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

PTK2 (Q00944) - Overview - Molecular Target Synopsis

Protein


PTK2, Focal adhesion kinase 1
Enzyme Classification 2.7.10.2
UniProt Q00944

Also Known as FAK1_CHICK, PTK2, FAK, FAK1

Non-receptor protein-tyrosine kinase that plays an essential role in regulating cell migration, adhesion, spreading, reorganization of the actin cytoskeleton, formation and disassembly of focal adhesions and cell protrusions, cell cycle progression, cell proliferation and apoptosis. Required for early embryonic development, embryonic angiogenesis, normal cardiomyocyte migration and proliferation, and normal heart development. Regulates axon growth and neuronal cell migration, axon branching and synapse formation; required for normal development of the nervous system. Plays a role in osteogenesis and differentiation of osteoblasts. Functions in integrin signal transduction, but also in signaling downstream of numerous growth factor receptors, G-protein coupled receptors (GPCR), ephrin receptors, netrin receptors and LDL receptors. Forms multisubunit signaling complexes with SRC and SRC family members upon activation; this leads to the phosphorylation of additional tyrosine residues, creating binding sites for scaffold proteins, effectors and substrates. Regulates numerous signaling pathways. Promotes activation of phosphatidylinositol 3-kinase and the AKT1 signaling cascade. Promotes activation of MAPK1/ERK2, MAPK3/ERK1 and the MAP kinase signaling cascade. Promotes localized and transient activation of guanine nucleotide exchange factors (GEFs) and GTPase-activating proteins (GAPs), and thereby modulates the activity of Rho family GTPases. Signaling via CAS family members mediates activation of RAC1. Regulates P53/TP53 activity and stability. Phosphorylates SRC; this increases SRC kinase activity. Isoform 2 (FRNK) does not contain a kinase domain and inhibits PTK2/FAK1 phosphorylation and signaling. Interacts with ARHGAP26, GRB7, DCC, PIK3R1, PXN and SRC. Interacts with the ARP2/3 complex.

6GCW
FOCAL ADHESION KINASE CATALYTIC DOMAIN IN COMPLEX WITH IRREVERSIBLE INHIBITOR
RCSB/PDB
Inspect Structure
See all 3D Structures for PTK2

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
1053Q00944-1
361Q00944-2

Sub-cellular localization


UniProt: PTK2 is active in the following subcellular-locations: cell junction, cell membrane, centrosome, cytoplasm, cytoskeleton, focal adhesion, microtubule organizing center, nucleus, perinuclear region.
GO terms: PTK2 is active in the following subcellular-locations: cell, cytoplasm, dendritic spine, focal adhesion, microtubule organizing center, nucleus, perinuclear region of cytoplasm, sarcolemma.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project PTK2 has gain in 0 cell-lines, loss in 0 cell-lines and no signal in 0 cell-lines. (see details)

3D Structures


For PTK2 there are:
32 structures (47 chains) solved
17 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


PTK2 has been screened with compounds ( bioactivities). (see details)