Target intelligence / Profile preview

Cyclin-dependent kinases 4 and 6 (CDK4/6)

Target
CDK4/6
Molecular classification
Enzyme, Kinase, Serine/threonine kinase
01

Overview

Cyclin-dependent kinases 4 and 6 (CDK4/6) are serine/threonine kinases that play a central role in regulating the cell cycle, specifically the transition from G1 phase to S phase. They function as part of complexes with D-type cyclins, and their activity is essential for cell proliferation. Dysregulation of the cyclin D–CDK4/6–Rb axis is common in many cancers. Selective inhibitors targeting CDK4/6 have become important therapies for certain cancers, primarily hormone receptor-positive/HER2-negative breast cancer.

02

Mechanism of action

Selective inhibition of CDK4/6, leading to RB-dependent proliferative arrest and potential impacts on DNA repair mechanisms and immune modulation within tumors.

03

Biological functions

Cell cycleCell proliferationDNA repairChromatin remodelingCellular metabolismDifferentiationApoptosis regulationAngiogenesisInflammatory cytokine productionSenescence
04

Disease associations

Cancer
05

Safety considerations

Development of resistance via upregulation/amplification/mutation of target genesActivation of alternative pathways such as Cyclin E-CDK2Increased expression/activity of upstream regulators like CDK7
06

Interacting drugs

Palbociclib

2 more in the full profile.

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