Artificial macrocycles as IL-17A/IL-17RA antagonists

Wenjia Wang; Matthew R. Groves; Alexander Domling

doi:10.1039/c7md00464h

Artificial macrocycles as IL-17A/IL-17RA antagonists

Wenjia Wang, Matthew R. Groves, Alexander Domling^*

^*Corresponding author for this work

Research output: Contribution to journal › Review article › peer-review

9 Citations (Scopus)

Abstract

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.

Original language	English
Pages (from-to)	22-26
Number of pages	5
Journal	MedChemCommun
Volume	9
Issue number	1
DOIs	https://doi.org/10.1039/c7md00464h
Publication status	Published - Jan-2018

Keywords

DRUG DISCOVERY
BINDING-SITE
T-CELLS
INTERLEUKIN-17
RECEPTOR
INFLAMMATION
IL-17A
COMBINATION
AUTOIMMUNE
CYTOKINES

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10.1039/c7md00464h

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Artificial macrocycles as IL-17A IL-17RA antagonists
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Cite this

@article{cd0cc19f5a894c23a4321ea9c0813ee4,

title = "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 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.",

keywords = "DRUG DISCOVERY, BINDING-SITE, T-CELLS, INTERLEUKIN-17, RECEPTOR, INFLAMMATION, IL-17A, COMBINATION, AUTOIMMUNE, CYTOKINES",

author = "Wenjia Wang and Groves, {Matthew R.} and Alexander Domling",

year = "2018",

month = jan,

doi = "10.1039/c7md00464h",

language = "English",

volume = "9",

pages = "22--26",

journal = "MedChemCommun",

issn = "2040-2503",

publisher = "ROYAL SOC CHEMISTRY",

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T1 - Artificial macrocycles as IL-17A/IL-17RA antagonists

AU - Wang, Wenjia

AU - Groves, Matthew R.

AU - Domling, Alexander

PY - 2018/1

Y1 - 2018/1

N2 - 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.

AB - 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.

KW - DRUG DISCOVERY

KW - BINDING-SITE

KW - T-CELLS

KW - INTERLEUKIN-17

KW - RECEPTOR

KW - INFLAMMATION

KW - IL-17A

KW - COMBINATION

KW - AUTOIMMUNE

KW - CYTOKINES

U2 - 10.1039/c7md00464h

DO - 10.1039/c7md00464h

M3 - Review article

VL - 9

SP - 22

EP - 26

JO - MedChemCommun

JF - MedChemCommun

SN - 2040-2503

IS - 1

ER -