Designing Irreversible Inhibitors—Worth the Effort?

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dc.contributor.affiliationUniversidade de Santiago de Compostela. Centro de Investigación en Química Biolóxica e Materiais Molecularesgl
dc.contributor.affiliationUniversidade de Santiago de Compostela. Departamento de Química Orgánicagl
dc.contributor.authorGonzález Bello, Concepción
dc.date.accessioned2018-07-02T12:54:18Z
dc.date.available2018-07-02T12:54:18Z
dc.date.issued2016-01-07
dc.descriptionThis 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-Archivinggl
dc.description.abstractDespite 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 examplesgl
dc.description.peerreviewedSIgl
dc.description.sponsorshipSpanish Ministry of Economy and Competitiveness. Grant Number: SAF2013-42899-R Xunta de Galicia. Grant Number: GRC2013-041 European Regional Development Fund (ERDF)gl
dc.identifier.citationGonzález-Bello, C. (2016). Designing Irreversible Inhibitors-Worth the Effort?. Chemmedchem, 11(1), 22-30. doi: 10.1002/cmdc.201500469gl
dc.identifier.doi10.1002/cmdc.201500469
dc.identifier.essn1860-7187
dc.identifier.issn1860-7179
dc.identifier.urihttp://hdl.handle.net/10347/16926
dc.language.isoenggl
dc.publisherWileygl
dc.relation.projectIDinfo:eu-repo/grantAgreement/MINECO/Plan Estatal de Investigación Científica y Técnica y de Innovación 2013-2016/SAF2013-42899-R/ES/DESARROLLO DE NUEVOS ANTIBIOTICOS PARA EL TRATAMIENTO DE INFECCIONES BACTERIANAS RESISTENTES: METABOLISMO, RESISTENCIA Y COMUNICACION CELULA-CELULA
dc.relation.publisherversionhttps://doi.org/10.1002/cmdc.201500469gl
dc.rights© 2016 WILEY‐VCH Verlag GmbH & Co. KGaA, Weinheim. This article may be used for non-commercial purposes in accordance with Wiley-VCH Terms and Conditions for Self-Archivinggl
dc.rights.accessRightsopen accessgl
dc.subjectCovalent catalysisgl
dc.subjectEfficiencygl
dc.subjectIrreversible inhibitiongl
dc.subjectSelectivitygl
dc.subjectToxicitygl
dc.titleDesigning Irreversible Inhibitors—Worth the Effort?gl
dc.typejournal articlegl
dc.type.hasVersionAMgl
dspace.entity.typePublication
relation.isAuthorOfPublicationf6672ba5-c599-442d-b04f-e5aafa7d2f3b
relation.isAuthorOfPublication.latestForDiscoveryf6672ba5-c599-442d-b04f-e5aafa7d2f3b

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