封面:利用(S)-丙氨酸酰胺作为精氨酸模拟分子开发蛋白精氨酸甲基转移酶 4 抑制剂的原药方法(ChemMedChem 17/2024)

IF 3.6 4区 医学 Q2 CHEMISTRY, MEDICINAL ChemMedChem Pub Date : 2024-09-02 DOI:10.1002/cmdc.202481701
Prof. Dr. Ciro Milite, Giuliana Sarno, Ida Pacilio, Dr. Agostino Cianciulli, Dr. Monica Viviano, Dr. Giulia Iannelli, Erica Gazzillo, Dr. Alessandra Feoli, Dr. Alessandra Cipriano, Prof. Dr. Maria Giovanna Chini, Prof. Dr. Sabrina Castellano, Prof. Dr. Giuseppe Bifulco, Prof. Dr. Gianluca Sbardella
{"title":"封面:利用(S)-丙氨酸酰胺作为精氨酸模拟分子开发蛋白精氨酸甲基转移酶 4 抑制剂的原药方法(ChemMedChem 17/2024)","authors":"Prof. Dr. Ciro Milite,&nbsp;Giuliana Sarno,&nbsp;Ida Pacilio,&nbsp;Dr. Agostino Cianciulli,&nbsp;Dr. Monica Viviano,&nbsp;Dr. Giulia Iannelli,&nbsp;Erica Gazzillo,&nbsp;Dr. Alessandra Feoli,&nbsp;Dr. Alessandra Cipriano,&nbsp;Prof. Dr. Maria Giovanna Chini,&nbsp;Prof. Dr. Sabrina Castellano,&nbsp;Prof. Dr. Giuseppe Bifulco,&nbsp;Prof. Dr. Gianluca Sbardella","doi":"10.1002/cmdc.202481701","DOIUrl":null,"url":null,"abstract":"<p>The front cover picture shows that the introduction of a NAD(P)H:quinone oxidoreductase 1 (NQO1)-responsive trigger group (in cyan sticks) to mask the S-alanine amido group turns PRMT4 inhibitors (in orange sticks) into cell-permeable prodrugs, that after in cell activation (magenta) are able to inhibit PRMT4 (yellow green) and reduce arginine dimethylation of the PRMT4 substrates BRG1-associated factor 155 (BAF155). More details can be found in the Research Article by Maria Giovanna Chini, Sabrina Castellano, and co-workers. Cover design by Gianluca Sbardella.\n <figure>\n <div><picture>\n <source></source></picture><p></p>\n </div>\n </figure>\n </p>","PeriodicalId":147,"journal":{"name":"ChemMedChem","volume":"19 17","pages":""},"PeriodicalIF":3.6000,"publicationDate":"2024-09-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://onlinelibrary.wiley.com/doi/epdf/10.1002/cmdc.202481701","citationCount":"0","resultStr":"{\"title\":\"Front Cover: Prodrug Approach to Exploit (S)-Alanine Amide as Arginine Mimic Moiety in the Development of Protein Arginine Methyltransferase 4 Inhibitors (ChemMedChem 17/2024)\",\"authors\":\"Prof. Dr. Ciro Milite,&nbsp;Giuliana Sarno,&nbsp;Ida Pacilio,&nbsp;Dr. Agostino Cianciulli,&nbsp;Dr. Monica Viviano,&nbsp;Dr. Giulia Iannelli,&nbsp;Erica Gazzillo,&nbsp;Dr. Alessandra Feoli,&nbsp;Dr. Alessandra Cipriano,&nbsp;Prof. Dr. Maria Giovanna Chini,&nbsp;Prof. Dr. Sabrina Castellano,&nbsp;Prof. Dr. Giuseppe Bifulco,&nbsp;Prof. Dr. Gianluca Sbardella\",\"doi\":\"10.1002/cmdc.202481701\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p>The front cover picture shows that the introduction of a NAD(P)H:quinone oxidoreductase 1 (NQO1)-responsive trigger group (in cyan sticks) to mask the S-alanine amido group turns PRMT4 inhibitors (in orange sticks) into cell-permeable prodrugs, that after in cell activation (magenta) are able to inhibit PRMT4 (yellow green) and reduce arginine dimethylation of the PRMT4 substrates BRG1-associated factor 155 (BAF155). More details can be found in the Research Article by Maria Giovanna Chini, Sabrina Castellano, and co-workers. Cover design by Gianluca Sbardella.\\n <figure>\\n <div><picture>\\n <source></source></picture><p></p>\\n </div>\\n </figure>\\n </p>\",\"PeriodicalId\":147,\"journal\":{\"name\":\"ChemMedChem\",\"volume\":\"19 17\",\"pages\":\"\"},\"PeriodicalIF\":3.6000,\"publicationDate\":\"2024-09-02\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://onlinelibrary.wiley.com/doi/epdf/10.1002/cmdc.202481701\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"ChemMedChem\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://onlinelibrary.wiley.com/doi/10.1002/cmdc.202481701\",\"RegionNum\":4,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q2\",\"JCRName\":\"CHEMISTRY, MEDICINAL\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"ChemMedChem","FirstCategoryId":"3","ListUrlMain":"https://onlinelibrary.wiley.com/doi/10.1002/cmdc.202481701","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
引用次数: 0

