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Updated November 2019

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Nomenclature

Short Name:
CK1g3
Full Name:
Casein kinase I, gamma 3 isoform
Alias:
  • CK1-gamma3
  • CSNK1G3
  • EC 2.7.11.1
  • KC13
  • KC1G3

Classification

Type:
Protein-serine/threonine kinase
Group:
CK1
Family:
CK1
SubFamily:
NA
 
 

Specific Links

Entrez-Gene Entry: 1456
Entrez-Protein Entry: NP_004375
GeneCards Entry: CKIGAMMA3
KinBASE Entry: CK1G3
OMIM Entry: 604253
Pfam Entry: Q9Y6M4
PhosphoNET Entry: Q9Y6M4
Phosphosite Plus Entry: 3751
Protein Data Bank Entry: 2CHL
Source Entry: CSNK1G3
UCSD-Nature Entry: A000491
UniProt Entry: Q9Y6M4

General Links

ClustalW2
GPS-Cuckoo
Human Protein Atlas
Kinase.com
Kinase Research
Kinasource
Kinomer
Netphorest
NetworKIN
Phosida
PhosphoElm
Protein Blast
ScanSite
String

Structure

Mol. Mass (Da):
51,389
# Amino Acids:
447
# mRNA Isoforms:
6
mRNA Isoforms:
52,378 Da (455 AA; Q9Y6M4-2); 51,389 Da (447 AA; Q9Y6M4); 49,027 Da (424 AA; Q9Y6M4-4); 48,898 Da (423 AA; Q9Y6M4-3); 40,729 Da (348 AA; Q9Y6M4-5); 36,492 Da (311 AA; Q9Y6M4-6)
4D Structure:
Monomer
1D Structure:
Retrieve Gene Sequence
Retrieve Full Protein Sequence
Retrieve Catalytic Domain Sequence
 
3D Image (rendered using PV Viewer):

PDB ID
2CHL

Subfamily Alignment
subfamily domain
 
Domain Distribution:
Start End Domain
43 304 Pkinase
 

Post-translation Modifications

For detailed information on phosphorylation of this kinase go to PhosphoNET
Serine phosphorylated:

S11, S31, S32, S34, S344, S345, S392, S413.
Threonine phosphorylated:

T29, T65, T256, T399, T421.
Tyrosine phosphorylated:

Y64, Y68, Y87, Y90, Y160, Y261.
Ubiquitinated:
K253.
 

Distribution

Based on gene microarray analysis from the NCBI
Human Tissue Distribution
% Max Expression:

Mean Expression:

Number of Samples:

Standard Deviation:
% Max Expression:

Mean Expression:

Number of Samples:

Standard Deviation:
  • adipose
    29

    1024

    28

    910

  • adrenal
    0.8

    27

    10

    23

  • bladder
    4

    153

    13

    87

  • brain
    9

    299

    123

    489

  • breast
    22

    756

    34

    665

  • cervix
    3

    118

    63

    157

  • colon
    4

    131

    35

    103

  • heart
    37

    1295

    44

    3065

  • intestine
    22

    757

    10

    739

  • kidney
    3

    97

    91

    82

  • liver
    4

    123

    34

    98

  • lung
    20

    686

    108

    653

  • lymphnode
    4

    133

    24

    81

  • ovary
    1.2

    43

    6

    41

  • pancreas
    3

    103

    31

    86

  • pituitary
    1.4

    47

    17

    34

  • prostate
    11

    381

    199

    2792

  • salivarygland
    3

    105

    18

    86

  • skeletalmuscle"
    2

    74

    85

    49

  • skin
    20

    695

    112

    661

  • spinalcord
    3

    109

    30

    98

  • spleen
    4

    122

    32

    109

  • stomach
    6

    193

    14

    108

  • testis
    4

    149

    18

    117

  • thymus
    3

    89

    30

    79

  • thyroid
    23

    790

    80

    878

  • tonsil
    3

    112

    27

    83

  • trachea
    4

    123

    18

    86

  • uterus
    5

    168

    18

    134

  • reticulocytes"
    2

    77

    42

    76

  • t-lymphocytes
    22

    765

    30

    535

  • b-lymphocytes
    100

    3473

    31

    6379

  • neutrophils
    4

    154

    78

    421

  • macrophages
    26

    892

    78

    727

  • sperm
    9

    309

    48

    512

 

Evolution

Species Conservation
PhosphoNET % Identity:
PhosphoNET % Similarity:
Homologene %
Identity:
PhosphoNET % Identity:
PhosphoNET % Similarity:
Homologene %
Identity:
  • tableheader
    100

