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Artificial Macrocycles as IL-17A/IL-17RA Antagonists.


ABSTRACT: 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.

SUBMITTER: Wang W 

PROVIDER: S-EPMC5937545 | biostudies-literature | 2018 Jan

REPOSITORIES: biostudies-literature

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Artificial Macrocycles as IL-17A/IL-17RA Antagonists.

Wang Wenjia W   Groves Matthew R MR   Dömling Alexander A  

MedChemComm 20171025 1


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 m  ...[more]

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