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)

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

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Abstract

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.

Abstract Image

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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）

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。

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来源期刊

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.