Anil Vasudevan, Maria A Argiriadi, Aleksandra Baranczak, Michael M Friedman, Julia Gavrilyuk, Adrian D Hobson, Jonathan J Hulce, Sami Osman, Noel S Wilson
{"title":"Covalent binders in drug discovery.","authors":"Anil Vasudevan, Maria A Argiriadi, Aleksandra Baranczak, Michael M Friedman, Julia Gavrilyuk, Adrian D Hobson, Jonathan J Hulce, Sami Osman, Noel S Wilson","doi":"10.1016/bs.pmch.2018.12.002","DOIUrl":null,"url":null,"abstract":"<p><p>Covalent modulation of protein function can have multiple utilities including therapeutics, and probes to interrogate biology. While this field is still viewed with scepticism due to the potential for (idiosyncratic) toxicities, significant strides have been made in terms of understanding how to tune electrophilicity to selectively target specific residues. Progress has also been made in harnessing the potential of covalent binders to uncover novel biology and to provide an enhanced utility as payloads for Antibody Drug Conjugates. This perspective covers the tenets and applications of covalent binders.</p>","PeriodicalId":20755,"journal":{"name":"Progress in medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":0.0000,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/bs.pmch.2018.12.002","citationCount":"24","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Progress in medicinal chemistry","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.1016/bs.pmch.2018.12.002","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2019/3/11 0:00:00","PubModel":"Epub","JCR":"Q1","JCRName":"Pharmacology, Toxicology and Pharmaceutics","Score":null,"Total":0}
引用次数: 24
Abstract
Covalent modulation of protein function can have multiple utilities including therapeutics, and probes to interrogate biology. While this field is still viewed with scepticism due to the potential for (idiosyncratic) toxicities, significant strides have been made in terms of understanding how to tune electrophilicity to selectively target specific residues. Progress has also been made in harnessing the potential of covalent binders to uncover novel biology and to provide an enhanced utility as payloads for Antibody Drug Conjugates. This perspective covers the tenets and applications of covalent binders.
期刊介绍：
This series has a long established reputation for excellent coverage of almost every facet of Medicinal Chemistry and is one of the most respected and instructive sources of information on the subject. The latest volume certifies to the continuing success of a unique series reflecting current progress in a broadly developing field of science.
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