期刊
PHARMACEUTICALS
卷 15, 期 12, 页码 -出版社
MDPI
DOI: 10.3390/ph15121478
关键词
covalent drugs; covalent inhibitors; targeted covalent inhibitors; drug discovery
资金
- National Creative Research Initiative Grant through the National Research Foundation of Korea (NRF) - Korean Government (Ministry of Science ICT) [2014R1A3A2030423]
- BK21 Plus Program
Covalent inhibitors have been accepted as a practical tool for targeting previously undruggable proteins. Despite the clinical success, there are still unmet medical needs. Categorizing and reviewing covalent inhibitors provide insights into the future development of this field.
Recently, small-molecule covalent inhibitors have been accepted as a practical tool for targeting previously undruggable proteins. The high target selectivity of modern covalent inhibitors is now alleviating toxicity concerns regarding the covalent modifications of proteins. However, despite the tremendous clinical success of current covalent inhibitors, there are still unmet medical needs that covalent inhibitors have not yet addressed. This review categorized representative covalent inhibitors based on their mechanism of covalent inhibition: conventional covalent inhibitors, targeted covalent inhibitors (TCIs), and expanded TCIs. By reviewing both Food and Drug Administration (FDA)-approved drugs and drug candidates from recent literature, we provide insight into the future direction of covalent inhibitor development.
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