodeling of the extracellular matrix by up-regulation of the collagenases MMP1, MMP2 and MMP13, and thereby facilitates cell migration and tumor cell invasion. Promotes fibroblast migration and proliferation, and thereby contributes to cutaneous wound healing
Subcellular location
Domains and Gene Ontology detail (45)Hide
Domains & features
Gene Ontology
- Capical plasma membrane
- Cfocal adhesion
- Cplasma membrane
- Creceptor complex
- FATP binding
- Fcollagen binding
- Fprotein tyrosine kinase collagen receptor activity
- Ftransmembrane receptor protein tyrosine kinase activity
- Pbiomineral tissue development
- Pcell adhesion
- Pcell surface receptor protein tyrosine kinase signaling pathway
- Pcellular response to angiotensin
Biological roles
What this protein does, drawn together from its UniProt function, Gene Ontology terms and Reactome pathways.
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Cell adhesion
- ·Tyrosine kinase involved in the regulation of tissues remodeling (PubMed:30449416). It f…
- ·cell adhesion
- ·positive regulation of extracellular matrix disassembly
- ·regulation of extracellular matrix disassembly
Kinase signalling
- ·transmembrane receptor protein tyrosine kinase activity
- ·peptidyl-tyrosine phosphorylation
- ·positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction
- ·positive regulation of protein kinase activity
Apoptosis & cell death
- ·negative regulation of apoptotic process
- ·negative regulation of hydrogen peroxide-mediated programmed cell death
Transcriptional regulation
- ·Tyrosine kinase involved in the regulation of tissues remodeling (PubMed:30449416). It f…
View underlying pathways (1)Hide underlying pathways
Concepts derived from UniProt GO Reactome — each badge above shows which sources supported that role.
Interaction neighbourhood
Proteins with the strongest functional or physical association. Node size and line weight reflect STRING confidence; hover or select a partner to inspect one association.
Functional and physical associations from STRING v12.0. Only associations with this protein are drawn — partner-to-partner links are not part of this evidence.
Drugs targeting this protein
Whether each drug engages this protein directly or through a complex, and how many other targets are recorded for it. Direct binders with few recorded targets are listed first.
Discoidin domain-containing receptor 2 inhibitor
Appears in clinical studies involving colorectal cancer, metastatic colorectal cancer, colorectal neoplasm, neoplasm
ChEMBL mechanism, action type and target identity. Open Targets clinical status and indications.
Translational evidence
Why this target matters therapeutically — disease associations, drugs in development, tractability and safety, from Open Targets.
Strongest genetic associations
Human genetic evidence — the most direct causal link between this target and a disease.
Highest-confidence therapeutic associations
Diseases where a drug acting on this target has already reached clinical development.
Show all associationsHide all associations
Open Targets ranks 1,017 associations for this target and we store the top 10 by aggregated score. The long tail is largely literature co-mention and RNA-expression evidence, not evidence that this target drives those diseases.
Known drugs · 1 total
colorectal cancer · metastatic colorectal cancer · colorectal neoplasm
Tractability
Clinical trials
Trials of drugs that target this protein — reached indirectly through those drugs, so a trial listed here studies the drug, not the protein.
Show remaining trials (24)Hide
ClinicalTrials.gov via the drug-target graph.
Forefront confidence
Our own weighting of the evidence behind each disease association. Human genetics and clinical evidence count for most; literature co-mention counts for little, because two entities sharing an abstract is not evidence that one drives the other.
The evidence agreement range shows how closely the independent evidence families agree — it is not a statistical confidence interval, and nothing here is fitted to outcome data. Derived from Open Targets evidence types under Forefront weighting; the underlying per-type scores are shown above so the calculation can be checked.
What's happening now
Recent activity around this target, drawn from one canonical event stream. Every item is reached through a drug that targets this protein, so each event is news about that drug rather than about the protein directly.
- New publicationEfficacy of pembrolizumab in microsatellite-stable, tumor mutational burden-high metastatic colorectal cancer: genomic signatures and clinical outcomes.
- New publicationLenvatinib Plus Pembrolizumab Versus Standard of Care for Previously Treated Metastatic Colorectal Cancer: Final Analysis of the Randomized, Open-Label, Phase III LEAP-017 Study.
- New publicationTargeted therapy for hepatocellular carcinoma.
- New publicationMolecular targeted and immune checkpoint therapy for advanced hepatocellular carcinoma.
- New publicationRandomized Double-Blind Phase II Study of Regorafenib in Patients With Metastatic Osteosarcoma.
- New publicationRegorafenib for patients with hepatocellular carcinoma who progressed on sorafenib treatment (RESORCE): a randomised, double-blind, placebo-controlled, phase 3 trial.
- Regulatory approval
Approval: Stivarga (EMA)
Objective event titles are shown unmodified; the event kind and significance line are derived from structured fields. Forefront AttentionEvent stream aggregating Europe PMC Regulatory filings ClinicalTrials.gov.