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Design, synthesis, and applications of ring-functionalized histidines in peptide-based medicinal chemistry and drug discovery
Medicinal Research Reviews ( IF 10.9 ) Pub Date : 2023-01-29 , DOI: 10.1002/med.21936
Komal Sharma 1 , Krishna K Sharma 1 , Amit Mahindra 1 , Naina Sehra 1 , Nitin Bagra 1 , Shams Aaghaz 1 , Rajesh Parmar 1 , Gajanan K Rathod 1 , Rahul Jain 1
Medicinal Research Reviews ( IF 10.9 ) Pub Date : 2023-01-29 , DOI: 10.1002/med.21936
Komal Sharma 1 , Krishna K Sharma 1 , Amit Mahindra 1 , Naina Sehra 1 , Nitin Bagra 1 , Shams Aaghaz 1 , Rajesh Parmar 1 , Gajanan K Rathod 1 , Rahul Jain 1
Affiliation
Modified and synthetic α-amino acids are known to show diverse applications. Histidine, which possesses numerous applications when subjected to synthetic modifications, is one such amino acid. The utility of modified histidines varies widely from remarkable biological activities to catalysis, and from nanotechnology to polymer chemistry. This renders histidine residue an important place in scientific research. Histidine is a well-studied scaffold and constitutes the active site of various enzymes catalyzing important reactions in the biological systems. A rational modification in histidine structure with a distinctly developed protocol extensively changes its physical and chemical properties. The utilization of modified histidines in search of potent, target selective and proteostable scaffolds is vital in the development of bioactive peptides with enhanced drug-likeliness. This review is a compilation and analysis of reported side-chain ring modifications at histidine followed by applications of ring-modified histidines in the synthesis of various categories of bioactive peptides and peptidomimetics.
中文翻译:
环功能化组氨酸的设计、合成及其在基于肽的药物化学和药物发现中的应用
已知修饰和合成的 α-氨基酸显示出多种应用。组氨酸在进行合成修饰时具有多种应用,就是这样一种氨基酸。修饰组氨酸的用途千差万别,从显着的生物活性到催化作用,从纳米技术到聚合物化学。这使得组氨酸残基在科学研究中占有重要地位。组氨酸是一种经过充分研究的支架,构成了催化生物系统中重要反应的各种酶的活性位点。通过明确开发的方案对组氨酸结构进行合理修饰,可广泛改变其物理和化学性质。利用修饰的组氨酸寻找有效的,靶向选择性和蛋白质稳定的支架对于开发具有增强药物可能性的生物活性肽至关重要。本综述汇编和分析了已报道的组氨酸侧链环修饰,以及环修饰组氨酸在各类生物活性肽和肽模拟物合成中的应用。
更新日期:2023-01-29
中文翻译:
![](https://scdn.x-mol.com/jcss/images/paperTranslation.png)
环功能化组氨酸的设计、合成及其在基于肽的药物化学和药物发现中的应用
已知修饰和合成的 α-氨基酸显示出多种应用。组氨酸在进行合成修饰时具有多种应用,就是这样一种氨基酸。修饰组氨酸的用途千差万别,从显着的生物活性到催化作用,从纳米技术到聚合物化学。这使得组氨酸残基在科学研究中占有重要地位。组氨酸是一种经过充分研究的支架,构成了催化生物系统中重要反应的各种酶的活性位点。通过明确开发的方案对组氨酸结构进行合理修饰,可广泛改变其物理和化学性质。利用修饰的组氨酸寻找有效的,靶向选择性和蛋白质稳定的支架对于开发具有增强药物可能性的生物活性肽至关重要。本综述汇编和分析了已报道的组氨酸侧链环修饰,以及环修饰组氨酸在各类生物活性肽和肽模拟物合成中的应用。