摘要

封面图片显示,引入一个 NAD(P)H:醌氧化还原酶 1 (NQO1) 响应触发基团(青色条纹)掩盖了 S-丙氨酸氨基基团,使 PRMT4 抑制剂(橙色条纹)变成了细胞渗透性原药,在细胞内活化(品红色)后能够抑制 PRMT4(黄绿色)并减少 PRMT4 底物 BRG1 相关因子 155(BAF155)的精氨酸二甲基化。更多详情,请参阅 Maria Giovanna Chini、Sabrina Castellano 及其合作者的研究文章。封面设计:Gianluca Sbardella。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

摘要图片

查看原文
分享 分享
微信好友 朋友圈 QQ好友 复制链接
本刊更多论文
Front Cover: Prodrug Approach to Exploit (S)-Alanine Amide as Arginine Mimic Moiety in the Development of Protein Arginine Methyltransferase 4 Inhibitors (ChemMedChem 17/2024)

The front cover picture shows that the introduction of a NAD(P)H:quinone oxidoreductase 1 (NQO1)-responsive trigger group (in cyan sticks) to mask the S-alanine amido group turns PRMT4 inhibitors (in orange sticks) into cell-permeable prodrugs, that after in cell activation (magenta) are able to inhibit PRMT4 (yellow green) and reduce arginine dimethylation of the PRMT4 substrates BRG1-associated factor 155 (BAF155). More details can be found in the Research Article by Maria Giovanna Chini, Sabrina Castellano, and co-workers. Cover design by Gianluca Sbardella.

求助全文
通过发布文献求助,成功后即可免费获取论文全文。 去求助
来源期刊
ChemMedChem
ChemMedChem 医学-药学
CiteScore
6.70
自引率
2.90%
发文量
280
审稿时长
1 months
期刊介绍: Quality research. Outstanding publications. With an impact factor of 3.124 (2019), ChemMedChem is a top journal for research at the interface of chemistry, biology and medicine. It is published on behalf of Chemistry Europe, an association of 16 European chemical societies. ChemMedChem publishes primary as well as critical secondary and tertiary information from authors across and for the world. Its mission is to integrate the wide and flourishing field of medicinal and pharmaceutical sciences, ranging from drug design and discovery to drug development and delivery, from molecular modeling to combinatorial chemistry, from target validation to lead generation and ADMET studies. ChemMedChem typically covers topics on small molecules, therapeutic macromolecules, peptides, peptidomimetics, and aptamers, protein-drug conjugates, nucleic acid therapies, and beginning 2017, nanomedicine, particularly 1) targeted nanodelivery, 2) theranostic nanoparticles, and 3) nanodrugs. Contents ChemMedChem publishes an attractive mixture of: Full Papers and Communications Reviews and Minireviews Patent Reviews Highlights and Concepts Book and Multimedia Reviews.
期刊最新文献
Virtual Screening and Biological Evaluation of Natural Products as Novel VPS34 Inhibitors that Modulate Autophagy. Artificial Ion Transporters as Potent Therapeutics for Channelopathies. Highlights from the Lowlands: Early Career Researchers Shine at Medicinal Chemistry Frontiers 2024. Front Cover: Conditional PROTAC: Recent Strategies for Modulating Targeted Protein Degradation (ChemMedChem 22/2024) Cover Feature: Exploring the Chemical Space of Mycobacterial Oxidative Phosphorylation Inhibitors Using Molecular Modeling (ChemMedChem 22/2024)
×
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
现在去查看 取消
×
提示
确定
0
微信
客服QQ
Book学术公众号 扫码关注我们
反馈
×
意见反馈
请填写您的意见或建议
请填写您的手机或邮箱
已复制链接
已复制链接
快去分享给好友吧!
我知道了
×
扫码分享
扫码分享
Book学术官方微信
Book学术文献互助
Book学术文献互助群
群 号:481959085
Book学术
文献互助 智能选刊 最新文献 互助须知 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 Book学术 All rights reserved.
ghs 京公网安备 11010802042870号 京ICP备2023020795号-1