Toll-like Receptor Agonist Conjugation: A Chemical Perspective.
Toll-like Receptor Agonist Conjugation: A Chemical Perspective.
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DOI：
10.1021/acs.bioconjchem.7b00808
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发表时间：
2018-03-21
影响因子：
4.7
通讯作者：
Verdoes, Martijn
中科院分区：
文献类型：
--
作者：
Ignacio, Bob J.;Albin, Tyler J.;Esser-Kahn, Aaron P.;Verdoes, Martijn
Toll 样受体 (TLR) 是哺乳动物免疫系统的重要组成部分，通过识别病原体相关分子模式 (PAMP)、桥接先天免疫和适应性免疫发挥作用。它们已成为治疗传染病、癌症和过敏的重要治疗靶点，许多 TLR 激动剂目前正在进行临床试验或被批准作为免疫刺激剂。大量研究表明，TLR 激动剂与其他分子的缀合可以有益地影响其效力、毒性、药代动力学或功能。然而，TLR 激动剂缀合物的功能特性高度依赖于所采用的连接策略。在这里，我们回顾了有效的功能性 TLR 激动剂缀合的化学结构要求。此外，我们还为那些尚未缀合的化合物提供类似的分析。此外，我们还讨论了共价 TLR 激动剂缀合的应用及其对临床应用的影响。
Toll-like receptors (TLRs) are vital elements of the mammalian immune system that function by recognizing pathogen-associated molecular patterns (PAMPs), bridging innate and adaptive immunity. They have become a prominent therapeutic target for the treatment of infectious diseases, cancer, and allergies, with many TLR agonists currently in clinical trials or approved as immunostimulants. Numerous studies have shown that conjugation of TLR agonists to other molecules can beneficially influence their potency, toxicity, pharmacokinetics, or function. The functional properties of TLR agonist conjugates, however, are highly dependent on the ligation strategy employed. Here, we review the chemical structural requirements for effective functional TLR agonist conjugation. In addition, we provide similar analysis for those that have yet to be conjugated. Moreover, we discuss applications of covalent TLR agonist conjugation and their implications for clinical use.
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影响因子：
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作者：
Bode C;Zhao G;Steinhagen F;Kinjo T;Klinman DM
通讯作者：
Klinman DM
影响因子：
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Carson, Dennis A.
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通讯作者：
Cottamt, Howard B.
影响因子：
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作者：
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Flavell, RA