{"title":"Cover Feature: Direct Inhibition of the YAP : TEAD Interaction: An Unprecedented Drug Discovery Challenge (ChemMedChem 19/2024)","authors":"Dr. Patrick Chène","doi":"10.1002/cmdc.202481902","DOIUrl":null,"url":null,"abstract":"<p>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.\n <figure>\n <div><picture>\n <source></source></picture><p></p>\n </div>\n </figure>\n </p>","PeriodicalId":147,"journal":{"name":"ChemMedChem","volume":null,"pages":null},"PeriodicalIF":3.6000,"publicationDate":"2024-10-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://onlinelibrary.wiley.com/doi/epdf/10.1002/cmdc.202481902","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"ChemMedChem","FirstCategoryId":"3","ListUrlMain":"https://onlinelibrary.wiley.com/doi/10.1002/cmdc.202481902","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
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Abstract
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.
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.
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