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.
Authors
- Jennifer Greaves
- Vânia M. Moreira (ORCID: https://orcid.org/0000-0001-6169-5035)
- Jorge A. R. Salvador (ORCID: https://orcid.org/0000-0003-0779-6083)
- Ludovico Pipitò (ORCID: https://orcid.org/0000-0002-1824-7541)
- Choa P. Ng
- Tiago A Duarte
Institutions
- Coventry University (GB)
- University of Coimbra (PT)
Publication Details
- 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
Funders
- UK Research and Innovation
- Coventry University