Binding site elucidation and structure guided design of macrocyclic IL-17A antagonists

Shenping Liu, Leslie A. Dakin,Li Xing,Jane M. Withka,Parag V. Sahasrabudhe,Wei Li,Mary Ellen Banker,Paul Balbo, Suman Shanker,Boris A. Chrunyk,Zuojun Guo, Jinshan M. Chen,Jennifer A. Young,Guoyun Bai,Jeremy T. Starr,Stephen W. Wright, Joerg Bussenius, Sheng Tan,Ariamala Gopalsamy,Bruce A. Lefker,Fabien Vincent,Lyn H. Jones,Hua Xu,Lise R. Hoth,Kieran F. Geoghegan,Xiayang Qiu,Mark E. Bunnage,Atli Thorarensen

SCIENTIFIC REPORTS（2016）

引用 38|浏览46

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摘要

Interleukin-17A (IL-17A) is a principal driver of multiple inflammatory and immune disorders. Antibodies that neutralize IL-17A or its receptor (IL-17RA) deliver efficacy in autoimmune diseases, but no small-molecule IL-17A antagonists have yet progressed into clinical trials. Investigation of a series of linear peptide ligands to IL-17A and characterization of their binding site has enabled the design of novel macrocyclic ligands that are themselves potent IL-17A antagonists.

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关键词

Acute inflammation,Lead optimization,Structure-based drug design,Science,Humanities and Social Sciences,multidisciplinary

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