Covalent inhibitors: A rational approach to drug discovery

Fandi Sutanto; Markella Konstantinidou; Alexander Domling

doi:10.1039/d0md00154f

Covalent inhibitors: A rational approach to drug discovery

Fandi Sutanto, Markella Konstantinidou, Alexander Domling^*

^*Corresponding author for this work

Research output: Contribution to journal › Review article › peer-review

250 Citations (Scopus)

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Abstract

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.

Original language	English
Pages (from-to)	876-884
Number of pages	9
Journal	Medicinal chemistry
Volume	11
Issue number	8
DOIs	https://doi.org/10.1039/d0md00154f
Publication status	Published - 1-Aug-2020

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POTENT

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abstract = "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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AB - 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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Covalent inhibitors: A rational approach to drug discovery

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