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Protein / target

Discoidin domain-containing receptor 2

Encoded byDDR2Q16832Homo sapiensSwiss-Prot
Clinically validated
Therapeutic maturity
1
Approved medicines
Open Targets target-level
View by indication →
30
Clinical trials
Small-molecule tractable
Druggability
Approved Drug

Protein at a glance

Biological role

Transmembrane receptor protein tyrosine kinase

Strongest disease association

Spondyloepimetaphyseal dysplasia-short limb-abnormal calcification syndrome

Via encoding gene DDR2 · Genetic evidence · score 0.86

Therapeutic position

Established drug target

Small molecules

Derived from structured UniProt, Open Targets and literature data on this page.

Protein profile

UniProt 2026_02

Canonical identity and biological annotation from UniProt.

Function overview

Tyrosine kinase involved in the regulation of tissues remodeling.

View complete UniProt function annotation

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

Cell membrane
Domains and Gene Ontology detail (45)

Domains & features

F5/8 type CProtein kinase

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

855 aa · 97 kDa

Biological roles

Reactome v97

What this protein does, drawn together from its UniProt function, Gene Ontology terms and Reactome pathways.

Cell migrationUniProt · GOReceptor tyrosine kinase signallingGOCell-cycle regulationGOCell adhesionUniProt · GOApoptosis & cell deathGO
View supporting evidence

Cell migration

  • ·Tyrosine kinase involved in the regulation of tissues remodeling (PubMed:30449416). It f…
  • ·positive regulation of vascular associated smooth muscle cell migration

Receptor tyrosine kinase signalling

  • ·transmembrane receptor protein tyrosine kinase activity
  • ·cell surface receptor protein tyrosine kinase signaling pathway

Cell-cycle regulation

  • ·positive regulation of G1/S transition of mitotic cell cycle

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

Apoptosis & cell death

  • ·negative regulation of apoptotic process
  • ·negative regulation of hydrogen peroxide-mediated programmed cell death
View underlying pathways (1)

Concepts derived from UniProt GO Reactome — each badge above shows which sources supported that role.

Interaction neighbourhood

STRING v12.0

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.

COL1A1COL3A1COL11A1COL5A1ITGA2SHC1EML4COL4A1VWFDDR1DDR2

10 strongest partners — larger node and heavier line mean higher confidence

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.

Approved medicines with mapped indications

1 medicine · 2 areas

Approved therapies targeting this protein, grouped by what they are approved to treat — the disease-first view of the medicines below. Relationships come from the canonical approved-indication graph (ChEMBL phase-4), the same source as the drug cards.

Colorectal Neoplasms1 medicine
Broader indication categories (1)
Neoplasms1 medicine

Broad umbrella indications (e.g. “Neoplasms”). Shown here because every medicine also appears under a more specific disease above — kept for completeness, de-emphasised for clarity.

Approved indications from ChEMBL (phase-4), via the canonical drug→disease graph.

Drugs targeting this protein

1

How approved and investigational drugs engage this protein — mechanism and action type, direct vs complex targeting, and how broadly each acts across other targets. A drug-first view (the section above groups the approved ones disease-first); direct binders with few recorded targets are listed first.

regorafenib
ApprovedInhibitor

Discoidin domain-containing receptor 2 inhibitor

Indicated for Colorectal Neoplasms, Neoplasms

Direct interaction with this protein · 1 of 18 recorded protein targets — broad pharmacology

ChEMBL mechanism, action type, target identity and approved indications. Open Targets clinical status.

Translational evidence

Open Targets 26

Why this target matters therapeutically, strongest evidence first. Disease associations are gene-level (via the gene that encodes this protein) and open into the full confidence synthesis; the development universe, tractability and safety annotations are target-level, from Open Targets.

Strongest disease associations · via encoding gene DDR2

Gene-level evidence surfaced through the gene DDR2that encodes this protein — not a direct protein–disease relationship. Ranked by Forefront's causal-directness weighting, so genetically- and clinically-evidenced diseases lead over ones that merely share the literature.

Spondyloepimetaphyseal dysplasia-short limb-abnormal calcification syndrome
0.88Well supported

Genetic evidence dominant · Open Targets 0.78

Spondyloepimetaphyseal dysplasia - short limb - abnormal calcification
0.86Well supported

Genetic evidence dominant · Open Targets 0.75

Colorectal Neoplasms
0.72Moderately supported

Clinical evidence dominant · Open Targets 0.58

Dupuytren Contracture
0.70Moderately supported

Genetic evidence dominant · Open Targets 0.42

Warburg-Cinotti syndrome
0.66Moderately supported

Genetic evidence dominant · Open Targets 0.57

View evidence synthesis (5)
Spondyloepimetaphyseal dysplasia-short limb-abnormal calcification syndromeWell supported
0.88
agreement 0.761.00
Genetic86%Animal model14%Genetic literaturedup

