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

DDR1 (Q08345) - Overview - Molecular Target Synopsis

Protein


DDR1, Epithelial discoidin domain-containing receptor 1
Enzyme Classification 2.7.10.1
UniProt Q08345

Also Known as DDR1_HUMAN, DDR1, CAK, EDDR1, NEP, NTRK4, PTK3A, RTK6, TRKE

Tyrosine kinase that functions as cell surface receptor for fibrillar collagen and regulates cell attachment to the extracellular matrix, remodeling of the extracellular matrix, cell migration, differentiation, survival and cell proliferation. Collagen binding triggers a signaling pathway that involves SRC and leads to the activation of MAP kinases. Regulates remodeling of the extracellular matrix by up-regulation of the matrix metalloproteinases MMP2, MMP7 and MMP9, and thereby facilitates cell migration and wound healing. Required for normal blastocyst implantation during pregnancy, for normal mammary gland differentiation and normal lactation. Required for normal ear morphology and normal hearing (By similarity). Promotes smooth muscle cell migration, and thereby contributes to arterial wound healing. Also plays a role in tumor cell invasion. Phosphorylates PTPN11. Homodimer. Interacts (via PPxY motif) with WWC1 (via WW domains) in a collagen-regulated manner. Forms a tripartite complex with WWC1 and PRKCZ, but predominantly in the absence of collagen. Interacts (tyrosine phosphorylated) with SHC1. Interacts with SRC. Interacts with MYH9. Interacts with CDH1. Interacts with PTPN11. Interacts with NCK2.

6HP9
STRUCTURE OF THE KINASE DOMAIN OF HUMAN DDR1 IN COMPLEX WITH A 2- AMINO-2,3-DIHYDRO-1H-INDENE-5-CARBOXAMIDE-BASED INHIBITOR
RCSB/PDB
Inspect Structure
See all 3D Structures for DDR1

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: DDR1 is active in the following subcellular-locations: cell membrane, secreted.
GO terms: DDR1 is active in the following subcellular-locations: extracellular exosome, extracellular space, integral component of plasma membrane, plasma membrane, receptor complex.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project DDR1 has gain in 0 cell-lines, loss in 0 cell-lines and no signal in 0 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: MCF7, T47D, HCC_2998

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: HCC4011, CAL 27, BHY

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: SK-N-SH, HMEC, NHEK

(see details)

3D Structures


For DDR1 there are:
21 structures (26 chains) solved
21 are solved in complex with at least one small molecule ligand
4 are solved with an approved drug

DDR1 is solved in complex with the approved drug(s):

STI/IMATINIB (4BKJ_A, 4BKJ_B),
0LI/PONATINIB (3ZOS_A, 3ZOS_B),
1N1/DASATINIB (5BVW_A, 6BSD_A).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


DDR1 has been screened with 234 compounds (318 bioactivities), 95 compounds have bioactivities that show binding affinity of <= 500nM (133 bioactivities). (see details)