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.