Nomenclature
Short Name:
PCTAIRE2
Full Name:
Serine-threonine-protein kinase PCTAIRE-2
Alias:
- CDK17
- Serine/threonine-protein kinase PCTAIRE-2
- EC 2.7.11.22
- KPT2
- PCTAIRE protein kinase 2
- PCTAIRE-motif protein kinase 2
- PCTK2
Classification
Type:
Protein-serine/threonine kinase
Group:
CMGC
Family:
CDK
SubFamily:
TAIRE
Specific Links
Structure
Mol. Mass (Da):
59,582
# Amino Acids:
523
# mRNA Isoforms:
2
mRNA Isoforms:
59,582 Da (523 AA; Q00537); 59,531 Da (523 AA; Q00537-2)
4D Structure:
Found in a complex containing CABLES1, CDK16 and TDRD7. Interacts with TDRD7
1D Structure:
Subfamily Alignment
Domain Distribution:
| Start | End | Domain |
|---|---|---|
| 192 | 473 | Pkinase |
Kinexus Products
Click on entries below for direct links to relevant products from Kinexus for this protein kinase.
hiddentext
Post-translation Modifications
For detailed information on phosphorylation of this kinase go to PhosphoNET
Acetylated:
K469.
Methylated:
K328.
Serine phosphorylated:
S9, S64, S75, S80, S92, S105, S122, S137, S146, S165, S176, S180, S182+, S346+, S444, S491, S520.
Threonine phosphorylated:
T11, T124, T202, T205.
Tyrosine phosphorylated:
Y203-, Y207.
Ubiquitinated:
K160, K194, K197, K221, K328, K452, K493.
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:
100
948
29
1115
5
46
16
43
13
127
2
104
69
652
91
698
87
822
24
732
12
118
82
143
24
228
35
295
43
403
38
519
44
417
17
374
7
63
89
72
8
80
26
125
66
622
188
679
9
87
24
63
5
48
15
51
7
67
20
88
7
70
16
66
8
78
272
100
4
34
13
27
7
64
83
51
66
621
109
706
21
197
19
324
20
185
22
301
3
27
12
39
8
77
13
73
20
187
19
352
63
594
52
674
8
73
27
54
5
49
13
41
8
80
13
95
6
56
28
39
59
560
24
398
72
684
30
640
9
89
105
246
93
881
57
776
15
145
35
138
Evolution
Species Conservation
PhosphoNET % Identity:
PhosphoNET % Similarity:
Homologene %
Identity:
PhosphoNET % Identity:
PhosphoNET % Similarity:
Homologene %
Identity:
100
100
100
93.6
93.8
100
67.3
80.1
100
-
-
99
-
-
-
94.6
95.1
98
-
-
-
98.6
99.8
99
96.3
97.7
98.5
-
-
-
98.4
99.4
-
95.7
97.1
98
43.4
56.9
92.5
38.2
53.9
92
-
-
-
-
-
-
-
-
-
-
-
57
-
-
-
-
-
-
31.5
44.5
-
-
-
-
31.5
44.1
-
-
-
-
-
-
-
For a wider analysis go to PhosphoNET Evolution in PhosphoNET
Binding Proteins
Examples of known interacting proteins
hiddentext
| No. | Name – UniProt ID |
|---|---|
| 1 | TDRD7 - Q8NHU6 |
| 2 | TGFBR1 - P36897 |
| 3 | YWHAG - P61981 |
Regulation
Activation:
NA
Inhibition:
NA
Synthesis:
NA
Degradation:
NA
Protein Kinase Specificity
Matrix of observed frequency (%) of amino acids in aligned protein substrate phosphosites
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 |
|---|
| R547 | Kd = 860 pM | 6918852 | 22037378 | |
| AT7519 | Kd = 950 pM | 11338033 | 22037378 | |
| AC1NS7CD | Kd = 13 nM | 5329665 | 295136 | 22037378 |
| SNS032 | Kd = 13 nM | 3025986 | 296468 | 18183025 |
| AST-487 | Kd = 15 nM | 11409972 | 574738 | 18183025 |
| CHEMBL1082152 | Kd = 69 nM | 11560568 | 1082152 | 20138512 |
| Nintedanib | Kd = 93 nM | 9809715 | 502835 | 22037378 |
| Staurosporine | Kd = 96 nM | 5279 | 18183025 | |
| Foretinib | Kd = 170 nM | 42642645 | 1230609 | 22037378 |
| JNJ-7706621 | Kd = 290 nM | 5330790 | 191003 | 18183025 |
| TG101348 | Kd = 350 nM | 16722836 | 1287853 | 22037378 |
| Alvocidib | Kd = 480 nM | 9910986 | 428690 | 18183025 |
| Lestaurtinib | Kd = 720 nM | 126565 | 22037378 | |
| NVP-TAE684 | Kd = 810 nM | 16038120 | 509032 | 22037378 |
| PHA-665752 | Kd = 880 nM | 10461815 | 450786 | 22037378 |
| WZ3146 | Kd > 1 µM | 44607360 | 20033049 | |
| WZ4002 | Kd > 1 µM | 44607530 | 20033049 | |
| Sunitinib | Kd = 1.2 µM | 5329102 | 535 | 18183025 |
| Sorafenib | Kd = 1.6 µM | 216239 | 1336 | 18183025 |
| A674563 | Kd = 1.9 µM | 11314340 | 379218 | 22037378 |
| KW2449 | Kd = 1.9 µM | 11427553 | 1908397 | 22037378 |
| Dovitinib | Kd = 3 µM | 57336746 | 18183025 |
Disease Linkage
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: Ovary adenocarcinomas (%CFC= -49, p<0.08); and Prostate cancer - primary (%CFC= +166, p<0.0001) The COSMIC website notes an up-regulated expression score for PCTAIRE2 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 147 for this protein kinase in human cancers was 2.5-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: 0.08 % in 24939 diverse cancer specimens. This rate is only 12 % higher 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: 0.54 % in 603 endometrium cancers tested; 0.44 % in 1270 large intestine cancers tested; 0.21 % in 273 cervix cancers tested; 0.2 % in 864 skin cancers tested; 0.16 % in 589 stomach cancers tested; 0.15 % in 1822 lung cancers tested; 0.11 % in 833 ovary cancers tested; 0.08 % in 710 oesophagus cancers tested; 0.08 % in 238 bone cancers tested; 0.07 % in 881 prostate cancers tested; 0.07 % in 1316 breast cancers tested; 0.06 % in 1512 liver cancers tested; 0.04 % in 2082 central nervous system cancers tested; 0.04 % in 1276 kidney cancers tested.
Frequency of Mutated Sites:
Most frequent mutations with the number of reports indicated in brackets: R312G (4) R310S (3).
Comments:
Only 1 deletion and 1 insertion, and no complex mutations are noted on the COSMIC website.