Covalent Warheads Targeting Cysteine Residue: The Promising Approach in Drug Development
Cysteine is one of the least abundant amino acids in proteins of many organisms, which plays a crucial role in catalysis, signal transduction, and redox regulation of gene expression. The thiol group of cysteine possesses the ability to perform nucleophilic and redox-active functions that are not fe...
| Main Authors: | , , , |
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| Format: | Article |
| Language: | English |
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MDPI AG
2022-11-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/27/22/7728 |
| _version_ | 1827644086401630208 |
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| author | Fangjiao Huang Xiaoli Han Xiaohui Xiao Jinming Zhou |
| author_facet | Fangjiao Huang Xiaoli Han Xiaohui Xiao Jinming Zhou |
| author_sort | Fangjiao Huang |
| collection | DOAJ |
| description | Cysteine is one of the least abundant amino acids in proteins of many organisms, which plays a crucial role in catalysis, signal transduction, and redox regulation of gene expression. The thiol group of cysteine possesses the ability to perform nucleophilic and redox-active functions that are not feasible for other natural amino acids. Cysteine is the most common covalent amino acid residue and has been shown to react with a variety of warheads, especially Michael receptors. These unique properties have led to widespread interest in this nucleophile, leading to the development of a variety of cysteine-targeting warheads with different chemical compositions. Herein, we summarized the various covalent warheads targeting cysteine residue and their application in drug development. |
| first_indexed | 2024-03-09T18:07:53Z |
| format | Article |
| id | doaj.art-5a53c43663f046fd969e24a41109d4b9 |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-09T18:07:53Z |
| publishDate | 2022-11-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-5a53c43663f046fd969e24a41109d4b92023-11-24T09:20:09ZengMDPI AGMolecules1420-30492022-11-012722772810.3390/molecules27227728Covalent Warheads Targeting Cysteine Residue: The Promising Approach in Drug DevelopmentFangjiao Huang0Xiaoli Han1Xiaohui Xiao2Jinming Zhou3Key Laboratory of the Ministry of Education for Advanced Catalysis Materials, Department of Chemistry, Zhejiang Normal University, 688 Yingbin Road, Jinhua 321004, ChinaKey Laboratory of the Ministry of Education for Advanced Catalysis Materials, Department of Chemistry, Zhejiang Normal University, 688 Yingbin Road, Jinhua 321004, ChinaKey Laboratory of the Ministry of Education for Advanced Catalysis Materials, Department of Chemistry, Zhejiang Normal University, 688 Yingbin Road, Jinhua 321004, ChinaKey Laboratory of the Ministry of Education for Advanced Catalysis Materials, Department of Chemistry, Zhejiang Normal University, 688 Yingbin Road, Jinhua 321004, ChinaCysteine is one of the least abundant amino acids in proteins of many organisms, which plays a crucial role in catalysis, signal transduction, and redox regulation of gene expression. The thiol group of cysteine possesses the ability to perform nucleophilic and redox-active functions that are not feasible for other natural amino acids. Cysteine is the most common covalent amino acid residue and has been shown to react with a variety of warheads, especially Michael receptors. These unique properties have led to widespread interest in this nucleophile, leading to the development of a variety of cysteine-targeting warheads with different chemical compositions. Herein, we summarized the various covalent warheads targeting cysteine residue and their application in drug development.https://www.mdpi.com/1420-3049/27/22/7728cysteinecovalent warheadscovalent inhibitor |
| spellingShingle | Fangjiao Huang Xiaoli Han Xiaohui Xiao Jinming Zhou Covalent Warheads Targeting Cysteine Residue: The Promising Approach in Drug Development Molecules cysteine covalent warheads covalent inhibitor |
| title | Covalent Warheads Targeting Cysteine Residue: The Promising Approach in Drug Development |
| title_full | Covalent Warheads Targeting Cysteine Residue: The Promising Approach in Drug Development |
| title_fullStr | Covalent Warheads Targeting Cysteine Residue: The Promising Approach in Drug Development |
| title_full_unstemmed | Covalent Warheads Targeting Cysteine Residue: The Promising Approach in Drug Development |
| title_short | Covalent Warheads Targeting Cysteine Residue: The Promising Approach in Drug Development |
| title_sort | covalent warheads targeting cysteine residue the promising approach in drug development |
| topic | cysteine covalent warheads covalent inhibitor |
| url | https://www.mdpi.com/1420-3049/27/22/7728 |
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