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Updated November 2019

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Nomenclature

Short Name:
Fused
Full Name:
Serine-threonine kinase 36
Alias:
  • EC 2.7.11.1
  • FU
  • Fused serine/threonine kinase
  • KIAA1278
  • Serine/threonine kinase 36, fused
  • STK36

Classification

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

Specific Links

Entrez-Gene Entry: 27148
Entrez-Protein Entry: NP_056505
GeneCards Entry: KIAA1278
KinBASE Entry: FUSED
Pfam Entry: Q9NRP7
PhosphoNET Entry: Q9NRP7
Phosphosite Plus Entry: 697
Source Entry: STK36
UCSD-Nature Entry: A002406
UniProt Entry: Q9NRP7
Kinexus Products: Fused
Serine/threonine-protein kinase 36 S159 phosphosite-specific antibody AB-PK643
Serine/threonine-protein kinase 36 (V156-G162, human) pS159 phosphopeptide - Powder PE-04AMO99

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):
143,995
# Amino Acids:
1315
# mRNA Isoforms:
2
mRNA Isoforms:
143,995 Da (1315 AA; Q9NRP7); 141,737 Da (1294 AA; Q9NRP7-2)
4D Structure:
NA
1D Structure:
Retrieve Gene Sequence
Retrieve Full Protein Sequence
Retrieve Catalytic Domain Sequence
 
Subfamily Alignment
subfamily domain
 
Domain Distribution:
Start End Domain
4 254 Pkinase
1109 1140 HEAT
1147 1183 HEAT
1187 1223 HEAT
1232 1264 HEAT
 

Kinexus Products

Click on entries below for direct links to relevant products from Kinexus for this protein kinase.
hiddentext
○ Serine/threonine-protein kinase 36 S159 phosphosite-specific antibody AB-PK643
○ Serine/threonine-protein kinase 36 (V156-G162, human) pS159 phosphopeptide - Powder PE-04AMO99
 

Post-translation Modifications

For detailed information on phosphorylation of this kinase go to PhosphoNET
Acetylated:
K37.
Serine phosphorylated:

S26, S151, S159, S332, S578, S1293.
Threonine phosphorylated:

T321, T331, T581.
Tyrosine phosphorylated:

Y19, Y25, Y1181.
Ubiquitinated:
K363.
 

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
    37

    1800

    21

    877

  • adrenal
    18

    884

    8

    1616

  • bladder
    -

    -

    -

    -

  • brain
    7

    358

    80

    1013

  • breast
    19

    923

    33

    652

  • cervix
    0.6

    28

    27

    14

  • colon
    0.7

    35

    33

    15

  • heart
    100

    4802

    10

    6877

  • intestine
    0.5

    25

    3

    1

  • kidney
    7

    316

    79

    750

  • liver
    29

    1378

    7

    2147

  • lung
    22

    1044

    36

    1037

  • lymphnode
    37

    1774

    2

    459

  • ovary
    31

    1483

    5

    2522

  • pancreas
    23

    1117

    7

    1705

  • pituitary
    8

    407

    17

    972

  • prostate
    9

    429

    78

    511

  • salivarygland
    19

    909

    5

    1214

  • skeletalmuscle"
    8

    383

    73

    1496

  • skin
    11

    545

    89

    647

  • spinalcord
    22

    1074

    7

    1529

  • spleen
    3

    152

    5

    189

  • stomach
    -

    -

    -

    -

  • testis
    88

    4216

    7

    4250

  • thymus
    20

    982

    7

    1316

  • thyroid
    23

    1120

    57

    790

  • tonsil
    28

    1350

    5

    1882

  • trachea
    35

    1701

    5

    2302

  • uterus
    32

    1536

    5

    2085

  • reticulocytes"
    5

    229

    42

    109

  • t-lymphocytes
    35

    1668

    12

    29

  • b-lymphocytes
    2

    94

    23

    92

  • neutrophils
    3

    149

    71

    301

  • macrophages
    19

    936

    78

    782

  • sperm
    25

    1205

    48

    3591

 

