封面专题：直接抑制 YAP ：TEAD 相互作用：前所未有的药物发现挑战（ChemMedChem 19/2024）

IF 3.6 4区医学 Q2 CHEMISTRY, MEDICINAL

ChemMedChem Pub Date : 2024-10-03 DOI:10.1002/cmdc.202481902

Dr. Patrick Chène

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引用次数: 0

摘要

在许多癌症中，Hippo 通路都发生了失调，而针对这些肿瘤的一种方法就是抑制 YAP 和 TEAD 之间的相互作用。这两种蛋白之间的界面很大，由几个不同的接触区域组成。因此，发现能抑制这种相互作用的分子尤其具有挑战性。Patrick Chène撰写的综述10.1002/cmdc.202400361总结了如何利用从YAP：TEAD相互作用的结构-功能研究中获得的知识来设计一种策略，以确定一种有效的低分子量化合物IAG933，该化合物目前正在进行临床试验。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

Cover Feature: Direct Inhibition of the YAP : TEAD Interaction: An Unprecedented Drug Discovery Challenge (ChemMedChem 19/2024)

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Cover Feature: Direct Inhibition of the YAP : TEAD Interaction: An Unprecedented Drug Discovery Challenge (ChemMedChem 19/2024)

The Hippo pathway is deregulated in many cancers, and one approach to target these tumors is by inhibiting the interaction between YAP and TEAD. The interface between these two proteins is large and consists of several distinct contact areas. Therefore, discovering molecules that can inhibit this interaction is particularly challenging. The review 10.1002/cmdc.202400361 by Patrick Chène summarizes how the knowledge obtained from structure-function studies of the YAP:TEAD interaction was used to devise a strategy for identifying a potent low-molecular weight compound, IAG933, which is currently undergoing clinical trials.

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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.