Modulators for palmitoylation of proteins and small molecules

Eur J Med Chem. 2024 May 5:271:116408. doi: 10.1016/j.ejmech.2024.116408.

Zeshuai Fan ¹, Yuchen Hao ¹, Yidan Huo ¹, Fei Cao ², Longfei Li ², Jianmei Xu ³, Yali Song ², Kan Yang ⁴

Affiliations

1 Key Laboratory of Pharmaceutical Quality Control of Hebei Province, College of Pharmaceutical Sciences, Hebei University, Baoding, 071002, China.
2 Key Laboratory of Pharmaceutical Quality Control of Hebei Province, College of Pharmaceutical Sciences, Hebei University, Baoding, 071002, China; Key Laboratory of Medicinal Chemistry and Molecular Diagnosis, Ministry of Education, Hebei University, Baoding, Hebei, 071002, China.
3 Department of hematopathology, Affiliated Hospital of Hebei University, Hebei University, Baoding, 071002, China.
4 Key Laboratory of Pharmaceutical Quality Control of Hebei Province, College of Pharmaceutical Sciences, Hebei University, Baoding, 071002, China; Key Laboratory of Medicinal Chemistry and Molecular Diagnosis, Ministry of Education, Hebei University, Baoding, Hebei, 071002, China. Electronic address: [email protected].

PMID: 38621327 DOI: 10.1016/j.ejmech.2024.116408

Abstract

As an essential form of lipid modification for maintaining vital cellular functions, palmitoylation plays an important role in in the regulation of various physiological processes, serving as a promising therapeutic target for diseases like Cancer and neurological disorders. Ongoing research has revealed that palmitoylation can be categorized into three distinct types: N-palmitoylation, O-palmitoylation and S-palmitoylation. Herein this paper provides an overview of the regulatory Enzymes involved in palmitoylation, including palmitoyltransferases and depalmitoylases, and discusses the currently available broad-spectrum and selective inhibitors for these Enzymes.

Keywords

Depalmitoylases; Inhibitors; Palmitoylation; Palmitoyltransferases.

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