DGIdb - CDK4 Gene Record

CDK4 1019 Druggable GenomeClinically ActionableDrug Resistance

Alternate Names:

1019
CYCLIN DEPENDENT KINASE 4
CDK4
CMM3
PSK-J3
123829
1773
ENSG00000135446
OTTHUMG00000170382
CDK 4,6
CDK 1,2,4,5,6,7,9 (pan-CDK)
P11802
cyclin-dependent kinase 4
CDK4_HUMAN
TTDC00165
CELL DIVISION PROTEIN KINASE 4
1976
NP_000066
NM_000075
CELL DIVISION PROTEIN KINASE 4 (EC 2.7.1.37) (CYCLIN-DEPENDENT KINASE 4) (PSK-J3). [SOURCE:UNIPROT/SWISSPROT;ACC:P11802]
13
BE0002216
PA102
T85799

Gene Info:

Human Readable Name	SERINE THREONINE KINASE
Interpro Type	Domain
Uniprot Status	Swiss-Prot
Interpro Name	Serine/threonine- / dual-specificity protein kinase, catalytic domain
Human Readable Name	DRUGGABLE GENOME
Interpro Acc	IPR002290
Human Readable Name	KINASE
Interpro Short Name	Ser/Thr_dual-sp_kinase_dom
Uniprot Evidence	1: Evidence at protein level
GuideToPharmacology Gene Category Name	CDK4 subfamily
GuideToPharmacology Gene Category ID	488
GuideToPharmacology Gene Type	enzyme
Target Class	Enzymes
Target Subclass	EC:2.7.11.22
CancerCommons Reported Gene Name	CDK4/6
CancerCommons Reported Gene Name	Pan CDK
Source Reported Gene Name	CDK4
Initial Gene Query	CDK4
Counted Citations from 1950-2000	3030
Gene Biotype	PROTEIN_CODING

(26 More Sources)

Gene Categories: Category Details

TRANSCRIPTION FACTOR COMPLEX
TUMOR SUPPRESSOR
KINASE
SERINE THREONINE KINASE
DRUG RESISTANCE
DRUGGABLE GENOME
CLINICALLY ACTIONABLE
TRANSCRIPTION FACTOR

Publications:

Dickson et al., 2016, Progression-Free Survival Among Patients With Well-Differentiated or Dedifferentiated Liposarcoma Treated With CDK4 Inhibitor Palbociclib: A Phase 2 Clinical Trial., JAMA Oncol
Dickson et al., 2013, Phase II trial of the CDK4 inhibitor PD0332991 in patients with advanced CDK4-amplified well-differentiated or dedifferentiated liposarcoma., J. Clin. Oncol.
Perez et al., 2015, Efficacy of CDK4 inhibition against sarcomas depends on their levels of CDK4 and p16ink4 mRNA., Oncotarget
Fry et al., 2004, Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts., Mol. Cancer Ther.
Reddy MV et al., 2014, Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5)., J Med Chem
Rocca A et al., 2017, Progress with palbociclib in breast cancer: latest evidence and clinical considerations., Ther Adv Med Oncol
Burgess A et al., 2006, Inhibition of S/G2 phase CDK4 reduces mitotic fidelity., J Biol Chem
Gelbert et al., 2014, Preclinical characterization of the CDK4/6 inhibitor LY2835219: in-vivo cell cycle-dependent/independent anti-tumor activities alone/in combination with gemcitabine., Invest New Drugs
Vora et al., 2014, CDK 4/6 inhibitors sensitize PIK3CA mutant breast cancer to PI3K inhibitors., Cancer Cell
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Rhee et al., 1995, c-Myc and cyclin D3 (CcnD3) genes are independent targets for glucocorticoid inhibition of lymphoid cell proliferation., Cancer Res.
Swarbrick et al., 2000, Cooperation of p27(Kip1) and p18(INK4c) in progestin-mediated cell cycle arrest in T-47D breast cancer cells., Mol. Cell. Biol.
Rader et al., 2013, Dual CDK4/CDK6 inhibition induces cell-cycle arrest and senescence in neuroblastoma., Clin. Cancer Res.
Banerji et al., 2005, Pharmacokinetic-pharmacodynamic relationships for the heat shock protein 90 molecular chaperone inhibitor 17-allylamino, 17-demethoxygeldanamycin in human ovarian cancer xenograft models., Clin. Cancer Res.
Park et al., 2000, Involvement of retinoblastoma family members and E2F/DP complexes in the death of neurons evoked by DNA damage., J. Neurosci.
Montagnoli A et al., 2008, A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity., Nat Chem Biol
Frazer-Abel et al., 2004, Nicotine activates nuclear factor of activated T cells c2 (NFATc2) and prevents cell cycle entry in T cells., J. Pharmacol. Exp. Ther.
Rolf MG et al., 2015, In vitro pharmacological profiling of R406 identifies molecular targets underlying the clinical effects of fostamatinib., Pharmacol Res Perspect

