Molecular Target Synopsis
Overview
Domains and Structures
Drugs and Clinical Candidates
Druggability
Chemistry
Ligand Efficiency Plot
Pathways
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
RNAi
Mutations
Germline Genetics

DDR2 (Q16832) - Overview - Molecular Target Synopsis

Protein


DDR2, Discoidin domain-containing receptor 2
Enzyme Classification 2.7.10.1
UniProt Q16832

Also Known as DDR2_HUMAN, DDR2, NTRKR3, TKT, TYRO10

Tyrosine kinase that functions as 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. Binds hydroxyproline-rich sequence motifs in fibrillar, glycosylated collagen, such as the GQOGVMGFO motif, where O stands for hydroxyproline. Interacts with SRC. Interacts (tyrosine phosphorylated) with SHC1.

6FER
CRYSTAL STRUCTURE OF HUMAN DDR2 KINASE IN COMPLEX WITH 2-[4,5- DIFLUORO-2-OXO-1'-(1H-PYRAZOLO[3,4-B]PYRIDINE-5-CARBONYL) SPIRO[INDOLE-3,4'-PIPERIDINE]-1-YL]-N-(2,2,2-TRIFLUOROETHYL)ACETAMIDE
RCSB/PDB
Inspect Structure
See all 3D Structures for DDR2

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: DDR2 is active in the following subcellular-locations: cell membrane.
GO terms: DDR2 is active in the following subcellular-locations: actin cytoskeleton, apical plasma membrane, focal adhesion, integral component of plasma membrane, plasma membrane, receptor complex.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project DDR2 has gain in 4 cell-lines, loss in 0 cell-lines and no signal in 1001 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: SNB_75, NCI_H226, HS578T

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: G130, Hs 675.T, MHH-ES-1

In Array Express (RNA-seq of long poly adenylated RNA and long non poly adenylated RNA from ENCODE cell lines), the highest expressing cell lines are: NHLF, BJ, AG445

(see details)

RNA Interference


DDR2 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: NY, TE10. (see details)

3D Structures


For DDR2 there are:
3 structures (14 chains) solved
1 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


DDR2 has been screened with 766 compounds (1439 bioactivities), 95 compounds have bioactivities that show binding affinity of <= 500nM (158 bioactivities). (see details)