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Information on EC 2.7.11.22 - cyclin-dependent kinase

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EC Tree
IUBMB Comments
Activation of cyclin-dependent kinases requires association of the enzyme with a regulatory subunit referred to as a cyclin. It is the sequential activation and inactivation of cyclin-dependent kinases, through the periodic synthesis and destruction of cyclins, that provides the primary means of cell-cycle regulation.
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This record set is specific for:
UNIPROT: P11802
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Word Map
The enzyme appears in viruses and cellular organisms
Reaction Schemes
+
a [protein]-(L-serine/L-threonine)
=
+
a [protein]-(L-serine/L-threonine) phosphate
Synonyms
cyclin-dependent kinase, cdk, p34cdc2, cdkl5, cdc2 kinase, cyclin-dependent kinase 5, cyclin-dependent kinase 2, cdc28, cyclin-dependent kinase 4, cyclin-dependent kinase 1, more
SYNONYM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
cell division protein kinase 4
-
Cyclin-dependent kinase pef1
-
-
-
-
PHO85 homolog
-
-
-
-
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
phospho group transfer
-
-
-
-
SYSTEMATIC NAME
IUBMB Comments
ATP:cyclin phosphotransferase
Activation of cyclin-dependent kinases requires association of the enzyme with a regulatory subunit referred to as a cyclin. It is the sequential activation and inactivation of cyclin-dependent kinases, through the periodic synthesis and destruction of cyclins, that provides the primary means of cell-cycle regulation.
CAS REGISTRY NUMBER
COMMENTARY hide
150428-23-2
-
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
additional information
?
-
NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
additional information
?
-
COFACTOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
cyclin D
in complex with CDK4
-
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
4-(1-ethyl-2-methyl-1H-imidazol-5-yl)-N-[4-(methylsulfonyl)phenyl]pyrimidin-2-amine
-
4-[(4-imidazo[1,2-a]pyridin-3-ylpyrimidin-2-yl)amino]-N-(2-methoxyethyl)benzenesulfonamide
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4-[(4-imidazo[1,2-a]pyridin-3-ylpyrimidin-2-yl)amino]benzenesulfonamide
-
4-[(4-imidazo[1,2-b]pyridazin-3-ylpyrimidin-2-yl)amino]-N-methylbenzenesulfonamide
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4-[2-methyl-1-(1-methylethyl)-1H-imidazol-5-yl]-N-(4-[[3-(1,3-oxazetidin-3-yl)propyl]sulfonyl]phenyl)pyrimidin-2-amine
-
4-[2-methyl-1-(1-methylethyl)-1H-imidazol-5-yl]-N-[4-(methylsulfonyl)phenyl]pyrimidin-2-amine
-
4-[2-methyl-1-(1-methylethyl)-1H-imidazol-5-yl]-N-[4-(propylsulfonyl)phenyl]pyrimidin-2-amine
-
4-[2-methyl-1-(1-methylethyl)-1H-imidazol-5-yl]-N-[4-[(tetrahydrofuran-2-ylmethyl)sulfonyl]phenyl]pyrimidin-2-amine
-
4-[[4-(1,2-dimethyl-1H-imidazol-5-yl)pyrimidin-2-yl]amino]-N-(2-methoxyethyl)-N-methylbenzenesulfonamide
-
4-[[4-(1,2-dimethyl-1H-imidazol-5-yl)pyrimidin-2-yl]amino]-N-(2-methoxyethyl)benzenesulfonamide
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4-[[4-(1,2-dimethyl-1H-imidazol-5-yl)pyrimidin-2-yl]amino]-N-methylbenzenesulfonamide
-
4-[[4-(1,2-dimethyl-1H-imidazol-5-yl)pyrimidin-2-yl]amino]-N-[3-(1-methylethoxy)propyl]benzenesulfonamide
-