PALBOCICLIB CDK4

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Reported Cancer Type Melanoma

Mechanism of Interaction CDK4/cyclin D1 inhibitor

Direct Interaction yes

Publications:

Dickson et al., 2016, Progression-Free Survival Among Patients With Well-Differentiated or Dedifferentiated Liposarcoma Treated With CDK4 Inhibitor Palbociclib: A Phase 2 Clinical Trial., JAMA Oncol

Dickson et al., 2013, Phase II trial of the CDK4 inhibitor PD0332991 in patients with advanced CDK4-amplified well-differentiated or dedifferentiated liposarcoma., J. Clin. Oncol.

Perez et al., 2015, Efficacy of CDK4 inhibition against sarcomas depends on their levels of CDK4 and p16ink4 mRNA., Oncotarget

ABEMACICLIB CDK4

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction CDK4/cyclin D1 complex expressed in and purified from insect cells. Assays used the methanesulfonate salt of the compound.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Publications:

Gelbert et al., 2014, Preclinical characterization of the CDK4/6 inhibitor LY2835219: in-vivo cell cycle-dependent/independent anti-tumor activities alone/in combination with gemcitabine., Invest New Drugs

chembl:CHEMBL1956070 CDK4

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

Publications:

Burgess A et al., 2006, Inhibition of S/G2 phase CDK4 reduces mitotic fidelity., J Biol Chem
ALVOCIDIB CDK4

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclin-dependent kinase 4 inhibitor

Direct Interaction yes

Novel drug target Novel Target

Publications:

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
RIBOCICLIB CDK4

Interaction Types & Directionality:

inhibitor (inhibitory)

antagonist (inhibitory)

Interaction Info:

Trial Name LEE011

Novel drug target Novel Target

Specific Action of the Ligand Inhibition

Publications:

Rader et al., 2013, Dual CDK4/CDK6 inhibition induces cell-cycle arrest and senescence in neuroblastoma., Clin. Cancer Res.
AT-7519 CDK4

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Cyclin-dependent kinase inhibitor

Specific Action of the Ligand Inhibition

Publications:
PHA-793887 CDK4

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclin-dependent kinase inhibitor

Direct Interaction yes

Publications:
RIVICICLIB CDK4

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclin-dependent kinase 4 inhibitor

Direct Interaction yes

Details of the Assay for Interaction CDK4/cyclin D1 complex

Publications:
FASCAPLYSIN CDK4

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Publications:
AZD-5438 CDK4

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Cyclin-dependent kinase inhibitor

Publications:
G1T28-1 CDK4

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclin-dependent kinase 4 inhibitor

Direct Interaction yes

Publications:
AG-24322 CDK4

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclin-dependent kinase 4 inhibitor

Direct Interaction yes

Publications:
BMS-387032 CDK4

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Publications:
TRILACICLIB CDK4

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Inhibition of CDK4/cyclin D3

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Publications:
MILCICLIB CDK4

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclin-dependent kinase 4 inhibitor

Direct Interaction yes

Details of the Assay for Interaction CDK4/cyclin D1 complex

Publications:
LEROCICLIB CDK4

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Inhibition of CDK4/cyclin D1

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Publications:
RGB-286638 CDK4

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Cyclin-dependent kinase 4 inhibitor

Details of the Assay for Interaction in association with cyclin D1

Publications:
RONICICLIB CDK4

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclin-dependent kinase inhibitor

