A mini review of small-molecule inhibitors targeting palmitoyltransferases
Palmitoylation occurs when fatty acids (such as palmitic acid) create covalent bonds between cysteine, serine, threonine, or other residues in proteins. The downstream effect of palmitoylation depends on the protein being palmitoylated because its blockage can render the protein useless in terms of...
| Main Authors: | , , , , , , , |
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| Format: | Article |
| Language: | English |
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Elsevier
2022-08-01
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| Series: | European Journal of Medicinal Chemistry Reports |
| Subjects: | |
| Online Access: | http://www.sciencedirect.com/science/article/pii/S2772417422000139 |
| _version_ | 1817987375057338368 |
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| author | Xiaotong Hu Xinyue Zhu Wei Yu Yiwen Zhang Kan Yang Zhenming Liu Xiaoqiang Qiao Yali Song |
| author_facet | Xiaotong Hu Xinyue Zhu Wei Yu Yiwen Zhang Kan Yang Zhenming Liu Xiaoqiang Qiao Yali Song |
| author_sort | Xiaotong Hu |
| collection | DOAJ |
| description | Palmitoylation occurs when fatty acids (such as palmitic acid) create covalent bonds between cysteine, serine, threonine, or other residues in proteins. The downstream effect of palmitoylation depends on the protein being palmitoylated because its blockage can render the protein useless in terms of its physiological function. Based on this, modulating the palmitoylation process becomes a good strategy for influencing cell proliferation, differentiation, metabolism, and apoptosis, allowing diabetes, obesity, and even cancer to be efficiently treated. As a determinant of the palmitoylation process, palmitoyltransferase is defined as an enzyme that catalyzes the transfer of the palmitate groups from Self-palmitoylated palmitoyl coenzyme A to another substrate. When it comes to the three most commonly cited palmitoyltransferases, serine palmitoyltransferase (SPT), carnitine palmitoyltransferase (CPT), and protein palmitoyltransferase (PAT), some similarities were found in the procedures by which they function, and in the structures of the small-molecule drugs that inhibit them. For this reason, we introduce the three above-mentioned palmitoyltransferases and describe the development of small molecule inhibitors for them to provide inspiration for the discovery of palmitoyltransferase inhibitors. |
| first_indexed | 2024-04-14T00:21:09Z |
| format | Article |
| id | doaj.art-cac9cc3fe1ae42b7a3862b87efc548a8 |
| institution | Directory Open Access Journal |
| issn | 2772-4174 |
| language | English |
| last_indexed | 2024-04-14T00:21:09Z |
| publishDate | 2022-08-01 |
| publisher | Elsevier |
| record_format | Article |
| series | European Journal of Medicinal Chemistry Reports |
| spelling | doaj.art-cac9cc3fe1ae42b7a3862b87efc548a82022-12-22T02:22:58ZengElsevierEuropean Journal of Medicinal Chemistry Reports2772-41742022-08-015100041A mini review of small-molecule inhibitors targeting palmitoyltransferasesXiaotong Hu0Xinyue Zhu1Wei Yu2Yiwen Zhang3Kan Yang4Zhenming Liu5Xiaoqiang Qiao6Yali Song7Key Laboratory of Pharmaceutical Quality Control of Hebei Province, College of Pharmaceutical Sciences, Hebei University, Baoding, Hebei, 071002, ChinaKey Laboratory of Pharmaceutical Quality Control of Hebei Province, College of Pharmaceutical Sciences, Hebei University, Baoding, Hebei, 071002, ChinaKey Laboratory of Pharmaceutical Quality Control of Hebei Province, College of Pharmaceutical Sciences, Hebei University, Baoding, Hebei, 071002, ChinaKey Laboratory of Pharmaceutical Quality Control of Hebei Province, College of Pharmaceutical Sciences, Hebei University, Baoding, Hebei, 071002, ChinaKey Laboratory of Pharmaceutical Quality Control of Hebei Province, College of Pharmaceutical Sciences, Hebei University, Baoding, Hebei, 071002, ChinaState Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing, 100191, ChinaKey Laboratory of Pharmaceutical Quality Control of Hebei Province, College of Pharmaceutical Sciences, Hebei University, Baoding, Hebei, 071002, China; Key Laboratory of Medicinal Chemistry and Molecular Diagnosis, Ministry of Education, Hebei University, Baoding, Hebei, 071002, China; Corresponding author. Key Laboratory of Pharmaceutical Quality Control of Hebei Province, College of Pharmaceutical Sciences, Hebei University, Baoding, Hebei, 071002, China.Key Laboratory of Pharmaceutical Quality Control of Hebei Province, College of Pharmaceutical Sciences, Hebei University, Baoding, Hebei, 071002, China; Corresponding author.Palmitoylation occurs when fatty acids (such as palmitic acid) create covalent bonds between cysteine, serine, threonine, or other residues in proteins. The downstream effect of palmitoylation depends on the protein being palmitoylated because its blockage can render the protein useless in terms of its physiological function. Based on this, modulating the palmitoylation process becomes a good strategy for influencing cell proliferation, differentiation, metabolism, and apoptosis, allowing diabetes, obesity, and even cancer to be efficiently treated. As a determinant of the palmitoylation process, palmitoyltransferase is defined as an enzyme that catalyzes the transfer of the palmitate groups from Self-palmitoylated palmitoyl coenzyme A to another substrate. When it comes to the three most commonly cited palmitoyltransferases, serine palmitoyltransferase (SPT), carnitine palmitoyltransferase (CPT), and protein palmitoyltransferase (PAT), some similarities were found in the procedures by which they function, and in the structures of the small-molecule drugs that inhibit them. For this reason, we introduce the three above-mentioned palmitoyltransferases and describe the development of small molecule inhibitors for them to provide inspiration for the discovery of palmitoyltransferase inhibitors.http://www.sciencedirect.com/science/article/pii/S2772417422000139InhibitorsSerine palmitoyltransferaseCarnitine palmitoyltransferaseProtein palmitoyltransferase |
| spellingShingle | Xiaotong Hu Xinyue Zhu Wei Yu Yiwen Zhang Kan Yang Zhenming Liu Xiaoqiang Qiao Yali Song A mini review of small-molecule inhibitors targeting palmitoyltransferases European Journal of Medicinal Chemistry Reports Inhibitors Serine palmitoyltransferase Carnitine palmitoyltransferase Protein palmitoyltransferase |
| title | A mini review of small-molecule inhibitors targeting palmitoyltransferases |
| title_full | A mini review of small-molecule inhibitors targeting palmitoyltransferases |
| title_fullStr | A mini review of small-molecule inhibitors targeting palmitoyltransferases |
| title_full_unstemmed | A mini review of small-molecule inhibitors targeting palmitoyltransferases |
| title_short | A mini review of small-molecule inhibitors targeting palmitoyltransferases |
| title_sort | mini review of small molecule inhibitors targeting palmitoyltransferases |
| topic | Inhibitors Serine palmitoyltransferase Carnitine palmitoyltransferase Protein palmitoyltransferase |
| url | http://www.sciencedirect.com/science/article/pii/S2772417422000139 |
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