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强效环状四肽解毒铅中毒。

Potent Cyclic Tetrapeptide for Lead Detoxification.

机构信息

Department of Chemistry, University of Zurich, Winterthurerstrasse 190, 8057, Zurich, Switzerland.

Institute of Organic Chemistry and Biochemistry, Czech Academy of Sciences, Flemingovo náměstí 2, 16610, Praha 6, Czech Republic.

出版信息

Angew Chem Int Ed Engl. 2021 May 25;60(22):12381-12385. doi: 10.1002/anie.202103217. Epub 2021 Apr 28.

DOI:10.1002/anie.202103217
PMID:33759306
Abstract

Lead (Pb) is a ubiquitous poisonous metal, affecting the health of vast populations worldwide. Medications to treat Pb poisoning suffer from various limitations and are often toxic owing to insufficient metal selectivity. Here, we report a cyclic tetrapeptide that selectively binds Pb and eradicates its toxic effect on the cellular level, with superior potency than state-of-the-art drugs. The Pb-peptide complex is remarkably strong and was characterized experimentally and computationally. Accompanied by the lack of toxicity and enhanced stability of this peptide, these qualities indicate its merit as a potential remedy for Pb poisoning.

摘要

铅(Pb)是一种普遍存在的有毒金属,影响着全球广大人群的健康。用于治疗铅中毒的药物存在各种局限性,而且往往由于金属选择性不足而具有毒性。在这里,我们报告了一种环状四肽,它选择性地结合铅并消除其在细胞水平上的毒性作用,其效力优于最先进的药物。Pb-肽复合物非常强,实验和计算都对其进行了表征。由于这种肽缺乏毒性和稳定性增强,这些特性表明它有潜力成为治疗铅中毒的一种潜在药物。

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