Journal
CHEMMEDCHEM
Volume 11, Issue 1, Pages 22-30Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cmdc.201500469
Keywords
covalent catalysis; efficiency; irreversible inhibition; selectivity; toxicity
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Funding
- Spanish Ministry of Economy and Competitiveness [SAF2013-42899-R]
- Xunta de Galicia [GRC2013-041]
- European Regional Development Fund (ERDF)
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Despite the unquestionable success of numerous irreversible drugs that are currently in clinical use, such as acetylsalicylic acid (Aspirin) and penicillin, the number of such approved drugs is much lower than that of noncovalent drugs. Over the years, the potential off-target effects of these types of compounds have been the primary concern that has hampered their development. However, their remarkable advantages over noncovalent drugs and a better analysis of the risks have decreased the widespread skepticism surrounding them. The design of irreversible inhibitors is a challenge, particularly considering that in some cases their efficacy is due to complex and unexpected mechanisms of action. In this review the main advantages of irreversible inhibition are summarized, and the complexity of certain covalent modification mechanisms is highlighted with selected examples.
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