Chemical synthesis and characterisation of the complement C5 inhibitory peptide zilucoplan

The complement component C5 inhibitory peptide zilucoplan is currently in phase III clinical trials for myasthenia gravis (MG). Despite being at an advanced stage of clinical development, there have been no published reports in the literature detailing its chemical synthesis. In this work, we descri...

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Detalles Bibliográficos
Autores principales: Gorman, Declan M., Lee, John, Payne, Colton D., Woodruff, Trent M., Clark, Richard J.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Springer Vienna 2021
Materias:
Short Communication
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7781173/
https://www.ncbi.nlm.nih.gov/pubmed/33398524
http://dx.doi.org/10.1007/s00726-020-02921-5
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author Gorman, Declan M.
Lee, John
Payne, Colton D.
Woodruff, Trent M.
Clark, Richard J.
author_facet Gorman, Declan M.
Lee, John
Payne, Colton D.
Woodruff, Trent M.
Clark, Richard J.
author_sort Gorman, Declan M.
collection PubMed
description The complement component C5 inhibitory peptide zilucoplan is currently in phase III clinical trials for myasthenia gravis (MG). Despite being at an advanced stage of clinical development, there have been no published reports in the literature detailing its chemical synthesis. In this work, we describe an approach for the chemical synthesis of zilucoplan and validate that the synthesised compound blocks LPS-induced C5a production from human blood. ELECTRONIC SUPPLEMENTARY MATERIAL: The online version of this article (10.1007/s00726-020-02921-5) contains supplementary material, which is available to authorized users.
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spelling pubmed-77811732021-01-05 Chemical synthesis and characterisation of the complement C5 inhibitory peptide zilucoplan Gorman, Declan M. Lee, John Payne, Colton D. Woodruff, Trent M. Clark, Richard J. Amino Acids Short Communication The complement component C5 inhibitory peptide zilucoplan is currently in phase III clinical trials for myasthenia gravis (MG). Despite being at an advanced stage of clinical development, there have been no published reports in the literature detailing its chemical synthesis. In this work, we describe an approach for the chemical synthesis of zilucoplan and validate that the synthesised compound blocks LPS-induced C5a production from human blood. ELECTRONIC SUPPLEMENTARY MATERIAL: The online version of this article (10.1007/s00726-020-02921-5) contains supplementary material, which is available to authorized users. Springer Vienna 2021-01-04 2021 /pmc/articles/PMC7781173/ /pubmed/33398524 http://dx.doi.org/10.1007/s00726-020-02921-5 Text en © Springer-Verlag GmbH Austria, part of Springer Nature 2021 This article is made available via the PMC Open Access Subset for unrestricted research re-use and secondary analysis in any form or by any means with acknowledgement of the original source. These permissions are granted for the duration of the World Health Organization (WHO) declaration of COVID-19 as a global pandemic.
spellingShingle Short Communication
Gorman, Declan M.
Lee, John
Payne, Colton D.
Woodruff, Trent M.
Clark, Richard J.
Chemical synthesis and characterisation of the complement C5 inhibitory peptide zilucoplan
title Chemical synthesis and characterisation of the complement C5 inhibitory peptide zilucoplan
title_full Chemical synthesis and characterisation of the complement C5 inhibitory peptide zilucoplan
title_fullStr Chemical synthesis and characterisation of the complement C5 inhibitory peptide zilucoplan
title_full_unstemmed Chemical synthesis and characterisation of the complement C5 inhibitory peptide zilucoplan
title_short Chemical synthesis and characterisation of the complement C5 inhibitory peptide zilucoplan
title_sort chemical synthesis and characterisation of the complement c5 inhibitory peptide zilucoplan
topic Short Communication
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7781173/
https://www.ncbi.nlm.nih.gov/pubmed/33398524
http://dx.doi.org/10.1007/s00726-020-02921-5
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