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Updated November 2019

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Nomenclature

Short Name:
CDKL1
Full Name:
Serine-threonine-protein kinase KKIALRE
Alias:
  • Cyclin-dependent kinase-like 1

Classification

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

Specific Links

Entrez-Gene Entry: 8814
Entrez-Protein Entry: NP_004187
GeneCards Entry: KKIALRE
KinBASE Entry: CDKL1
OMIM Entry: 603441
Pfam Entry: Q00532
PhosphoNET Entry: Q00532
Phosphosite Plus Entry: 703
ScanSite Entry: Q00532
Source Entry: CDKL1
UCSD-Nature Entry: A001345
UniProt Entry: Q00532
Kinexus Products: CDKL1
Cyclin-dependent kinase-like 1; Serine/threonine protein kinase KKIALRE pan-specific antibody AB-NK199

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):
41671
# Amino Acids:
357
# mRNA Isoforms:
2
mRNA Isoforms:
41,671 Da (357 AA; Q00532); 41,671 Da (357 AA; Q00532-2)
4D Structure:
NA
1D Structure:
Retrieve Gene Sequence
Retrieve Full Protein Sequence
Retrieve Catalytic Domain Sequence
 
3D Image (rendered using PV Viewer):

PDB ID
4AGU

Subfamily Alignment
subfamily domain
 
Domain Distribution:
Start End Domain
4 287 Pkinase
 

Kinexus Products

Click on entries below for direct links to relevant products from Kinexus for this protein kinase.
hiddentext
○ Cyclin-dependent kinase-like 1; Serine/threonine protein kinase KKIALRE pan-specific antibody AB-NK199
 

Post-translation Modifications

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

T26.
Tyrosine phosphorylated:

Y161.
 

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
    100

    762

    28

    1077

  • adrenal
    1

    9

    14

    8

  • bladder
    25

    189

    9

    146

  • brain
    16

    122

    108

    279

  • breast
    54

    412

    27

    225

  • cervix
    0.7

    5

    55

    6

  • colon
    26

    198

    43

    396

  • heart
    78

    594

    33

    1646

  • intestine
    36

    275

    10

    281

  • kidney
    9

    66

    84

    63

  • liver
    2

    13

    25

    13

  • lung
    54

    409

    139

    505

  • lymphnode
    6

    46

    20

    67

  • ovary
    2

    14

    9

    15

  • pancreas
    3

    24

    21

    22

  • pituitary
    1

    9

    19

    10

  • prostate
    3

    24

    201

    19

  • salivarygland
    3

    25

    17

    21

  • skeletalmuscle"
    2

    13

    75

    13

  • skin
    50

    379

    107

    309

  • spinalcord
    5

    38

    22

    43

  • spleen
    11

    82

    23

    113

  • stomach
    5

    36

    18

    36

  • testis
    2

    17

    18

    18

  • thymus
    4

    28

    24

    21

  • thyroid
    59

    450

    70

    469

  • tonsil
    3

    25

    23

    36

  • trachea
    8

    59

    15

    64

  • uterus
    45

    341

    16

    412

  • reticulocytes"
    17

    129

    28

    118

  • t-lymphocytes
    66

    502

    18

    368

  • b-lymphocytes
    36

    276

    31

    363

  • neutrophils
    0.4

    3

    41

    1

  • macrophages
    88

    673

    83

    627

  • sperm
    3

    24

    48

    9

 

Evolution

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

    100

    100
  • tableheader
    0

    0

    99
  • tableheader
    97.7

    99.1

    -
  • tableheader
    -

    -

    91.5
  • tableheader
    -

    -

    -
  • tableheader
    88.5

    92.6

    91
  • tableheader
    -

    -

    -
  • tableheader
    88.8

    92.7

    90
  • tableheader
    88.2

    93

    89.5
  • tableheader
    -

    -

    -
  • tableheader
    86.5

    92.7

    -
  • tableheader
    37.8

    52.3

    84
  • tableheader
    36.9

    54.6

    85
  • tableheader
    77

    87.9

    79
  • tableheader
    -

    -

    -
  • tableheader
    43.1

    54.6

    61
  • tableheader
    53.2

    69.6

    -
  • tableheader
    -

    -

    62
  • tableheader
    59.5

    73

    -
  • tableheader
    -

    -

    -
  • tableheader
    34.4

    54.3

    -
  • tableheader
    -

    -

    -
  • tableheader
    33

    54.6

    -
  • 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
AST-487 Kd = 13 nM 11409972 574738 22037378
Staurosporine Kd = 330 nM 5279 22037378
Lestaurtinib Kd = 490 nM 126565 22037378
WZ3146 Kd > 1 µM 44607360 20033049
WZ4002 Kd > 1 µM 44607530 20033049
R406 Kd = 2.1 µM 11984591 22037378
 

Disease Linkage

General Disease Association:

Cancer
Specific Cancer Types:
Gastric cancer
Comments:
CDKL1 may be an oncoprotein (OP). Significantly elevated CDKL1 expression was observed in gastric cancer tissue specimens. In addition, loss of CDKL1 function in gastric cancer cell lines (SGC7901 and MGC-803) resulted in impaired cell proliferation and enhanced apoptosis, indicating that CDKL1 functions as an oncoprotein. Furthermore, siRNA-mediated knockdown of CDKL1 expression stimulated the pro-apoptotic factor Bcl-2-interacting killer (BIK) and reduced cellular expression of the proliferating cell nuclear antigen (PCNA), indicating reduced cellular proliferation. Therefore, CDKL1 is thought to play a key role in gastric cancer cell proliferation and survival.
 
Gene Expression in Cancers:

The COSMIC website notes an up-regulated expression score for CDKL1 in diverse human cancers of 369, which is 0.8-fold of the average score of 462 for the human protein kinases. The down-regulated expression score of 2 for this protein kinase in human cancers was 97% lower than 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: 0.05 % in 24727 diverse cancer specimens. This rate is only -31 % 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: 0.29 % in 1270 large intestine cancers tested.
Frequency of Mutated Sites:

None > 3 in 20,012 cancer specimens
Comments:
No deletions, insertions or complex mutations are noted on the COSMIC website.
 
COSMIC Entry:
CDKL1
OMIM Entry:
603441
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