Target intelligence / Profile preview

Cyclin-dependent kinase inhibitor 2A (CDKN2A)

Target
CDKN2A
Molecular classification
Tumor Suppressor, INK4 family member
01

Overview

Cyclin-dependent kinase inhibitor 2A (CDKN2A) is a critical tumor suppressor gene that encodes two main proteins: p16(INK4A) and p14(ARF). These proteins regulate the cell cycle and prevent uncontrolled cell proliferation. p16(INK4A) inhibits CDK4 and CDK6, preventing Rb protein phosphorylation and G1 to S-phase transition. p14(ARF) activates the p53 tumor suppressor pathway by binding to MDM2 and preventing its degradation of p53, ultimately inducing G2 arrest and apoptosis. CDKN2A plays a vital role in cellular senescence. Mutations or deletions in CDKN2A are common in various cancers, and the gene is also associated with vascular disease and Moyamoya Disease. CDK inhibitors are being developed to target the pathways affected by CDKN2A loss, demonstrating its therapeutic relevance.

Other names
p16(INK4A)p14(ARF)p19ARF (mouse)
02

Mechanism of action

CDK1, CDK4, CDK5, and CDK7 inhibitor

03

Biological functions

Cell cycle regulationTumor suppressionCellular senescenceApoptosis
04

Disease associations

CancerMelanomaPancreatic cancerGlioblastomaLung cancerBreast cancerMalignant mesotheliomaThymic epithelial tumorsCoronary artery diseaseMoyamoya Disease
05

Safety considerations

Potential for disrupting normal cell cycle control leading to off-target effects.
06

Interacting drugs

Milciclib

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