Chemo-selective modification of cysteine residue: synthesis and application in the discovery of potential drug candidates
Chemo-select modification of peptides, targeting a handful of the most reactive proteinogenic amino acids (AAs), is gradually utilized to address the medical needs of peptide drugs and biopharmaceuticals. Cysteine (Cys), one of the less abundant AAs in many biological proteins, plays a vital role in...
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Open Exploration
2024-09-01
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| Series: | Exploration of Drug Science |
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| Online Access: | https://www.explorationpub.com/uploads/Article/A100860/100860.pdf |
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| author | Yanyan Liao Xuefeng Jiang |
| author_facet | Yanyan Liao Xuefeng Jiang |
| author_sort | Yanyan Liao |
| collection | DOAJ |
| description | Chemo-select modification of peptides, targeting a handful of the most reactive proteinogenic amino acids (AAs), is gradually utilized to address the medical needs of peptide drugs and biopharmaceuticals. Cysteine (Cys), one of the less abundant AAs in many biological proteins, plays a vital role in the catalysis, signal transduction, and redox regulation of gene expression. In natural AAs (α-AAs) residues, Cys exhibits high nucleophilicity and low redox-active potential, making it a primary target for site-selective conjugation. This review summarizes several representative Cys-peptide/protein conjugation strategies developed in recent years, including polar reactions, radical coupling reactions, and stapling techniques. |
| format | Article |
| id | doaj-art-ba79ac71e14b4e9789b71ce9a62a37c5 |
| institution | Kabale University |
| issn | 2836-7677 |
| language | English |
| publishDate | 2024-09-01 |
| publisher | Open Exploration |
| record_format | Article |
| series | Exploration of Drug Science |
| spelling | doaj-art-ba79ac71e14b4e9789b71ce9a62a37c52025-02-08T03:29:23ZengOpen ExplorationExploration of Drug Science2836-76772024-09-012554055410.37349/eds.2024.00060Chemo-selective modification of cysteine residue: synthesis and application in the discovery of potential drug candidatesYanyan Liao0Xuefeng Jiang1https://orcid.org/0000-0002-1849-6572Hainan Institute, East China Normal University, Shanghai 200062, China; State Key Laboratory of Petroleum Molecular & Process Engineering, School of Chemistry and Molecular Engineering, East China Normal University, Shanghai 200062, China; Shanghai Key Laboratory of Green Chemistry and Chemical Processes, School of Chemistry and Molecular Engineering, East China Normal University, Shanghai 200062, ChinaHainan Institute, East China Normal University, Shanghai 200062, China; State Key Laboratory of Petroleum Molecular & Process Engineering, School of Chemistry and Molecular Engineering, East China Normal University, Shanghai 200062, China; Shanghai Key Laboratory of Green Chemistry and Chemical Processes, School of Chemistry and Molecular Engineering, East China Normal University, Shanghai 200062, China; School of Chemistry and Chemical Engineering, Henan Normal University, Xinxiang 453007, Henan, China; State Key Laboratory of Organometallic Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, Shanghai 200032, ChinaChemo-select modification of peptides, targeting a handful of the most reactive proteinogenic amino acids (AAs), is gradually utilized to address the medical needs of peptide drugs and biopharmaceuticals. Cysteine (Cys), one of the less abundant AAs in many biological proteins, plays a vital role in the catalysis, signal transduction, and redox regulation of gene expression. In natural AAs (α-AAs) residues, Cys exhibits high nucleophilicity and low redox-active potential, making it a primary target for site-selective conjugation. This review summarizes several representative Cys-peptide/protein conjugation strategies developed in recent years, including polar reactions, radical coupling reactions, and stapling techniques.https://www.explorationpub.com/uploads/Article/A100860/100860.pdfcysteinebioconjugationchemo-selectivitystaplingmedicinal chemistry |
| spellingShingle | Yanyan Liao Xuefeng Jiang Chemo-selective modification of cysteine residue: synthesis and application in the discovery of potential drug candidates Exploration of Drug Science cysteine bioconjugation chemo-selectivity stapling medicinal chemistry |
| title | Chemo-selective modification of cysteine residue: synthesis and application in the discovery of potential drug candidates |
| title_full | Chemo-selective modification of cysteine residue: synthesis and application in the discovery of potential drug candidates |
| title_fullStr | Chemo-selective modification of cysteine residue: synthesis and application in the discovery of potential drug candidates |
| title_full_unstemmed | Chemo-selective modification of cysteine residue: synthesis and application in the discovery of potential drug candidates |
| title_short | Chemo-selective modification of cysteine residue: synthesis and application in the discovery of potential drug candidates |
| title_sort | chemo selective modification of cysteine residue synthesis and application in the discovery of potential drug candidates |
| topic | cysteine bioconjugation chemo-selectivity stapling medicinal chemistry |
| url | https://www.explorationpub.com/uploads/Article/A100860/100860.pdf |
| work_keys_str_mv | AT yanyanliao chemoselectivemodificationofcysteineresiduesynthesisandapplicationinthediscoveryofpotentialdrugcandidates AT xuefengjiang chemoselectivemodificationofcysteineresiduesynthesisandapplicationinthediscoveryofpotentialdrugcandidates |