Target intelligence / Profile preview

K(lysine) acetyltransferase 2B (PCAF)

Target
PCAF
Molecular classification
Enzyme, Histone acetyltransferase, Transcription coregulator, Chromatin modifier
01

Overview

K(lysine) acetyltransferase 2B (PCAF) is a nuclear enzyme that acts as a histone acetyltransferase, facilitating acetylation of histone and non-histone proteins to regulate chromatin structure and gene expression[1][3][4]. It interacts with transcriptional coactivators p300 and CBP, playing a crucial role in transcriptional activation in response to cellular signals and stress[1][6]. PCAF is involved in various biological processes including cell cycle progression, apoptosis, differentiation, autophagy, and metabolic regulation. Aberrant expression or function of PCAF is implicated in several cancers, particularly hepatocellular carcinoma, where its downregulation is linked to disease progression and poor prognosis[4]. PCAF serves as a coactivator for multiple transcription factors, such as ATF4 and p53, and its acetyltransferase activity can be regulated by autoacetylation and interaction with other epigenetic modifiers[1][6].

Other names
p300/CBP-associated factorPCAFKAT2B
02

Mechanism of action

Inhibition of acetyltransferase activity (blocks acetylation of histones and non-histone proteins, affecting gene expression and cell fate); Modulation of protein-protein interactions affecting transcriptional regulation

03

Biological functions

Transcriptional regulationChromatin remodelingCell cycle progressionCell differentiationApoptosisModulation of autophagyAngiogenesisGluconeogenesis
04

Disease associations

Cancer (e.g., hepatocellular carcinoma, through downregulation or dysregulation of PCAF)Other (Role in cell survival and response to nutrient stress)
05

Safety considerations

Potential off-target effects due to the broad role of acetyltransferases in gene regulationPossible impact on normal cellular differentiation and survival
06

Interacting drugs

garcinol

2 more in the full profile.

07

Biomarkers

PCAF expression level (notably decreased in hepatocellular carcinoma, correlated with survival after surgery)Histone acetylation marks (e.g., H3K14ac)

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