NOD2受体激动药MDP构效关系研究进展

马晓雪,陈旭东,杨洋,李雪,隋强

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主办:上海医药工业研究院
   中国药学会
   中国化学制药工业协会
ISSN 1001-8255   CN 31-1243/R   ZYGZEA
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中国医药工业杂志 ›› 2021, Vol. 52 ›› Issue (12) : 1584-1594. DOI: 10.16522/j.cnki.cjph.2021.12.004
专论与综述 Perspectives & Review

NOD2受体激动药MDP构效关系研究进展

作者信息 +

Research Progress in the Structure-activity Relationship of NOD2 Agonist MDP

Author information +
History +

摘要

胞壁酰二肽(muramyl dipeptide,MDP)是细菌细胞骨架中具有免疫佐剂活性的最小结构单元,可与核苷酸结合寡聚化结构域蛋白2(nucleotide-binding oligomerization domain-containing protein 2,NOD2)结合并发挥免疫调节作用。MDP具有佐剂、抗肿瘤、抗感染等生物活性,但因其细胞渗透能力差,在生物体内易被清除,存在催眠、致热等不良反应,应用受到一定的限制。化学结构修饰是提高MDP生物活性、减轻不良反应的一种手段。本研究总结了近年来对其结构中二肽以及糖环C1位、C2位、C4位、C6位进行修饰的MDP类似物的构效关系,期望可为设计活性较高、不良反应少的新型免疫佐剂提供思路。

Abstract

Muramyl dipeptide(MDP) is the minimal active structural unit with adjuvanticity in bacterial cytoskeletons, which can respond to nucleotide-binding oligomerization domain-containing protein 2(NOD2) and participate in immunomodulatory. MDP has extensive biological activities such as adjuvanticity, antitumor and antiinfection, while the application is limited due to its poor cellular penetration, rapid elimination, hypnosis and pyrogenicity. Chemical structure modification is a practical approach to improving biological activities and reducing toxic side effects. In this review, the structure-activity relationships of MDP analogs with modification of the dipeptide and C1, C2, C4, C6 in the sugar ring were summarized, providing the strategy for designing novel adjuvants with high activity and low toxic side effects.

关键词

胞壁酰二肽 / 构效关系 / 生物活性

Key words

muramyl dipeptide / structure-activity relationship / biological activity

引用本文

导出引用
马晓雪,陈旭东,杨洋,李雪,隋强. NOD2受体激动药MDP构效关系研究进展. 中国医药工业杂志. 2021, 52(12): 1584-1594 https://doi.org/10.16522/j.cnki.cjph.2021.12.004
MA Xiaoxue, CHEN Xudong, YANG Yang, LI Xue, SUI Qiang. Research Progress in the Structure-activity Relationship of NOD2 Agonist MDP. Chinese Journal of Pharmaceuticals. 2021, 52(12): 1584-1594 https://doi.org/10.16522/j.cnki.cjph.2021.12.004

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