Total Synthesis of Biologically Potent Peptides and their In Silico Studies: A TAG Approach.

IF 3.3 4区 医学 Q3 CHEMISTRY, MEDICINAL
Ramya M, Veeranjaneyulu Avula, Kiran Kumar B, Nagendra G
{"title":"Total Synthesis of Biologically Potent Peptides and their In Silico Studies: A TAG Approach.","authors":"Ramya M, Veeranjaneyulu Avula, Kiran Kumar B, Nagendra G","doi":"10.2174/0115680266377804250721145504","DOIUrl":null,"url":null,"abstract":"<p><strong>Introduction: </strong>Current trends in peptide synthesis protocols have emerged as the most attractive domain in the field of pharma and medicine. Since most of the peptide/peptidomimeticbased molecules serve as potential candidates for many diseases, as they are bioavailable molecules.</p><p><strong>Methods: </strong>We present the synthesis of bioactive peptides through TAGGING approach with the help of TAG-OH as a linker to the Nα-protected amino acid.</p><p><strong>Results: </strong>FRDEHKK and NKDRG are two peptides that possess antioxidant and antiproliferative activity, and their in-silico investigations reveal that they exhibit anticancer properties when bound to the AXL kinase and EGFR proteins.</p><p><strong>Discussion: </strong>This TAG method enables the easy isolation of peptides at each step as solids, and all the impurities were washed off by simple filtration. The method allows a bulk-scale preparation of the peptides without any difficulty, and hence the protocol is highly efficient for the production of peptides of therapeutic importance.</p><p><strong>Conclusion: </strong>The two peptides FRDEHKK and NKDRG were isolated as fine solids with 82% and 85% yield and were characterized by NMR and MASS spectroscopy. In-silico studies reveal FRDEHKK and NKDRG peptides exhibit good affinity towards EGFR and AXL kinase.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3000,"publicationDate":"2025-08-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Current topics in medicinal chemistry","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.2174/0115680266377804250721145504","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
引用次数: 0

Abstract

Introduction: Current trends in peptide synthesis protocols have emerged as the most attractive domain in the field of pharma and medicine. Since most of the peptide/peptidomimeticbased molecules serve as potential candidates for many diseases, as they are bioavailable molecules.

Methods: We present the synthesis of bioactive peptides through TAGGING approach with the help of TAG-OH as a linker to the Nα-protected amino acid.

Results: FRDEHKK and NKDRG are two peptides that possess antioxidant and antiproliferative activity, and their in-silico investigations reveal that they exhibit anticancer properties when bound to the AXL kinase and EGFR proteins.

Discussion: This TAG method enables the easy isolation of peptides at each step as solids, and all the impurities were washed off by simple filtration. The method allows a bulk-scale preparation of the peptides without any difficulty, and hence the protocol is highly efficient for the production of peptides of therapeutic importance.

Conclusion: The two peptides FRDEHKK and NKDRG were isolated as fine solids with 82% and 85% yield and were characterized by NMR and MASS spectroscopy. In-silico studies reveal FRDEHKK and NKDRG peptides exhibit good affinity towards EGFR and AXL kinase.

生物有效肽的全合成及其在计算机上的研究:TAG方法。
肽合成方案的当前趋势已经成为制药和医学领域最具吸引力的领域。由于大多数肽/聚肽基分子是生物可利用的分子,因此它们是许多疾病的潜在候选者。方法:利用TAG-OH作为n - α保护氨基酸的连接物,采用标记法合成生物活性肽。结果:FRDEHKK和NKDRG是两种具有抗氧化和抗增殖活性的肽,它们的计算机研究表明,当它们与AXL激酶和EGFR蛋白结合时,它们表现出抗癌特性。讨论:这种TAG方法可以很容易地在每一步分离肽作为固体,所有的杂质通过简单的过滤被洗掉。该方法允许在没有任何困难的情况下批量制备肽,因此该方案对于生产具有治疗重要性的肽是高效的。结论:FRDEHKK和NKDRG肽分离得到细固体,产率分别为82%和85%,并通过NMR和质谱进行了表征。芯片研究表明,FRDEHKK和NKDRG肽对EGFR和AXL激酶具有良好的亲和力。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
求助全文
约1分钟内获得全文 求助全文
来源期刊
CiteScore
6.40
自引率
2.90%
发文量
186
审稿时长
3-8 weeks
期刊介绍: Current Topics in Medicinal Chemistry is a forum for the review of areas of keen and topical interest to medicinal chemists and others in the allied disciplines. Each issue is solely devoted to a specific topic, containing six to nine reviews, which provide the reader a comprehensive survey of that area. A Guest Editor who is an expert in the topic under review, will assemble each issue. The scope of Current Topics in Medicinal Chemistry will cover all areas of medicinal chemistry, including current developments in rational drug design, synthetic chemistry, bioorganic chemistry, high-throughput screening, combinatorial chemistry, compound diversity measurements, drug absorption, drug distribution, metabolism, new and emerging drug targets, natural products, pharmacogenomics, and structure-activity relationships. Medicinal chemistry is a rapidly maturing discipline. The study of how structure and function are related is absolutely essential to understanding the molecular basis of life. Current Topics in Medicinal Chemistry aims to contribute to the growth of scientific knowledge and insight, and facilitate the discovery and development of new therapeutic agents to treat debilitating human disorders. The journal is essential for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important advances.
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
确定
请完成安全验证×
copy
已复制链接
快去分享给好友吧!
我知道了
右上角分享
点击右上角分享
0
联系我们:info@booksci.cn Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。 Copyright © 2023 布克学术 All rights reserved.
京ICP备2023020795号-1
ghs 京公网安备 11010802042870号
Book学术文献互助
Book学术文献互助群
群 号:604180095
Book学术官方微信