Journal
NATURE REVIEWS DRUG DISCOVERY
Volume 10, Issue 4, Pages 307-317Publisher
NATURE PUBLISHING GROUP
DOI: 10.1038/nrd3410
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Funding
- NIGMS NIH HHS [R01 GM094551] Funding Source: Medline
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Covalent drugs have proved to be successful therapies for various indications, but largely owing to safety concerns, they are rarely considered when initiating a target-directed drug discovery project. There is a need to reassess this important class of drugs, and to reconcile the discordance between the historic success of covalent drugs and the reluctance of most drug discovery teams to include them in their armamentarium. This Review surveys the prevalence and pharmacological advantages of covalent drugs, discusses how potential risks and challenges may be addressed through innovative design, and presents the broad opportunities provided by targeted covalent inhibitors.
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