    100

    100
  • tableheader
    80.4

    88.8

    100
  • tableheader
    99.8

    99.8

    100
  • tableheader
    -

    -

    99
  • tableheader
    -

    -

    -
  • tableheader
    99.3

    99.8

    100
  • tableheader
    -

    -

    -
  • tableheader
    85.7

    88.6

    99
  • tableheader
    98.9

    99.5

    99
  • tableheader
    -

    -

    -
  • tableheader
    -

    -

    -
  • tableheader
    79.6

    88.2

    -
  • tableheader
    77

    86.1

    97
  • tableheader
    77.6

    83.9

    82
  • tableheader
    -

    -

    -
  • tableheader
    41.4

    58.8

    71
  • tableheader
    -

    -

    -
  • tableheader
    -

    -

    -
  • tableheader
    -

    -

    -
  • tableheader
    -

    -

    -
  • tableheader
    -

    -

    -
  • tableheader
    -

    -

    -
  • tableheader
    46

    62.7

    -
  • tableheader
    38.8

    53.3

    49
  • tableheader
    -

    -

    64
For a wider analysis go to PhosphoNET Evolution in PhosphoNET
 

Binding Proteins

Examples of known interacting proteins
hiddentext
No. Name – UniProt ID
1 PPP1R14A - Q96A00
2 CSNK1G2 - P78368
3 CSNK1G1 - Q9HCP0
4 CSNK1D - P48730
 

Regulation

Activation:
NA
Inhibition:
NA
Synthesis:
NA
Degradation:
NA
 

Protein Kinase Specificity

Matrix of observed frequency (%) of amino acids in aligned protein substrate phosphosites

Kinections GIF
Matrix Type:
Predicted from the application of the Kinexus Kinase Substrate Predictor Version 2.0 algorithm, which was trained with over 10,000 kinase-protein substrate pairs and 8,000 kinase-peptide substrate pairs.
Domain #:
1
 

Inhibitors

For further details on these inhibitors click on the Compound Name and enter it into DrugKiNET or click on the ID's
Based on in vitro and/or in vivo phosphorylation data
Compound Name KD, Ki or IC50 (nM) PubChem ID ChEMBL ID PubMed ID
Aloisine A IC50 > 50 nM 5326843 75680 22037377
Compound 52 IC50 > 50 nM 2856 22037377
AST-487 Kd = 97 nM 11409972 574738 18183025
Cdk1/2 Inhibitor III IC50 > 150 nM 5330812 261720 22037377
Purvalanol A IC50 > 150 nM 456214 23327 22037377
Sunitinib Kd = 240 nM 5329102 535 18183025
TG003 Kd = 290 nM 1893668 408982 19837585
CGP74514A IC50 = 500 nM 2794188 367625 22037377
SU11652 IC50 = 500 nM 24906267 13485 22037377
Lestaurtinib Kd = 570 nM 126565 18183025
SU14813 Kd = 570 nM 10138259 1721885 18183025
A674563 Kd = 910 nM 11314340 379218 22037378
A 443654 IC50 < 1 µM 10172943 379300 19465931
Aurora A Inhibitor 29 (DF) Kd = 1 µM 21992004
Icotinib IC50 > 1 µM 22024915 22112293
IRAK-1-4 Inhibitor I IC50 > 1 µM 11983295 379787 22037377
MK5108 IC50 > 1 µM 24748204 20053775
ML3403 IC50 > 1 µM 6419739 111364 22037377
NU6140 IC50 > 1 µM 10202471 1802728 22037377
PKR Inhibitor IC50 > 1 µM 6490494 235641 22037377
WZ3146 Kd > 1 µM 44607360 20033049
WZ4002 Kd > 1 µM 44607530 20033049
KW2449 Kd = 1.2 µM 11427553 1908397 22037378
BI2536 Kd = 2.4 µM 11364421 513909 22037378
Roscovitine Kd = 2.9 µM 160355 14762 18183025
 

Disease Linkage

General Disease Association:

Cancer
Specific Cancer Types:
Non-small cell lung cancer (NSCLC); Anaplastic large cell lymphomas (ALCL); Gastric carcinomas
Gene Expression in Cancers:

TranscriptoNET (www.transcriptonet.ca) analysis with mRNA expression data retrieved from the National Center for Biotechnology Information's Gene Expression Omnibus (GEO) database, which was normalized against 60 abundantly and commonly found proteins, indicated altered expression for this protein kinase as shown here as the percent change from normal tissue controls (%CFC) as supported with the Student T-test in the following types of human cancers: Bladder carcinomas (%CFC= +90, p<0.0001); Pituitary adenomas (ACTH-secreting) (%CFC= +51); Skin fibrosarcomas (%CFC= +57); and Skin squamous cell carcinomas (%CFC= +48, p<0.022). The COSMIC website notes an up-regulated expression score for CK1g3 in diverse human cancers of 362, which is 0.8-fold of the average score of 462 for the human protein kinases. The down-regulated expression score of 258 for this protein kinase in human cancers was 4.3-fold of the average score of 60 for the human protein kinases.
Mutagenesis Experiments:

Insertional mutagenesis studies in mice support a role for this protein kinase in mouse cancer oncogenesis.
Mutation Rate in All Cancers:

Percent mutation rates per 100 amino acids length in human cancers: 0.07 % in 24752 diverse cancer specimens. This rate is only -5 % lower and is very similar to the average rate of 0.075 % calculated for human protein kinases in general.
Mutation Rate in Specific Cancers:

Highest percent mutation rates per 100 amino acids length in human cancers: 0.37 % in 1270 large intestine cancers tested; 0.3 % in 603 endometrium cancers tested; 0.27 % in 589 stomach cancers tested.
Frequency of Mutated Sites:

None > 3 in 20,035 cancer specimens
Comments:
Only 4 deletions, 3 insertions, and no complex mutations are noted on the COSMIC website.
 
COSMIC Entry:
CSNK1G3
OMIM Entry:
604253
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