Direct Interaction yes

Publications:
RIBOCICLIB SUCCINATE CDK4

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclin-dependent kinase 4 inhibitor

Direct Interaction yes

Publications:
VORUCICLIB CDK4

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Inhibition of CDK4/cyclinD1.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Publications:
RG-547 CDK4

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclin-dependent kinase 4 inhibitor

Direct Interaction yes

Publications:
UCN-01 CDK4

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclin-dependent kinase 4 inhibitor

Direct Interaction yes

Publications:
FOSTAMATINIB CDK4

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

Rolf MG et al., 2015, In vitro pharmacological profiling of R406 identifies molecular targets underlying the clinical effects of fostamatinib., Pharmacol Res Perspect
chembl:CHEMBL1956069 CDK4

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Burgess A et al., 2006, Inhibition of S/G2 phase CDK4 reduces mitotic fidelity., J Biol Chem
ALPELISIB CDK4

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Vora et al., 2014, CDK 4/6 inhibitors sensitize PIK3CA mutant breast cancer to PI3K inhibitors., Cancer Cell
DEXAMETHASONE CDK4

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Rhee et al., 1995, c-Myc and cyclin D3 (CcnD3) genes are independent targets for glucocorticoid inhibition of lymphoid cell proliferation., Cancer Res.
PROGESTERONE CDK4

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Swarbrick et al., 2000, Cooperation of p27(Kip1) and p18(INK4c) in progestin-mediated cell cycle arrest in T-47D breast cancer cells., Mol. Cell. Biol.

TANESPIMYCIN CDK4

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Banerji et al., 2005, Pharmacokinetic-pharmacodynamic relationships for the heat shock protein 90 molecular chaperone inhibitor 17-allylamino, 17-demethoxygeldanamycin in human ovarian cancer xenograft models., Clin. Cancer Res.

CAMPTOTHECIN CDK4

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Park et al., 2000, Involvement of retinoblastoma family members and E2F/DP complexes in the death of neurons evoked by DNA damage., J. Neurosci.
chembl:CHEMBL225519 CDK4

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Montagnoli A et al., 2008, A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity., Nat Chem Biol
NICOTINE CDK4

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Frazer-Abel et al., 2004, Nicotine activates nuclear factor of activated T cells c2 (NFATc2) and prevents cell cycle entry in T cells., J. Pharmacol. Exp. Ther.
APREMILAST CDK4

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL319467 CDK4

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Ensembl: ENSG00000135446
- Version: 101_38
Alternate Names:

CDK4 Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
HopkinsGroom: P11802
- Version: 11-September-2012
Alternate Names:

CDK4 Uniprot Gene Name

1019 Entrez Gene Id

ENSG00000135446 Ensembl Gene Id

Gene Info:

Interpro Type Domain

Uniprot Status Swiss-Prot

Interpro Name Serine/threonine- / dual-specificity protein kinase, catalytic domain

Gene Categories:

KINASE, DRUGGABLE GENOME

Publications:
RussLampel: ENSG00000135446
- Version: 26-July-2011
Alternate Names:

CELL DIVISION PROTEIN KINASE 4 (EC 2.7.1.37) (CYCLIN-DEPENDENT KINASE 4) (PSK-J3). [SOURCE:UNIPROT/SWISSPROT;ACC:P11802] Description

ENSG00000135446 Ensembl Gene Id

CDK4 Display Id

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:
CancerCommons: CDK4
- Version: 25-July-2013
Alternate Names:

1019 Entrez Gene ID

Gene Info:

CancerCommons Reported Gene Name CDK4/6

CancerCommons Reported Gene Name Pan CDK

Publications:
BaderLabGenes: CDK4
- Version: February-2014
Alternate Names:

1019 Entrez Gene ID

Gene Info:

Initial Gene Query CDK4

Counted Citations from 1950-2000 3030

Gene Categories:

KINASE

Publications:
TdgClinicalTrial: P11802
- Version: January-2014
Alternate Names:

CDK4 Gene Symbol

Gene Info:

