质谱分析显示β-内酰胺类药物可能成为 SARS-CoV-2 M 蛋白抑制剂。
Mass spectrometry reveals potential of β-lactams as SARS-CoV-2 M inhibitors.
机构信息
Chemistry Research Laboratory, Department of Chemistry, 12 Mansfield Road, Oxford, OX1 3TA, UK.
Diamond Light Source, Harwell Science & Innovation Campus, Didcot, Oxfordshire OX11 0DE, UK and Research Complex at Harwell, Harwell Science & Innovation Campus, Didcot, Oxfordshire OX11 0FA, UK.
出版信息
Chem Commun (Camb). 2021 Feb 15;57(12):1430-1433. doi: 10.1039/d0cc06870e.
The main viral protease (Mpro) of SARS-CoV-2 is a nucleophilic cysteine hydrolase and a current target for anti-viral chemotherapy. We describe a high-throughput solid phase extraction coupled to mass spectrometry Mpro assay. The results reveal some β-lactams, including penicillin esters, are active site reacting Mpro inhibitors, thus highlighting the potential of acylating agents for Mpro inhibition.
新型冠状病毒的主要病毒蛋白酶（Mpro）是一种亲核半胱氨酸水解酶，也是当前抗病毒化学疗法的靶标。我们描述了一种高通量固相萃取与质谱联用的 Mpro 测定法。结果表明，一些β-内酰胺类药物，包括青霉素酯，是活性部位反应的 Mpro 抑制剂，这突出了酰化剂对 Mpro 抑制的潜力。
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