Open Targets aggregate 0.78 · 2 independent evidence families · 1 not counted as duplicate

Spondyloepimetaphyseal dysplasia - short limb - abnormal calcificationWell supported
0.86
agreement 0.730.98
Genetic86%Animal model14%Genetic literaturedup

Open Targets aggregate 0.75 · 2 independent evidence families · 1 not counted as duplicate

Colorectal NeoplasmsModerately supported
0.72
agreement 0.580.85
Clinical93%RNA expression5%Literature3%

Open Targets aggregate 0.58 · 3 independent evidence families

Dupuytren ContractureModerately supported
0.70
agreement 0.580.82
Genetic100%

Open Targets aggregate 0.42 · 1 independent evidence family

Warburg-Cinotti syndromeModerately supported
0.66
agreement 0.520.80
Genetic97%Literature3%Genetic literaturedup

Open Targets aggregate 0.57 · 2 independent evidence families · 1 not counted as duplicate

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 per-type scores above show the calculation.

Show all associations
Spondyloepimetaphyseal dysplasia-short limb-abnormal calcification syndrome0.78
Spondyloepimetaphyseal dysplasia - short limb - abnormal calcification0.75
Colorectal Neoplasms0.58
Warburg-Cinotti syndrome0.57
Carcinoma, Hepatocellular0.45
Dupuytren Contracture0.42
Neoplasms0.41
Gastrointestinal Stromal Tumors0.41

Drug development

1 compounds recorded · 1 approved

Open Targets' development universe — every compound recorded against the target at any stage, not all approved medicines. Distinct from the 1 drug that targets this protein in Forefront's canonical graph (1 with a mapped approved indication, shown above): these count different sets and are not a subset relation.

View all recorded compounds (1)
REGORAFENIBApproval

Open Targets known-drugs universe. Drug name and highest clinical stage only — the disease relationship is NOT read from this slice (it carries trial-context noise); approved indications come from the canonical graph above.

Tractability

Small moleculesStrong

Approved Drug and Structure with Ligand support this modality.

AntibodiesEmerging

Feasibility evidence (uniprot loc high conf and go cc high conf) — no clinical-stage drug of this modality recorded.

Protein degradersEmerging

Feasibility evidence (literature and small molecule binder) — no clinical-stage drug of this modality recorded.

View underlying tractability evidence (9)
SM · Approved DrugSM · Structure with LigandSM · High-Quality LigandSM · Druggable FamilyAB · UniProt loc high confAB · GO CC high confAB · UniProt SigP or TMHMMPR · LiteraturePR · Small Molecule Binder

Raw Open Targets tractability assessment buckets, by modality.

Clinical trials

30

Trials of drugs that target this protein — reached indirectly through those drugs, so a trial listed here studies the drug, not the protein. Ranked by active status, then clinical phase and recency, and spread across the targeting drugs.

View all trials (26)

ClinicalTrials.gov via the drug-target graph.

What's happening now

6

Recent therapeutic activity around this target — regulatory actions, clinical trials and safety signals for a drug that targets this protein, plus publications where such a drug is a genuine subject. Every item is reached indirectly through the drug, not the protein itself; incidental mentions (a paper that merely measures a drug) and press items are excluded.

  1. New publication2024-06-04
    Lenvatinib Plus Pembrolizumab Versus Standard of Care for Previously Treated Metastatic Colorectal Cancer: Final Analysis of the Randomized, Open-Label, Phase III LEAP-017 Study.

    Journal of clinical oncology : official journal of the American Society of Clinical Oncology · 2024 · 69 citations · Europe PMC · via regorafenib

  2. New publication2020-08-11
    Targeted therapy for hepatocellular carcinoma.

    Signal transduction and targeted therapy · 2020 · 565 citations · Europe PMC · via regorafenib

  3. New publication2019-11-04
    Molecular targeted and immune checkpoint therapy for advanced hepatocellular carcinoma.

    Journal of experimental & clinical cancer research : CR · 2019 · 162 citations · Europe PMC · via regorafenib

  4. New publication2019-04-23
    Randomized Double-Blind Phase II Study of Regorafenib in Patients With Metastatic Osteosarcoma.

    Journal of clinical oncology : official journal of the American Society of Clinical Oncology · 2019 · 199 citations · Europe PMC · via regorafenib

  5. New publication2016-12-06
    Regorafenib for patients with hepatocellular carcinoma who progressed on sorafenib treatment (RESORCE): a randomised, double-blind, placebo-controlled, phase 3 trial.

    Lancet (London, England) · 2017 · 2,767 citations · Europe PMC · via regorafenib

  6. Regulatory approval2013-08-26

    Approval: Stivarga (EMA)

    ema · regulatory · ema · via regorafenib

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.