Covalent inhibitors: a rational approach to drug discovery

Covalent inhibitors are recognized as an important component in drug discovery and therapeutics. Since the first appearance of covalent inhibitors in the late 18th century, the field has advanced significantly and currently about 30% of the marketed drugs are covalent inhibitors. The numerous advant...

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Detalles Bibliográficos
Autores principales: Sutanto, Fandi, Konstantinidou, Markella, Dömling, Alexander
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Royal Society of Chemistry 2020
Materias:
Chemistry
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7557570/
https://www.ncbi.nlm.nih.gov/pubmed/33479682
http://dx.doi.org/10.1039/d0md00154f
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author Sutanto, Fandi
Konstantinidou, Markella
Dömling, Alexander
author_facet Sutanto, Fandi
Konstantinidou, Markella
Dömling, Alexander
author_sort Sutanto, Fandi
collection PubMed
description Covalent inhibitors are recognized as an important component in drug discovery and therapeutics. Since the first appearance of covalent inhibitors in the late 18th century, the field has advanced significantly and currently about 30% of the marketed drugs are covalent inhibitors. The numerous advantages of covalent inhibitors are counteracting the initial concerns regarding potential off-target toxicity. Thus, continuous research, especially for cancer targets is reported. The aim of this review is to provide a short historic overview and focus on recently developed covalent inhibitors (2011–2019), including structural aspects and examples on challenging targets.
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spelling pubmed-75575702020-10-30 Covalent inhibitors: a rational approach to drug discovery Sutanto, Fandi Konstantinidou, Markella Dömling, Alexander RSC Med Chem Chemistry Covalent inhibitors are recognized as an important component in drug discovery and therapeutics. Since the first appearance of covalent inhibitors in the late 18th century, the field has advanced significantly and currently about 30% of the marketed drugs are covalent inhibitors. The numerous advantages of covalent inhibitors are counteracting the initial concerns regarding potential off-target toxicity. Thus, continuous research, especially for cancer targets is reported. The aim of this review is to provide a short historic overview and focus on recently developed covalent inhibitors (2011–2019), including structural aspects and examples on challenging targets. Royal Society of Chemistry 2020-07-02 /pmc/articles/PMC7557570/ /pubmed/33479682 http://dx.doi.org/10.1039/d0md00154f Text en This journal is © The Royal Society of Chemistry 2020 http://creativecommons.org/licenses/by-nc/3.0/ This article is freely available. This article is licensed under a Creative Commons Attribution Non Commercial 3.0 Unported Licence (CC BY-NC 3.0)
spellingShingle Chemistry
Sutanto, Fandi
Konstantinidou, Markella
Dömling, Alexander
Covalent inhibitors: a rational approach to drug discovery
title Covalent inhibitors: a rational approach to drug discovery
title_full Covalent inhibitors: a rational approach to drug discovery
title_fullStr Covalent inhibitors: a rational approach to drug discovery
title_full_unstemmed Covalent inhibitors: a rational approach to drug discovery
title_short Covalent inhibitors: a rational approach to drug discovery
title_sort covalent inhibitors: a rational approach to drug discovery
topic Chemistry
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7557570/
https://www.ncbi.nlm.nih.gov/pubmed/33479682
http://dx.doi.org/10.1039/d0md00154f
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AT konstantinidoumarkella covalentinhibitorsarationalapproachtodrugdiscovery
AT domlingalexander covalentinhibitorsarationalapproachtodrugdiscovery

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