Target Class Enzymes

Target Subclass EC:2.7.11.22

Publications:
GuideToPharmacologyGenes: 1976
- Version: 4-March-2015
Alternate Names:

cyclin-dependent kinase 4 HUGO Gene Name

1773 HUGO Gene ID

CDK4 Gene Symbol

Gene Info:

GuideToPharmacology Gene Category Name CDK4 subfamily

GuideToPharmacology Gene Category ID 488

GuideToPharmacology Gene Type enzyme

Gene Categories:

SERINE THREONINE KINASE, KINASE

Publications:
PharmGKB: CDK4
- Version: 18-August-2020
Alternate Names:

PA102 PharmGKB ID

Gene Info:

Publications:

Stevens A et al., 2014, Pharmacogenomics of insulin-like growth factor-I generation during GH treatment in children with GH deficiency or Turner syndrome., Pharmacogenomics J

DrugBank: BE0002216

Version: 5.1.7

Alternate Names:

CDK4 DrugBank Gene Name

P11802 UniProt Accession

1019 Entrez Gene Id

Gene Info:

Publications:

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

Rocca A et al., 2017, Progress with palbociclib in breast cancer: latest evidence and clinical considerations., Ther Adv Med Oncol

Fry et al., 2004, Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts., Mol. Cancer Ther.

NCI: CDK4

Version: 14-September-2017

Alternate Names:

Gene Info:

Publications:

Grillo et al., 2006, Validation of cyclin D1/CDK4 as an anticancer drug target in MCF-7 breast cancer cells: Effect of regulated overexpression of cyclin D1 and siRNA-mediated inhibition of endogenous cyclin D1 and CDK4 expression., Breast Cancer Res. Treat.

Hu et al., 2001, Differential effects of transforming growth factor on cell cycle regulatory molecules in human myeloid leukemia cells., Oncogene

Banerji et al., 2005, Pharmacokinetic-pharmacodynamic relationships for the heat shock protein 90 molecular chaperone inhibitor 17-allylamino, 17-demethoxygeldanamycin in human ovarian cancer xenograft models., Clin. Cancer Res.

DTC: CDK4

Version: 02-September-2020

Alternate Names:

Gene Info:

Publications:

Burgess A et al., 2006, Inhibition of S/G2 phase CDK4 reduces mitotic fidelity., J Biol Chem

Montagnoli A et al., 2008, A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity., Nat Chem Biol

Reddy MV et al., 2014, Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5)., J Med Chem

HingoraniCasas: ENSG00000135446
- Version: 31-May-2017
Alternate Names:

ENSG00000135446 Gene Symbol

CDK4 Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
MyCancerGenome: CDK4
- Version: 20-Jun-2017
Alternate Names:

1019 Entrez Gene Id

CDK4 MyCancerGenome Gene Symbol

CDK 1,2,4,5,6,7,9 (pan-CDK) MyCancerGenome Reported Gene Name

Gene Info:

Publications:
TALC: CDK4
- Version: 12-May-2016
Alternate Names:

CDK4 Gene Symbol

Gene Info:

Publications:
ChemblInteractions: CDK4
- Version: chembl_23
Alternate Names:

CDK4 GENE_SYMBOL

Cyclin-dependent kinase 4 UNIPROT

Cell division protein kinase 4 UNIPROT

Gene Info:

Publications:
GuideToPharmacologyInteractions: ENSG00000135446
- Version: 20-July-2020
Alternate Names:

cyclin dependent kinase 4 GuideToPharmacology Name

P11802 UniProtKB ID

Gene Info:

Publications:
OncoKB: CDK4
- Version: 23-July-2020
Alternate Names:

1019 OncoKB Entrez Id

PSK-J3 OncoKB Gene Synonym

CMM3 OncoKB Gene Synonym

Gene Info:

Publications:
TTD: Cyclin-dependent kinase 4
- Version: 2020.06.01
Alternate Names:

CDK4 TTD Gene Abbreviation

T85799 TTD Target ID

Gene Info:

Publications:
Pharos: CDK4
- Version: 03-September-2020
Alternate Names:

Cyclin-dependent kinase 4 Gene Name

P11802 UniProt ID

Gene Info:

Gene Categories:

