{"title":"Opening the Door to a New Treatment Paradigm: The Re-emergence of Chymase Inhibitors","authors":"Franz von Nussbaum, Giambattista Testolin","doi":"10.1021/acs.jmedchem.5c00413","DOIUrl":null,"url":null,"abstract":"Chymase is a serine protease that has been studied as a drug target in inflammatory diseases, so far with limited success. Fulacimstat is a novel drug candidate inhibiting chymase that has been investigated in clinical trials for the role of chymase in inflammation. Despite a good safety profile, further clinical development of fulacimstat was not pursued due to a lack of efficacy. Recently, a new role of chymase in blood clot biology has been identified, this resparks interest in chymase inhibitors, and positions fulacimstat as a potential innovative option to treat thrombotic conditions.","PeriodicalId":46,"journal":{"name":"Journal of Medicinal Chemistry","volume":"51 1","pages":""},"PeriodicalIF":6.8000,"publicationDate":"2025-02-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of Medicinal Chemistry","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1021/acs.jmedchem.5c00413","RegionNum":1,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
引用次数: 0
Abstract
Chymase is a serine protease that has been studied as a drug target in inflammatory diseases, so far with limited success. Fulacimstat is a novel drug candidate inhibiting chymase that has been investigated in clinical trials for the role of chymase in inflammation. Despite a good safety profile, further clinical development of fulacimstat was not pursued due to a lack of efficacy. Recently, a new role of chymase in blood clot biology has been identified, this resparks interest in chymase inhibitors, and positions fulacimstat as a potential innovative option to treat thrombotic conditions.
期刊介绍:
The Journal of Medicinal Chemistry is a prestigious biweekly peer-reviewed publication that focuses on the multifaceted field of medicinal chemistry. Since its inception in 1959 as the Journal of Medicinal and Pharmaceutical Chemistry, it has evolved to become a cornerstone in the dissemination of research findings related to the design, synthesis, and development of therapeutic agents.
The Journal of Medicinal Chemistry is recognized for its significant impact in the scientific community, as evidenced by its 2022 impact factor of 7.3. This metric reflects the journal's influence and the importance of its content in shaping the future of drug discovery and development. The journal serves as a vital resource for chemists, pharmacologists, and other researchers interested in the molecular mechanisms of drug action and the optimization of therapeutic compounds.