Exploring covalent inhibitors of SARS-CoV-2 main protease: from peptidomimetics to novel scaffolds

被引：0
作者：
Atatreh, Noor [1 ,2 ]
Mahgoub, Radwa E. [1 ,2 ]
Ghattas, Mohammad A. [1 ,2 ]
机构：
[1] Al Ain Univ, Coll Pharm, Abu Dhabi, U Arab Emirates
[2] Al Ain Univ, AAU Hlth & Biomed Res Ctr, Abu Dhabi, U Arab Emirates
来源：
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY | 2025年 / 40卷 / 01期
关键词：
Anti-viral; irreversible inhibition; covalent inhibitor; Covid-19; warheads reactivity; PEPTIDE ALDEHYDE INHIBITORS; COV M-PRO; 3C-LIKE PROTEASE; CRYSTAL-STRUCTURES; DESIGN; DISCOVERY; PROTEINASE; REVEALS; TARGET; SITE;
D O I：
10.1080/14756366.2025.2460045
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
Peptidomimetic inhibitors mimic natural peptide substrates, employing electrophilic warheads to covalently interact with the catalytic Cys145 of Mpro. Examples include aldehydes, alpha-ketoamides, and aza-peptides, with discussions on their mechanisms of action, potency, and structural insights. Non-peptidomimetic inhibitors utilise diverse scaffolds and mechanisms, achieving covalent modification of Mpro.
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页数：26
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