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zilucoplan 的化学合成与补体 C5 抑制肽的特性分析。

Chemical synthesis and characterisation of the complement C5 inhibitory peptide zilucoplan.

机构信息

School of Biomedical Sciences, The University of Queensland, Brisbane, Australia.

Queensland Brain Institute, The University of Queensland, Brisbane, Australia.

出版信息

Amino Acids. 2021 Jan;53(1):143-147. doi: 10.1007/s00726-020-02921-5. Epub 2021 Jan 4.

Abstract

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.

摘要

补体成分 C5 抑制剂zilucoplan 目前正处于重症肌无力 (MG) 的 III 期临床试验阶段。尽管处于临床开发的后期阶段,但目前文献中尚无详细描述其化学合成的报道。在这项工作中,我们描述了一种zilucoplan 的化学合成方法,并验证了合成化合物可阻断 LPS 诱导的人血液中 C5a 的产生。

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