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Cyclic Octapeptides Composed of Two Glutathione Units Outperform the Monomer in Lead Detoxification
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SYSNO ASEP 0557865 Document Type J - Journal Article R&D Document Type Journal Article Subsidiary J Článek ve WOS Title Cyclic Octapeptides Composed of Two Glutathione Units Outperform the Monomer in Lead Detoxification Author(s) Sauser, L. (CH)
Kalvoda, Tadeáš (UOCHB-X) ORCID
Kavas, A. (CH)
Rulíšek, Lubomír (UOCHB-X) RID, ORCID
Shoshan, M. S. (CH)Article number e202200152 Source Title ChemMedChem. - : Wiley - ISSN 1860-7179
Roč. 17, č. 15 (2022)Number of pages 7 s. Language eng - English Country DE - Germany Keywords lead ; peptides ; chelates ; glutathione ; bioinoganic chemistry OECD category Physical chemistry R&D Projects GA20-08772S GA ČR - Czech Science Foundation (CSF) Method of publishing Open access Institutional support UOCHB-X - RVO:61388963 UT WOS 000799312900001 EID SCOPUS 85130498319 DOI 10.1002/cmdc.202200152 Annotation A rationally-designed scaffold of cyclic octapeptides composed of two units of the natural tripeptide glutathione (GSH) was optimized to strongly and selectively capture toxic lead ions (Pb(II)). Using state-of-the-art computational tools, a list of eleven plausible peptides was shortened to five analogs based on their calculated affinity to Pb(II) ions. We then synthesized and investigated them for their abilities to recover Pb-poisoned human cells. A clear pattern was observed from the in vitro detoxification results, indicating the importance of cavity size and polar moieties to enhance metal capturing. These, together with the apparent benefit of cyclizing the peptides, improved the detoxification of the two lead peptides by approximately two folds compared to GSH and the benchmark chelating agents against Pb poisoning. Moreover, the two peptides did not show any toxicity and, therefore, were thoroughly investigated to determine their potential as next-generation remedies for Pb poisoning. Workplace Institute of Organic Chemistry and Biochemistry Contact asep@uochb.cas.cz ; Kateřina Šperková, Tel.: 232 002 584 ; Viktorie Chládková, Tel.: 232 002 434 Year of Publishing 2023 Electronic address https://doi.org/10.1002/cmdc.202200152
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