Artificial Macrocycles as IL-17A/IL-17RA Antagonists.
Artificial Macrocycles as IL-17A/IL-17RA Antagonists.
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DOI：
10.1039/c7md00464h
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发表时间：
2018-01-01
期刊：
影响因子：
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通讯作者：
Dömling A
中科院分区：
文献类型：
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作者：
Wang W;Groves MR;Dömling A
白细胞介素17(A)是一种促炎细胞因子，参与多种自身免疫性和炎症性疾病。目前在临床试验中显示有效的针对IL17(A)或其受体（IL17R）的拮抗剂是单克隆抗体（mab）。然而，最近设计的人工大环是有效的IL17-IL17R拮抗剂。基于共晶结构，我们对大环的生物活性和SAR有了更深入的了解，表明大环可以与单克隆抗体在PPIs等困难靶点上竞争。
Interleukin 17(A) is a pro-inflammatory cytokine involved in several auto-immune and inflammatory diseases. Current antagonists against IL17(A) or its receptor (IL17R) that show efficacy in clinical trials are monoclonal-antibodies (mAbs). However, recently designed artificial macrocyles are potent IL17-IL17R antagonists. Based on Co-crystal structures, a better understanding the biological activity and SAR of the macrocycles has been elucidated, demonstrating that macrocycles can compete with mAbs for difficult targets such as PPIs.