Evolution

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

    100

    100
  • tableheader
    0

    0

    99
  • tableheader
    96.5

    98

    97
  • tableheader
    -

    -

    88
  • tableheader
    -

    -

    92
  • tableheader
    87.9

    92.7

    88
  • tableheader
    -

    -

    -
  • tableheader
    81.9

    87.1

    85
  • tableheader
    85.3

    91.3

    85.5
  • tableheader
    -

    -

    -
  • tableheader
    -

    -

    -
  • tableheader
    51.7

    66.5

    54
  • tableheader
    -

    -

    -
  • tableheader
    32.7

    46.2

    -
  • tableheader
    -

    -

    -
  • tableheader
    25.1

    38.4

    -
  • tableheader
    27.5

    41.5

    -
  • tableheader
    -

    -

    -
  • tableheader
    29.5

    42

    -
  • tableheader
    -

    -

    -
  • tableheader
    -

    -

    -
  • tableheader
    -

    -

    33
  • tableheader
    26.9

    43.6

    -
  • tableheader
    -

    -

    -
  • tableheader
    -

    -

    -
For a wider analysis go to PhosphoNET Evolution in PhosphoNET
 

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
SureCN7018367 Kd < 10 nM 18792927 450519 19035792
Foretinib Kd = 180 nM 42642645 1230609 22037378
Dasatinib Kd = 210 nM 11153014 1421 18183025
R406 Kd = 230 nM 11984591 22037378
AC1NS7CD Kd = 260 nM 5329665 295136 22037378
SNS032 Kd = 260 nM 3025986 296468 18183025
Pazopanib Kd = 470 nM 10113978 477772 18183025
Bosutinib Kd = 570 nM 5328940 288441 22037378
SB202190 Kd = 790 nM 5353940 278041 18183025
SB203580 Kd = 860 nM 176155 10 15711537
TG101348 Kd = 870 nM 16722836 1287853 22037378
WZ3146 Kd > 1 µM 44607360 20033049
WZ4002 Kd > 1 µM 44607530 20033049
Pelitinib Kd = 1.2 µM 6445562 607707 15711537
CHEMBL249097 Kd < 1.25 µM 25138012 249097 19035792
AST-487 Kd = 1.3 µM 11409972 574738 18183025
NVP-TAE684 Kd = 1.4 µM 16038120 509032 22037378
IKK-2 Inhibitor IV Kd < 2.5 µM 9903786 257167 19035792
GSK690693 Kd = 2.6 µM 16725726 494089 22037378
Canertinib Kd = 2.7 µM 156414 31965 15711537
PLX4720 Kd = 2.9 µM 24180719 1230020 22037378
Staurosporine Kd = 2.9 µM 5279 15711537
Lestaurtinib Kd = 3.8 µM 126565 22037378
Sorafenib Kd = 3.8 µM 216239 1336 18183025
Erlotinib Kd = 4.4 µM 176870 553 22037378
BMS-690514 Kd < 4.5 µM 11349170 21531814
Barasertib Kd = 4.6 µM 16007391 215152 18183025
 

Disease Linkage

General Disease Association:

Developmental disorders
Specific Diseases (Non-cancerous):

Syndactyly Type 1
Comments:
Syndactyly type 1 (SD1) is a development disease characterized by the malformation of the limbs, specifically the presence of partial or complete webbing between the third and fourth fingers and/or the second and third toes. The STK36 gene is located on chromosome 2q35 at 217.56 Mb, which is the same region that the SD1 disease maps to, indicating a potential link between STK36 activity and the disease phenotype. In patients with SD1, the STK36 coding region was observed to contain 3 different single nucleotide polymorphisms (SNPs) resulting in two alternative splicing events and the production of two protein isoforms that differed significantly in length. Therefore, the SNPs may be correlated with an increased risk for the development of SD1.
 
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: Brain glioblastomas (%CFC= -97, p<0.08); Brain oligodendrogliomas (%CFC= -100, p<0.075); Breast epithelial carcinomas (%CFC= -50, p<0.088); Breast epithelial hyperplastic enlarged lobular units (HELU) (%CFC= +58, p<0.072); Ovary adenocarcinomas (%CFC= +79, p<0.0002); and Prostate cancer (%CFC= +52, p<(0.0003). The COSMIC website notes an up-regulated expression score for Fused in diverse human cancers of 392, which is 0.9-fold of the average score of 462 for the human protein kinases. The down-regulated expression score of 40 for this protein kinase in human cancers was 0.7-fold of the average score of 60 for the human protein kinases.
Mutagenesis Experiments:

Insertional mutagenesis studies in mice have not yet revealed 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: 0.06 % in 24971 diverse cancer specimens. This rate is only -15 % lower than 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: 0.33 % in 864 skin cancers tested; 0.23 % in 1270 large intestine cancers tested; 0.17 % in 589 stomach cancers tested; 0.13 % in 238 bone cancers tested; 0.11 % in 603 endometrium cancers tested; 0.11 % in 1822 lung cancers tested; 0.08 % in 273 cervix cancers tested; 0.08 % in 1276 kidney cancers tested; 0.07 % in 834 ovary cancers tested; 0.07 % in 548 urinary tract cancers tested; 0.07 % in 441 autonomic ganglia cancers tested; 0.06 % in 942 upper aerodigestive tract cancers tested; 0.05 % in 1512 liver cancers tested; 0.04 % in 1459 pancreas cancers tested; 0.02 % in 2009 haematopoietic and lymphoid cancers tested.
Frequency of Mutated Sites:

Most frequent mutations with the number of reports indicated in brackets: Q103* (9).
Comments:
Only 3 deletions, no insertions or complex mutations are noted on the COSMIC website.
 
COSMIC Entry:
STK36
OMIM Entry:
607652
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