Target intelligence / Profile preview

Retinoblastoma-associated Protein (pRb)

Target
pRb
Molecular classification
Pocket proteins, Tumor suppressor protein
01

Overview

The retinoblastoma-associated protein (pRb), encoded by the RB1 gene, is a crucial tumor suppressor protein. It regulates cell cycle progression at the G1/S transition by inhibiting E2F transcription factors. Loss or dysfunction of pRb is implicated in retinoblastoma, osteosarcoma, and other cancers. pRb is phosphorylated by cyclin-dependent kinases (CDKs), which releases E2Fs allowing cell cycle progression. Targeting the RB pathway is a potential therapeutic strategy, but direct targeting is challenging due to pRb's role as a suppressor.

Other names
RbRB1
02

Mechanism of action

Indirectly targeted via upstream regulators of phosphorylation; direct targeting challenging due to suppressor function

03

Biological functions

Cell cycle regulationTumor suppressionRegulation of G1/S transitionTranscriptional repressionInhibition of E2F transcription factors
04

Disease associations

RetinoblastomaOsteosarcomaLung cancerBladder cancerMelanomaCancer
05

Safety considerations

Restoration of RB function without causing cell cycle arrest in normal cellsIndirect targeting may have off-target effects
06

Biomarkers

RB1 expression levelRB1 mutation status

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