Interleukin 17(A) is a pro-inflammatory cytokine involved in several auto-immune and inflammatory diseases. Current antagonists against IL-17(A) or its receptor (IL-17RA) that show efficacy in clinical trials are monoclonal antibodies (mAbs). However, recently designed artificial macrocycles are potent IL-17A/IL-17RA antagonists. Based on co-crystal structures, a better understanding of the biological activity and SAR of the macrocycles has been gained, demonstrating that they can compete with mAbs for difficult targets such as PPIs.

中文翻译：

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人工大环化合物作为IL-17A / IL- 17RA拮抗剂

白介素17（A）是一种促炎性细胞因子，参与多种自身免疫性疾病和炎症性疾病。在临床试验中显示功效的当前针对IL-17（A）或其受体（IL- 17RA）的拮抗剂是单克隆抗体（mAbs）。但是，最近设计的人工大环化合物是有效的IL-17A / IL- 17RA拮抗剂。基于共晶体结构，人们已经对大环的生物活性和SAR有了更好的了解，这表明它们可以与mAb竞争诸如PPI的困难靶标。