Target intelligence / Profile preview

CREB-binding protein and E1A binding protein p300 (CBP and p300)

Target
CBP and p300
Molecular classification
Transcriptional coactivator, Histone acetyltransferase, Chromatin regulator, Epigenetic modifier
01

Overview

CREB-binding protein (CBP/CREBBP) and E1A binding protein p300 (p300/EP300) are highly conserved, ubiquitously expressed transcriptional coactivators with intrinsic histone acetyltransferase activity. They facilitate gene transcription by acetylating histones and transcription factors, thereby modulating chromatin accessibility and recruiting the transcriptional apparatus. Both proteins function as platforms for integrating multiple signaling pathways, including cAMP/PKA/CREB and NF-κB, which impact cell proliferation, differentiation, DNA repair, immune responses, metabolism, and stress adaptation. They play key roles in the etiologies of cancer, neurodegenerative diseases, and metabolic disorders, and have emerged as promising (but challenging) targets for epigenetic therapies.

Other names
CBPCREBBPKAT3ARSTSp300EP300
02

Mechanism of action

Inhibition of histone acetyltransferase activity (blockade of lysine acetylation on histones and transcription factors); modulation of transcriptional coactivation; altered chromatin accessibility and gene expression profiles; disruption of protein-protein interactions with transcription factors (e.g., CREB, β-catenin, NF-κB/p65).

03

Biological functions

Gene transcription regulationChromatin remodelingSignal transductionDNA repairCell cycle regulationCell differentiationMetabolism regulationStress response
04

Disease associations

CancerNeurodegenerative diseasesDiabetesInflammation/immune disordersCardiovascular diseaseMetabolic disease
05

Safety considerations

On-target toxicityPotential for hematologic and neurological side effectsRisk of impaired DNA repair and cell cycle controlChallenges with selectivity
06

Interacting drugs

C646

1 more in the full profile.

07

Biomarkers

Gene mutations in CBP or p300Altered protein expression levelsHistone acetylation status

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