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

MedChemComm
Wenjia WangAlexander Dömling

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.

References

Jun 1, 1996·The Journal of Experimental Medicine·F FossiezS Lebecque
Jul 12, 2002·Chemical Communications : Chem Comm·Dudley H WilliamsRosa Zerella
Oct 16, 2004·Immunity·Jay K Kolls, Anders Lindén
Jun 21, 2006·The Journal of Immunology : Official Journal of the American Association of Immunologists·Dean ToyJacques Peschon
Jun 27, 2006·The Journal of Biological Chemistry·Fang ShenSarah L Gaffen
Oct 13, 2006·The Journal of Biological Chemistry·Seon Hee ChangChen Dong
Jul 2, 2008·Nature Reviews. Drug Discovery·Edward M DriggersNicholas K Terrett
Oct 20, 2009·Nature Immunology·Lauren K ElyK Christopher Garcia
Nov 18, 2011·Journal of Chemical Information and Modeling·Bernd KuhnNeil R Taylor
Aug 4, 2012·Future Medicinal Chemistry·Jamie Mallinson, Ian Collins
May 23, 2013·Nature Communications·Shenping LiuMatthew C Griffor
Sep 21, 2013·Journal of Medicinal Chemistry·Fabrizio Giordanetto, Jan Kihlberg
Jul 10, 2014·The New England Journal of Medicine·Richard G LangleyUNKNOWN FIXTURE Study Group
Feb 9, 2016·Journal of Medicinal Chemistry·Alfonso EspadaJeffrey A Dodge
May 18, 2016·Scientific Reports·Shenping LiuLauren D Wood
Aug 17, 2016·Scientific Reports·Shenping LiuAtli Thorarensen

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Citations

Jun 9, 2021·Journal of Medicinal Chemistry·Sanja KoštrunMartin Stahlhut
Dec 4, 2020·Journal of Chemical Information and Modeling·Atilio Reyes RomeroAlexander Dömling
Aug 19, 2021·Immunological Reviews·Matthew G ThompsonStacy M Horner
Aug 19, 2018·Biomedicine & Pharmacotherapy = Biomédecine & Pharmacothérapie·Gamal AllamAsmaa M Gaber

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