疫苗佐剂QS-7-Api的合成与结构验证。对同质皂树免疫刺激剂的合成方法。
Synthesis and structure verification of the vaccine adjuvant QS-7-Api. Synthetic access to homogeneous Quillaja saponaria immunostimulants.
作者信息
Deng Kai, Adams Michelle M, Gin David Y
机构信息
Memorial Sloan-Kettering Cancer Center, 1275 York Avenue, New York, New York 10065, USA.
出版信息
J Am Chem Soc. 2008 May 7;130(18):5860-1. doi: 10.1021/ja801008m. Epub 2008 Apr 15.
Abstract
QS-7-Api is an exceedingly potent immuno-adjuvant isolated from the bark of Quillaja saponaria. It is significantly less toxic than QS-21, a related saponin that is currently the favored adjuvant in anticancer and antiviral vaccine clinical trials. Tedious isolation/purification protocols and uncertainty in its structural constitution have hindered the clinical development of QS-7. A chemical synthesis of QS-7-Api is described, providing structural verification of the adjuvant. A novel semisynthetic sequence to QS-7-Api has also been established, greatly facilitating access to QS-7 for preclinical and clinical evaluation.
摘要
QS-7-Api是一种从皂树树皮中分离出来的极具效力的免疫佐剂。它的毒性明显低于QS-21，QS-21是一种相关的皂苷，目前是抗癌和抗病毒疫苗临床试验中最常用的佐剂。繁琐的分离/纯化方案及其结构组成的不确定性阻碍了QS-7的临床开发。本文描述了QS-7-Api的化学合成方法，对该佐剂进行了结构验证。还建立了一种合成QS-7-Api的新型半合成方法，极大地促进了QS-7用于临床前和临床评估。
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