RT Journal Article
T1 Designing Irreversible Inhibitors—Worth the Effort?
A1 González Bello, Concepción
K1 Covalent catalysis
K1 Efficiency
K1 Irreversible inhibition
K1 Selectivity
K1 Toxicity
AB 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
PB Wiley
SN 1860-7179
YR 2016
FD 2016-01-07
LK http://hdl.handle.net/10347/16926
UL http://hdl.handle.net/10347/16926
LA eng
NO González-Bello, C. (2016). Designing Irreversible Inhibitors-Worth the Effort?. Chemmedchem, 11(1), 22-30. doi: 10.1002/cmdc.201500469
NO This is the peer-reviewed version of the following article: González-Bello, C. (2016). Designing Irreversible Inhibitors-Worth the Effort?. Chemmedchem, 11(1), 22-30, which has been published in final form at https://doi.org/10.1002/cmdc.201500469. This article may be used for non-commercial purposes in accordance with Wiley-VCH Terms and Conditions for Self-Archiving
NO Spanish Ministry of Economy and Competitiveness. Grant Number: SAF2013-42899-RXunta de Galicia. Grant Number: GRC2013-041European Regional Development Fund (ERDF)
DS Minerva
RD 24 abr 2026