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Binding site elucidation and structure guided design of macrocyclic IL-17A antagonists
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 ser...
Autores principales: | , , , , , , , , , , , , , , , , , , , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Nature Publishing Group
2016
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4985813/ https://www.ncbi.nlm.nih.gov/pubmed/27527709 http://dx.doi.org/10.1038/srep30859 |
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author | Liu, Shenping Dakin, Leslie A. Xing, Li Withka, Jane M. Sahasrabudhe, Parag V. Li, Wei Banker, Mary Ellen Balbo, Paul Shanker, Suman Chrunyk, Boris A. Guo, Zuojun Chen, Jinshan M. Young, Jennifer A. Bai, Guoyun Starr, Jeremy T. Wright, Stephen W. Bussenius, Joerg Tan, Sheng Gopalsamy, Ariamala Lefker, Bruce A. Vincent, Fabien Jones, Lyn H. Xu, Hua Hoth, Lise R. Geoghegan, Kieran F. Qiu, Xiayang Bunnage, Mark E. Thorarensen, Atli |
author_facet | Liu, Shenping Dakin, Leslie A. Xing, Li Withka, Jane M. Sahasrabudhe, Parag V. Li, Wei Banker, Mary Ellen Balbo, Paul Shanker, Suman Chrunyk, Boris A. Guo, Zuojun Chen, Jinshan M. Young, Jennifer A. Bai, Guoyun Starr, Jeremy T. Wright, Stephen W. Bussenius, Joerg Tan, Sheng Gopalsamy, Ariamala Lefker, Bruce A. Vincent, Fabien Jones, Lyn H. Xu, Hua Hoth, Lise R. Geoghegan, Kieran F. Qiu, Xiayang Bunnage, Mark E. Thorarensen, Atli |
author_sort | Liu, Shenping |
collection | PubMed |
description | 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. |
format | Online Article Text |
id | pubmed-4985813 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2016 |
publisher | Nature Publishing Group |
record_format | MEDLINE/PubMed |
spelling | pubmed-49858132016-08-22 Binding site elucidation and structure guided design of macrocyclic IL-17A antagonists Liu, Shenping Dakin, Leslie A. Xing, Li Withka, Jane M. Sahasrabudhe, Parag V. Li, Wei Banker, Mary Ellen Balbo, Paul Shanker, Suman Chrunyk, Boris A. Guo, Zuojun Chen, Jinshan M. Young, Jennifer A. Bai, Guoyun Starr, Jeremy T. Wright, Stephen W. Bussenius, Joerg Tan, Sheng Gopalsamy, Ariamala Lefker, Bruce A. Vincent, Fabien Jones, Lyn H. Xu, Hua Hoth, Lise R. Geoghegan, Kieran F. Qiu, Xiayang Bunnage, Mark E. Thorarensen, Atli Sci Rep Article 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. Nature Publishing Group 2016-08-16 /pmc/articles/PMC4985813/ /pubmed/27527709 http://dx.doi.org/10.1038/srep30859 Text en Copyright © 2016, The Author(s) http://creativecommons.org/licenses/by/4.0/ This work is licensed under a Creative Commons Attribution 4.0 International License. The images or other third party material in this article are included in the article’s Creative Commons license, unless indicated otherwise in the credit line; if the material is not included under the Creative Commons license, users will need to obtain permission from the license holder to reproduce the material. To view a copy of this license, visit http://creativecommons.org/licenses/by/4.0/ |
spellingShingle | Article Liu, Shenping Dakin, Leslie A. Xing, Li Withka, Jane M. Sahasrabudhe, Parag V. Li, Wei Banker, Mary Ellen Balbo, Paul Shanker, Suman Chrunyk, Boris A. Guo, Zuojun Chen, Jinshan M. Young, Jennifer A. Bai, Guoyun Starr, Jeremy T. Wright, Stephen W. Bussenius, Joerg Tan, Sheng Gopalsamy, Ariamala Lefker, Bruce A. Vincent, Fabien Jones, Lyn H. Xu, Hua Hoth, Lise R. Geoghegan, Kieran F. Qiu, Xiayang Bunnage, Mark E. Thorarensen, Atli Binding site elucidation and structure guided design of macrocyclic IL-17A antagonists |
title | Binding site elucidation and structure guided design of macrocyclic IL-17A antagonists |
title_full | Binding site elucidation and structure guided design of macrocyclic IL-17A antagonists |
title_fullStr | Binding site elucidation and structure guided design of macrocyclic IL-17A antagonists |
title_full_unstemmed | Binding site elucidation and structure guided design of macrocyclic IL-17A antagonists |
title_short | Binding site elucidation and structure guided design of macrocyclic IL-17A antagonists |
title_sort | binding site elucidation and structure guided design of macrocyclic il-17a antagonists |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4985813/ https://www.ncbi.nlm.nih.gov/pubmed/27527709 http://dx.doi.org/10.1038/srep30859 |
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