S-acylation and neuroinflammation: the therapeutic potential of zDHHC and deacylase modulation

Neuroinflammation is a hallmark of many neurodegenerative diseases, including Alzheimer's, Parkinson's and Huntington's disease, multiple sclerosis, and infantile neuronal ceroid lipofuscinosis. Dynamic protein S-acylation, a reversible lipid post-translational modification, is an important regulator in these processes. S-acylation is catalysed by the zDHHC palmitoyl acyltransferases, and removal of the acyl groups is mediated by acyl-protein thioesterases. S-acylation controls the localisation, stability, and function of around 48 % of all proteins in the nervous system, including synaptic scaffolds, ion channels, immune receptors, and trafficking proteins. Moreover, dysregulated S-acylation contributes to synaptic loss, aberrant immune signalling, and neurodegeneration. This review examines proteins implicated in neuroinflammation with reported S-acylase or deacylase activity, outlines current knowledge on disease-related alterations in S-acylation, and assesses the therapeutic promise of available small-molecule modulators. Linking the activity of these enzymes with human disease highlights the potential of reversible S-acylation as a source of innovative targets for drug discovery in neuroinflammation.

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Journal
European Journal of Medicinal Chemistry
Published
2025-11-29
DOI
https://doi.org/10.1016/j.ejmech.2025.118429
Primary Topic
Peptidase Inhibition and Analysis
Type
article
Field-Weighted Citation Impact
0.00

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article

S-acylation and neuroinflammation: the therapeutic potential of zDHHC and deacylase modulation

Jennifer Greaves, Vânia M. Moreira, Jorge A. R. Salvador, Ludovico Pipitò et al.
European Journal of Medicinal Chemistry
Peptidase Inhibition and Analysis
article

S-acylation and neuroinflammation: the therapeutic potential of zDHHC and deacylase modulation

Jennifer Greaves, Vânia M. Moreira, Jorge A. R. Salvador, Ludovico Pipitò, Choa P. Ng, Tiago A Duarte
article en

Abstract

Neuroinflammation is a hallmark of many neurodegenerative diseases, including Alzheimer's, Parkinson's and Huntington's disease, multiple sclerosis, and infantile neuronal ceroid lipofuscinosis. Dynamic protein S-acylation, a reversible lipid post-translational modification, is an important regulator in these processes. S-acylation is catalysed by the zDHHC palmitoyl acyltransferases, and removal of the acyl groups is mediated by acyl-protein thioesterases. S-acylation controls the localisation, stability, and function of around 48 % of all proteins in the nervous system, including synaptic scaffolds, ion channels, immune receptors, and trafficking proteins. Moreover, dysregulated S-acylation contributes to synaptic loss, aberrant immune signalling, and neurodegeneration. This review examines proteins implicated in neuroinflammation with reported S-acylase or deacylase activity, outlines current knowledge on disease-related alterations in S-acylation, and assesses the therapeutic promise of available small-molecule modulators. Linking the activity of these enzymes with human disease highlights the potential of reversible S-acylation as a source of innovative targets for drug discovery in neuroinflammation.

European Journal of Medicinal ChemistryVol. 303
Coventry University (GB), University of Coimbra (PT)
UK Research and Innovation, Coventry University
Openalex Percentile: Top 48%
Peptidase Inhibition and Analysis
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S-acylation and neuroinflammation: the therapeutic potential of zDHHC and deacylase modulation — Jennifer Greaves, Vânia M. Moreira, et al. · European Journal of Medicinal Chemistry (2025) | TGRS Research Map | TGRS