4-[[4-(1,2-dimethyl-1H-imidazol-5-yl)pyrimidin-2-yl]amino]benzenesulfonamide
-
4-[[4-(1-cyclopentyl-2-methyl-1H-imidazol-5-yl)pyrimidin-2-yl]amino]-N-(2-methoxyethyl)benzenesulfonamide
-
4-[[4-(1-cyclopropyl-2-methyl-1H-imidazol-5-yl)pyrimidin-2-yl]amino]-N-(2-methoxyethyl)benzenesulfonamide
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4-[[4-(1-ethyl-2-methyl-1H-imidazol-5-yl)pyrimidin-2-yl]amino]-N-(2-methoxyethyl)benzenesulfonamide
-
N-(2-methoxyethyl)-4-([4-[2-methyl-1-(1-methylethyl)-1H-imidazol-5-yl]pyrimidin-2-yl]amino)benzenesulfonamide
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N-(2-methoxyethyl)-4-([4-[2-methyl-1-(2-methylpropyl)-1H-imidazol-5-yl]pyrimidin-2-yl]amino)benzenesulfonamide
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N-(2-methoxyethyl)-4-[[4-(1,2,4-trimethyl-1H-imidazol-5-yl)pyrimidin-2-yl]amino]benzenesulfonamide
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N-(4-[[3-(dimethylamino)propyl]sulfonyl]phenyl)-4-(1,2-dimethyl-1H-imidazol-5-yl)pyrimidin-2-amine
-
N-(4-[[3-(dimethylamino)propyl]sulfonyl]phenyl)-4-[2-methyl-1-(1-methylethyl)-1H-imidazol-5-yl]pyrimidin-2-amine
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N-[2-(1-aminohydrazino)ethyl]-4-[[4-(1,2-dimethyl-1H-imidazol-5-yl)pyrimidin-2-yl]amino]benzenesulfonamide
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N-[2-(dimethylamino)ethyl]-4-[(4-imidazo[1,2-b]pyridazin-3-ylpyrimidin-2-yl)amino]benzenesulfonamide
-
N-[4-(benzylsulfonyl)phenyl]-4-[2-methyl-1-(1-methylethyl)-1H-imidazol-5-yl]pyrimidin-2-amine
-
N-[4-[(2-methoxyethyl)sulfonyl]phenyl]-4-[2-methyl-1-(1-methylethyl)-1H-imidazol-5-yl]pyrimidin-2-amine
-
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.00021
4-[2-methyl-1-(1-methylethyl)-1H-imidazol-5-yl]-N-(4-[[3-(1,3-oxazetidin-3-yl)propyl]sulfonyl]phenyl)pyrimidin-2-amine
Homo sapiens
with CDK4
0.00045
4-[2-methyl-1-(1-methylethyl)-1H-imidazol-5-yl]-N-[4-(methylsulfonyl)phenyl]pyrimidin-2-amine
Homo sapiens
with isozyme CDK4
0.00053
4-[2-methyl-1-(1-methylethyl)-1H-imidazol-5-yl]-N-[4-[(tetrahydrofuran-2-ylmethyl)sulfonyl]phenyl]pyrimidin-2-amine
Homo sapiens
with CDK4
0.0056
4-[[4-(1,2-dimethyl-1H-imidazol-5-yl)pyrimidin-2-yl]amino]-N-(2-methoxyethyl)benzenesulfonamide
Homo sapiens
with isozyme CDK4
0.009
4-[[4-(1-cyclopropyl-2-methyl-1H-imidazol-5-yl)pyrimidin-2-yl]amino]-N-(2-methoxyethyl)benzenesulfonamide
Homo sapiens
with CDK4, IC50 above 0.009 mM
0.0013
4-[[4-(1-ethyl-2-methyl-1H-imidazol-5-yl)pyrimidin-2-yl]amino]-N-(2-methoxyethyl)benzenesulfonamide
Homo sapiens
with CDK4
0.0002
N-(2-methoxyethyl)-4-([4-[2-methyl-1-(1-methylethyl)-1H-imidazol-5-yl]pyrimidin-2-yl]amino)benzenesulfonamide
Homo sapiens
with CDK4
0.0086
N-(2-methoxyethyl)-4-[[4-(1,2,4-trimethyl-1H-imidazol-5-yl)pyrimidin-2-yl]amino]benzenesulfonamide
Homo sapiens
with CDK4, IC50 above 0.0086 mM
0.00014
N-(4-[[3-(dimethylamino)propyl]sulfonyl]phenyl)-4-[2-methyl-1-(1-methylethyl)-1H-imidazol-5-yl]pyrimidin-2-amine
Homo sapiens
with CDK4
0.0015
N-[4-(benzylsulfonyl)phenyl]-4-[2-methyl-1-(1-methylethyl)-1H-imidazol-5-yl]pyrimidin-2-amine
Homo sapiens
with CDK4
0.00049
N-[4-[(2-methoxyethyl)sulfonyl]phenyl]-4-[2-methyl-1-(1-methylethyl)-1H-imidazol-5-yl]pyrimidin-2-amine
Homo sapiens
with CDK4
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION?
