Target intelligence / Profile preview

Retinoblastoma-associated protein pathway (RB)

Target
RB
Molecular classification
Signaling pathway, Tumor suppressor pathway
01

Overview

The retinoblastoma protein (pRb or RB) pathway is a crucial tumor suppressor pathway that regulates cell cycle progression, differentiation, and apoptosis. Dysfunction or loss of pRb function is implicated in a wide range of cancers. The pathway is centered around the RB1 gene and its protein product, pRb, which controls the G1 to S phase transition in the cell cycle by binding to E2F transcription factors. The activity of pRb is regulated by phosphorylation, primarily by cyclin-dependent kinases (CDKs). Therapeutic strategies targeting the RB pathway, such as CDK4/6 inhibitors, aim to restore or maintain pRb function, particularly in cancers with intact RB function.

Other names
pRb pathwayRB1 pathwayRetinoblastoma protein pathway
02

Mechanism of action

CDK4/6 inhibitors prevent phosphorylation of Rb, maintaining it in an active, growth-suppressive state.

03

Biological functions

Cell cycle regulationCell differentiationApoptosisChromatin remodelingTranscriptional regulation
04

Disease associations

CancerRetinoblastomaOsteosarcoma
05

Safety considerations

Resistance to CDK4/6 inhibitorsPotential for off-target effects due to pathway complexity
06

Interacting drugs

CDK4/6 inhibitors
07

Biomarkers

RB1 expressionpRb phosphorylation statusRB1 mutations

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