KINASE, TRANSCRIPTION FACTOR

Publications:
Tempus: CDK4
- Version: 11-November-2018
Alternate Names:

CDK4 Gene Symbol

Gene Info:

Publications:
dGene: CDK4
- Version: 27-Jun-2013
Alternate Names:

1019 Gene ID

CMM3 dGene Synonym

PSK-J3 dGene Synonym

Gene Info:

Gene Categories:

SERINE THREONINE KINASE, KINASE

Publications:
ClearityFoundationClinicalTrial: CDK4
- Version: 15-June-2013
Alternate Names:

Gene Info:

Publications:
MyCancerGenomeClinicalTrial: CDK4
- Version: 30-February-2014
Alternate Names:

Gene Info:

Publications:
ClearityFoundationBiomarkers: CDK4
- Version: 26-July-2013
Alternate Names:

Gene Info:

Publications:
MskImpact: CDK4
- Version: May-2015
Alternate Names:

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
FoundationOneGenes: CDK4
- Version: 03-September-2020
Alternate Names:

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
CarisMolecularIntelligence: CDK4
- Version: 04-September-2020
Alternate Names:

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
GO: CDK4
- Version: 05-September-2020
Alternate Names:

Gene Info:

Gene Categories:

TUMOR SUPPRESSOR, TRANSCRIPTION FACTOR COMPLEX, DRUG RESISTANCE

Publications:
Oncomine: CDK4
- Version: v3
Alternate Names:

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
CGI: CDK4
- Version: 14-September-2020
Alternate Names:

Gene Info:

Publications:

Reported Cancer Type	Melanoma
Mechanism of Interaction	CDK4/cyclin D1 inhibitor
Direct Interaction	yes

Details of the Assay for Interaction	CDK4/cyclin D1 complex expressed in and purified from insect cells. Assays used the methanesulfonate salt of the compound.
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

Mechanism of Interaction	Cyclin-dependent kinase 4 inhibitor
Direct Interaction	yes
Novel drug target	Novel Target

Trial Name	LEE011
Novel drug target	Novel Target
Specific Action of the Ligand	Inhibition

Direct Interaction	yes
Mechanism of Interaction	Cyclin-dependent kinase inhibitor
Specific Action of the Ligand	Inhibition

Direct Interaction?	True
Endogenous Drug?	False
Specific Action of the Ligand	Inhibition

Details of the Assay for Interaction	Inhibition of CDK4/cyclin D3
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

Details of the Assay for Interaction	Inhibition of CDK4/cyclin D1
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

Details of the Assay for Interaction	Inhibition of CDK4/cyclinD1.
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

CDK4	Uniprot Gene Name
1019	Entrez Gene Id
ENSG00000135446	Ensembl Gene Id

CELL DIVISION PROTEIN KINASE 4 (EC 2.7.1.37) (CYCLIN-DEPENDENT KINASE 4) (PSK-J3). [SOURCE:UNIPROT/SWISSPROT;ACC:P11802]	Description
ENSG00000135446	Ensembl Gene Id
CDK4	Display Id

cyclin-dependent kinase 4	HUGO Gene Name
1773	HUGO Gene ID
CDK4	Gene Symbol

CDK4	DrugBank Gene Name
P11802	UniProt Accession
1019	Entrez Gene Id

CDK4	GENE_SYMBOL
Cyclin-dependent kinase 4	UNIPROT
Cell division protein kinase 4	UNIPROT

cyclin dependent kinase 4	GuideToPharmacology Name
P11802	UniProtKB ID

1019	OncoKB Entrez Id
PSK-J3	OncoKB Gene Synonym
CMM3	OncoKB Gene Synonym

CDK4 Gene Record

CDK4 1019 Druggable GenomeClinically ActionableDrug Resistance

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Reported Cancer Type Melanoma Mechanism of Interaction CDK4/cyclin D1 inhibitor Direct Interaction yes

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Details of the Assay for Interaction CDK4/cyclin D1 complex expressed in and purified from insect cells. Assays used the methanesulfonate salt of the compound. Specific Action of the Ligand Inhibition Endogenous Drug? False