CDK4_HUMAN
303
0
33730
Swiss-Prot
other Location (Reliability: 2)
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
34000
x * 34000
SUBUNIT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
?
x * 34000
PROTEIN VARIANTS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Hanks, S.K.
Homology probing: identification of cDNA clones encoding members of the protein-serine kinase family
Proc. Natl. Acad. Sci. USA
84
388-392
1987
Homo sapiens (P11802)
Manually annotated by BRENDA team
Soufir, N.; Avril, M.F.; Chompret, A.; Demenais, F.; Bombled, J.; Spatz, A.; Stoppa-Lyonnet, D.; Benard, J.; Bressac-de Paillerets, B.
Prevalence of p16 and CDK4 germline mutations in 48 melanoma-prone families in France. The French Familial Melanoma Study Group
Hum. Mol. Genet.
7
209-216
1998
Homo sapiens (P11802)
Manually annotated by BRENDA team
Elkahloun, A.G.; Krizman, D.B.; Wang, Z.; Hofmann, T.A.; Roe, B.; Meltzer, P.S.
Transcript mapping in a 46-kb sequenced region at the core of 12q13.3 amplification in human cancers
Genomics
42
295-301
1997
Homo sapiens (P11802)
Manually annotated by BRENDA team
Zuo, L.; Weger, J.; Yang, Q.; Goldstein, A.M.; Tucker, M.A.; Walker, G.J.; Hayward, N.; Dracopoli, N.C.
Germline mutations in the p16INK4a binding domain of CDK4 in familial melanoma
Nat. Genet.
12
97-99
1996
Homo sapiens (P11802)
Manually annotated by BRENDA team
Wolfel, T.; Hauer, M.; Schneider, J.; Serrano, M.; Wolfel, C.; Klehmann-Hieb, E.; De Plaen, E.; Hankeln, T.; Meyer zum Buschenfelde, K.H.; Beach, D.
A p16INK4a-insensitive CDK4 mutant targeted by cytolytic T lymphocytes in a human melanoma
Science
269
1281-1284
1995
Homo sapiens (P11802), Homo sapiens
Manually annotated by BRENDA team
Khatib, Z.A.; Matsushime, H.; Valentine, M.; Shapiro, D.N.; Sherr, C.J.; Look, A.T.
Coamplification of the CDK4 gene with MDM2 and GLI in human sarcomas
Cancer Res.
53
5535-5541
1993
Homo sapiens (P11802), Homo sapiens
Manually annotated by BRENDA team
Anderson, M.; Andrews, D.M.; Barker, A.J.; Brassington, C.A.; Breed, J.; Byth, K.F.; Culshaw, J.D.; Finlay, M.R.; Fisher, E.; McMiken, H.H.; Green, C.P.; Heaton, D.W.; Nash, I.A.; Newcombe, N.J.; Oakes, S.E.; Pauptit, R.A.; Roberts, A.; Stanway, J.J.; Thomas, A.P.; Tucker, J.A.; Walker, M.; Weir, H.M.
Imidazoles: SAR and development of a potent class of cyclin-dependent kinase inhibitors
Bioorg. Med. Chem. Lett.
18
5487-5492
2008
Homo sapiens (P11802), Homo sapiens (P24941)
Manually annotated by BRENDA team