Target intelligence / Profile preview

Cyclin-dependent kinase 2–cyclin A or E complex (CDK2–cyclin A complex, CDK2–cyclin E complex)

Target
CDK2–cyclin A complex, CDK2–cyclin E complex
Molecular classification
Enzyme, Serine/threonine protein kinase, Kinase complex
01

Overview

The **Cyclin-dependent kinase 2–cyclin A or E complex** is a heterodimeric protein complex where CDK2, a serine/threonine kinase, binds to cyclin A or cyclin E, forming the active kinase complex required for cell cycle progression. CDK2 bound to cyclin E is key for the G1-to-S phase transition, while CDK2–cyclin A acts predominantly during S phase to facilitate DNA replication. CDK2 is activated through phosphorylation and allosteric changes upon cyclin binding, which primes the complex for substrate phosphorylation, notably of proteins such as the retinoblastoma protein, driving cell cycle transitions[1][2][3][4][5][6][7]. Dysregulation or hyperactivation of CDK2–cyclin complexes is closely associated with tumorigenesis, making the complex a validated cancer drug target[5]. Several selective inhibitors have been developed, largely aiming to arrest cell proliferation by inhibiting this kinase complex.

Other names
CDK2/cyclin A complexCDK2/cyclin E complexCDK2–cyclin complex
02

Mechanism of action

Inhibition of kinase activity (cell cycle arrest) Prevention of phosphorylation of cell cycle proteins

03

Biological functions

Cell cycle regulationDNA replicationCell proliferation
04

Disease associations

CancerOther diseases involving abnormal cell proliferation
05

Safety considerations

Bone marrow suppressionOff-target kinase inhibitionGastrointestinal toxicityRisk of impaired tissue regeneration
06

Interacting drugs

Roscovitine (Seliciclib)

3 more in the full profile.

07

Biomarkers

Phosphorylated retinoblastoma protein (pRb)Cyclin A expressionCyclin E expression

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