Publications: Gelbert et al., 2014, Preclinical characterization of the CDK4/6 inhibitor LY2835219: in-vivo cell cycle-dependent/independent anti-tumor activities alone/in combination with gemcitabine., Invest New Drugs

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False Direct Interaction? True

Publications: Burgess A et al., 2006, Inhibition of S/G2 phase CDK4 reduces mitotic fidelity., J Biol Chem

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Cyclin-dependent kinase 4 inhibitor Direct Interaction yes Novel drug target Novel Target

Publications: Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

Interaction Types & Directionality: inhibitor (inhibitory) antagonist (inhibitory)

Interaction Info: Trial Name LEE011 Novel drug target Novel Target Specific Action of the Ligand Inhibition

Publications: Rader et al., 2013, Dual CDK4/CDK6 inhibition induces cell-cycle arrest and senescence in neuroblastoma., Clin. Cancer Res.

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Cyclin-dependent kinase inhibitor Specific Action of the Ligand Inhibition

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Cyclin-dependent kinase inhibitor Direct Interaction yes

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Cyclin-dependent kinase 4 inhibitor Direct Interaction yes Details of the Assay for Interaction CDK4/cyclin D1 complex

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction? True Endogenous Drug? False Specific Action of the Ligand Inhibition

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Cyclin-dependent kinase inhibitor

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Cyclin-dependent kinase 4 inhibitor Direct Interaction yes

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Cyclin-dependent kinase 4 inhibitor Direct Interaction yes

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction? False Endogenous Drug? False Specific Action of the Ligand Inhibition

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Details of the Assay for Interaction Inhibition of CDK4/cyclin D3 Specific Action of the Ligand Inhibition Endogenous Drug? False

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Cyclin-dependent kinase 4 inhibitor Direct Interaction yes Details of the Assay for Interaction CDK4/cyclin D1 complex

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Details of the Assay for Interaction Inhibition of CDK4/cyclin D1 Specific Action of the Ligand Inhibition Endogenous Drug? False

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Cyclin-dependent kinase 4 inhibitor Details of the Assay for Interaction in association with cyclin D1

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Cyclin-dependent kinase inhibitor Direct Interaction yes

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Cyclin-dependent kinase 4 inhibitor Direct Interaction yes

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Details of the Assay for Interaction Inhibition of CDK4/cyclinD1. Specific Action of the Ligand Inhibition Endogenous Drug? False

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Cyclin-dependent kinase 4 inhibitor Direct Interaction yes

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Cyclin-dependent kinase 4 inhibitor Direct Interaction yes

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

Publications: Rolf MG et al., 2015, In vitro pharmacological profiling of R406 identifies molecular targets underlying the clinical effects of fostamatinib., Pharmacol Res Perspect

Interaction Types & Directionality: n/a

Interaction Info:

Publications: Burgess A et al., 2006, Inhibition of S/G2 phase CDK4 reduces mitotic fidelity., J Biol Chem

Interaction Types & Directionality: n/a

Interaction Info:

Publications: Vora et al., 2014, CDK 4/6 inhibitors sensitize PIK3CA mutant breast cancer to PI3K inhibitors., Cancer Cell

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Reported Cancer Type Melanoma

Mechanism of Interaction CDK4/cyclin D1 inhibitor

Direct Interaction yes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction CDK4/cyclin D1 complex expressed in and purified from insect cells. Assays used the methanesulfonate salt of the compound.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Publications:

Gelbert et al., 2014, Preclinical characterization of the CDK4/6 inhibitor LY2835219: in-vivo cell cycle-dependent/independent anti-tumor activities alone/in combination with gemcitabine., Invest New Drugs

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

Publications:

Burgess A et al., 2006, Inhibition of S/G2 phase CDK4 reduces mitotic fidelity., J Biol Chem

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclin-dependent kinase 4 inhibitor

Direct Interaction yes

Novel drug target Novel Target

Publications:

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

Interaction Types & Directionality:

inhibitor (inhibitory)

antagonist (inhibitory)

Interaction Info:

Trial Name LEE011

Novel drug target Novel Target

Specific Action of the Ligand Inhibition

Publications:

Rader et al., 2013, Dual CDK4/CDK6 inhibition induces cell-cycle arrest and senescence in neuroblastoma., Clin. Cancer Res.

