Drug intelligence / Profile preview

P300i

Development stage
Preclinical
Lead developer
University of North Texas Health Science Center
Modality
Small Molecules
01

Overview

P300i (p300 inhibitor) refers to a class of small molecules that inhibit the histone acetyltransferase (HAT) activity of the p300 protein (also known as EP300). In the context of the provided research, P300i specifically refers to a tool compound, likely the small molecule **C646**, used to modulate the function of FoxP3+ regulatory T cells (Tregs). p300 is a critical co-activator that acetylates FoxP3, thereby increasing its protein stability and transcriptional activity. Inhibition of p300 leads to reduced Treg suppressive capacity and altered Treg distribution. In aged mouse models of multiple sclerosis (EAE), treatment with a p300 inhibitor has been shown to mitigate disease severity by preventing the accumulation of pathogenic Tregs in the choroid plexus and facilitating the entry of reparative, myelin-specific Tregs into the central nervous system to repair neuroinflammatory damage.

Other names
p300 inhibitorp-300 inhibitorp 300 inhibitorEP300 inhibitorEP-300 inhibitorEP 300 inhibitorC646C-646C 646
02

Targets

EP300 (Histone acetyltransferase p300 (EP300) catalytic domain)CREBBP (CREB-binding protein)

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