Kinases

Protein kinases constitute 1.7% of all genes in human and this large protein family consists of more than 500 diverse family members. Here we will provide an up to date overview of the current status of structural information for human protein kinases and closely related orthologues (>95% sequence identity) that are available in the protein databank (PDB). Currently the PDB contains the structures of 168 unique human protein kinase domain and 172 kinases considering also closelyrelated orthologues available in the PDB.

Recent unique kinase domain depositions in the PDB

PDB code
Release date
Kinase
Species
Resolution
Sector
10/8/11
CDK8
Human
2.2
Academia
6/7/11
LIMK1
Human
1.65
SGC Oxford
30/3/11
HER2/ErbB2
Human
2.25
Takeda
23/2/11
IRE1
Human
2.7
Academia
9/2/11
ACTR2
Human
1.96
SGC Oxford
9/2/11
PHKg2
Human
2.5
SGC Oxford
19/1/11
KSR2
Human
3.46
Academia
12/1/11
JNK1
Human
2.7
Abbot
24/11/10
RON
Human
2.24
OSI Pharmaceuticals
3/11/10
MYT1
Human
1.7
SGC Oxford
27/10/10
MAP2K4
Human
2.3
PharmAxess
22/9/10
VRK1
Human
2.4
SGC Oxford
25/8/10
CLK2
Human
2.89
SGC Oxford
28/7/10
ALK
Human
1.95
Nerviano
21/7/10
ALK1
Human
2.65
SGC Oxford
14/7/10
ZC1/HGK
Human
2.8
SGC Oxford 

An Excel spreadsheet showing the list of unique human kinase domain depositions in the PDB is available here.

Kinase Domain Structural Coverage

Phylogenetic tree of the kinase family. Kinases with known three dimensional structure that are at least 95% identical to the human reference sequence are highlighted by dots. Structures deposited for the first time by academic structural chemistry laboratories, by industry and by Structural genomics as well as the SGC are shown as red, green, cyan and blue dots, respectively. The tree has been adapted from a phylogenetic analysis by Manning et al. (2002), Science 298:1912-1934. Atypical kinases are not included.

Downloads

Excel spreadsheet of unique human kinase structures available in the protein databank

 

 
 

Contribution of different structure determination groups to the structure determination of the human kinome

During the past 4 years kinase targeted structural genomics has significantly increased the number of novel protein structures and has surpassed published industrial efforts last year.

 

 

Contribution of different structure determination groups to the structure determination of the kinome

Here, only kinases structures that are at least 95% identical to the human reference sequence and with a resolution of at least 3Å have been considered.

 

 

Coverage of the human kinome in terms of sequence identity to the closest available crystal structure

Coverage of the human kinome in terms of sequence identity to the closest available crystal structure. The plot indicated that there are still a large number of kinases targets of unknown structure that share only modest sequence identity with kinases of known structure.