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Cyclin-dependent kinase inhibitor

Specific Action of the Ligand Inhibition

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclin-dependent kinase inhibitor

Direct Interaction yes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclin-dependent kinase 4 inhibitor

Direct Interaction yes

Details of the Assay for Interaction CDK4/cyclin D1 complex

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Cyclin-dependent kinase inhibitor

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclin-dependent kinase 4 inhibitor

Direct Interaction yes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclin-dependent kinase 4 inhibitor

Direct Interaction yes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Inhibition of CDK4/cyclin D3

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclin-dependent kinase 4 inhibitor

Direct Interaction yes

Details of the Assay for Interaction CDK4/cyclin D1 complex

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Inhibition of CDK4/cyclin D1

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Cyclin-dependent kinase 4 inhibitor

Details of the Assay for Interaction in association with cyclin D1

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclin-dependent kinase inhibitor

Direct Interaction yes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclin-dependent kinase 4 inhibitor

Direct Interaction yes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Inhibition of CDK4/cyclinD1.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclin-dependent kinase 4 inhibitor

Direct Interaction yes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclin-dependent kinase 4 inhibitor

Direct Interaction yes

Interaction Types & Directionality:

inhibitor (inhibitory)

Publications:

Rolf MG et al., 2015, In vitro pharmacological profiling of R406 identifies molecular targets underlying the clinical effects of fostamatinib., Pharmacol Res Perspect

Interaction Types & Directionality:

n/a

Publications:

Burgess A et al., 2006, Inhibition of S/G2 phase CDK4 reduces mitotic fidelity., J Biol Chem

Interaction Types & Directionality:

n/a

Publications:

Vora et al., 2014, CDK 4/6 inhibitors sensitize PIK3CA mutant breast cancer to PI3K inhibitors., Cancer Cell

Interaction Types & Directionality:

n/a

Publications:

Rhee et al., 1995, c-Myc and cyclin D3 (CcnD3) genes are independent targets for glucocorticoid inhibition of lymphoid cell proliferation., Cancer Res.

Interaction Types & Directionality:

n/a

Publications:

Swarbrick et al., 2000, Cooperation of p27(Kip1) and p18(INK4c) in progestin-mediated cell cycle arrest in T-47D breast cancer cells., Mol. Cell. Biol.

Interaction Types & Directionality:

n/a

Publications:

Banerji et al., 2005, Pharmacokinetic-pharmacodynamic relationships for the heat shock protein 90 molecular chaperone inhibitor 17-allylamino, 17-demethoxygeldanamycin in human ovarian cancer xenograft models., Clin. Cancer Res.

Interaction Types & Directionality:

n/a

Publications:

Park et al., 2000, Involvement of retinoblastoma family members and E2F/DP complexes in the death of neurons evoked by DNA damage., J. Neurosci.

Interaction Types & Directionality:

n/a

Publications:

Montagnoli A et al., 2008, A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity., Nat Chem Biol

Interaction Types & Directionality:

n/a

Publications:

Frazer-Abel et al., 2004, Nicotine activates nuclear factor of activated T cells c2 (NFATc2) and prevents cell cycle entry in T cells., J. Pharmacol. Exp. Ther.

Interaction Types & Directionality:

n/a

Interaction Types & Directionality:

n/a

Alternate Names:

CDK4 Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Alternate Names:

CDK4 Uniprot Gene Name

1019 Entrez Gene Id

ENSG00000135446 Ensembl Gene Id

Gene Info:

Interpro Type Domain

Uniprot Status Swiss-Prot

Interpro Name Serine/threonine- / dual-specificity protein kinase, catalytic domain

Gene Categories:

KINASE, DRUGGABLE GENOME

Alternate Names:

CELL DIVISION PROTEIN KINASE 4 (EC 2.7.1.37) (CYCLIN-DEPENDENT KINASE 4) (PSK-J3). [SOURCE:UNIPROT/SWISSPROT;ACC:P11802] Description

ENSG00000135446 Ensembl Gene Id

CDK4 Display Id

Gene Info:

Human Readable Name DRUGGABLE GENOME