Covalent inhibitors design and discovery

S De Cesco, J Kurian, C Dufresne… - European Journal of …, 2017 - Elsevier
In the history of therapeutics, covalent drugs occupy a very distinct category. While
representing a significant fraction of the drugs on the market, very few have been …

Drug discovery considerations in the development of covalent inhibitors

R Mah, JR Thomas, CM Shafer - Bioorganic & medicinal chemistry letters, 2014 - Elsevier
In recent years, the number of drug candidates with a covalent mechanism of action
progressing through clinical trials or being approved by the FDA has increased significantly …

Recent advances in the development of covalent inhibitors

H Kim, YS Hwang, M Kim, SB Park - RSC Medicinal Chemistry, 2021 - pubs.rsc.org
The use of covalent inhibitors in the field of drug discovery has attracted considerable
attention in the 2000s. As a result, more than 50 covalent drugs are currently on the market …

Covalent versus non-covalent enzyme inhibition: which route should we take? A justification of the good and bad from molecular modelling perspective

A Aljoundi, I Bjij, A El Rashedy, MES Soliman - The protein journal, 2020 - Springer
The pace and efficiency of drug target strategies have been emanating debates among
researchers in the field of drug development. Covalent inhibitors possess significant …

Structure-based design of targeted covalent inhibitors

R Lonsdale, RA Ward - Chemical Society Reviews, 2018 - pubs.rsc.org
Covalent inhibition is a rapidly growing discipline within drug discovery. Many historical
covalent inhibitors were discovered by serendipity, with such a mechanism of action often …

New electrophiles and strategies for mechanism-based and targeted covalent inhibitor design

S Ray, AS Murkin - Biochemistry, 2019 - ACS Publications
Covalent inhibitors are experiencing a growing resurgence in drug design and are an
increasingly useful tool in molecular biology. The ability to attach inhibitors to their targets by …

Drug discovery for a new generation of covalent drugs

AS Kalgutkar, DK Dalvie - Expert opinion on drug discovery, 2012 - Taylor & Francis
Introduction: The design of target-specific covalent inhibitors is conceptually attractive
because of increased biochemical efficiency through covalency and increased duration of …

10 years into the resurgence of covalent drugs

E De Vita - Future Medicinal Chemistry, 2021 - Taylor & Francis
In the first decade of targeted covalent inhibition, scientists have successfully reversed the
previous trend that had impeded the use of covalent inhibition in drug development …

Covalent inhibitors: a rational approach to drug discovery

F Sutanto, M Konstantinidou, A Dömling - RSC medicinal chemistry, 2020 - pubs.rsc.org
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 …

The taxonomy of covalent inhibitors

A Tuley, W Fast - Biochemistry, 2018 - ACS Publications
Covalent enzyme inhibitors are widely applied as biochemical tools and therapeutic agents.
As a complement to categorization of these inhibitors by reactive group or modification site …