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Literature DB >> 29750108

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

Wenjia Wang¹, Matthew R Groves¹, Alexander Dömling¹.

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.

Entities: Chemical Disease Gene Mutation Species

Year: 2017 PMID： 29750108 PMCID： PMC5937545 DOI： 10.1039/C7MD00464H

Source DB: PubMed Journal: Medchemcomm ISSN： 2040-2503 Impact factor: 3.597

25 in total

1. A Binding Site on IL-17A for Inhibitory Macrocycles Revealed by Hydrogen/Deuterium Exchange Mass Spectrometry.

Authors: Alfonso Espada; Howard Broughton; Spencer Jones; Michael J Chalmers; Jeffrey A Dodge
Journal: J Med Chem Date: 2016-02-18 Impact factor: 7.446

2. Cutting edge: interleukin 17 signals through a heteromeric receptor complex.

Authors: Dean Toy; David Kugler; Martin Wolfson; Tim Vanden Bos; Jesse Gurgel; Jonathan Derry; Joel Tocker; Jacques Peschon
Journal: J Immunol Date: 2006-07-01 Impact factor: 5.422

Review 3. Macrocyclic drugs and clinical candidates: what can medicinal chemists learn from their properties?

Authors: Fabrizio Giordanetto; Jan Kihlberg
Journal: J Med Chem Date: 2013-09-17 Impact factor: 7.446

Review 4. The exploration of macrocycles for drug discovery--an underexploited structural class.

Authors: Edward M Driggers; Stephen P Hale; Jinbo Lee; Nicholas K Terrett
Journal: Nat Rev Drug Discov Date: 2008-07 Impact factor: 84.694

5. The combination of tumor necrosis factor alpha blockade with interleukin-1 and interleukin-17 blockade is more effective for controlling synovial inflammation and bone resorption in an ex vivo model.

Authors: M Chabaud; P Miossec
Journal: Arthritis Rheum Date: 2001-06

6. Combination of IL-17 and TNFα induces a pro-inflammatory, pro-coagulant and pro-thrombotic phenotype in human endothelial cells.

Authors: Arnaud Hot; Vanina Lenief; Pierre Miossec
Journal: Ann Rheum Dis Date: 2012-01-18 Impact factor: 19.103

7. Molecular characterization of the human interleukin (IL)-17 receptor.

Authors: Z Yao; M K Spriggs; J M Derry; L Strockbine; L S Park; T VandenBos; J D Zappone; S L Painter; R J Armitage
Journal: Cytokine Date: 1997-11 Impact factor: 3.861

8. Secukinumab in plaque psoriasis--results of two phase 3 trials.

Authors: Richard G Langley; Boni E Elewski; Mark Lebwohl; Kristian Reich; Christopher E M Griffiths; Kim Papp; Lluís Puig; Hidemi Nakagawa; Lynda Spelman; Bárður Sigurgeirsson; Enrique Rivas; Tsen-Fang Tsai; Norman Wasel; Stephen Tyring; Thomas Salko; Isabelle Hampele; Marianne Notter; Alexander Karpov; Silvia Helou; Charis Papavassilis
Journal: N Engl J Med Date: 2014-07-09 Impact factor: 91.245

Review 9. Macrocycles in new drug discovery.

Authors: Jamie Mallinson; Ian Collins
Journal: Future Med Chem Date: 2012-07 Impact factor: 3.808

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

1. A Binding Site on IL-17A for Inhibitory Macrocycles Revealed by Hydrogen/Deuterium Exchange Mass Spectrometry.

2. Cutting edge: interleukin 17 signals through a heteromeric receptor complex.

Review 3. Macrocyclic drugs and clinical candidates: what can medicinal chemists learn from their properties?

Review 4. The exploration of macrocycles for drug discovery--an underexploited structural class.

5. The combination of tumor necrosis factor alpha blockade with interleukin-1 and interleukin-17 blockade is more effective for controlling synovial inflammation and bone resorption in an ex vivo model.

6. Combination of IL-17 and TNFα induces a pro-inflammatory, pro-coagulant and pro-thrombotic phenotype in human endothelial cells.

7. Molecular characterization of the human interleukin (IL)-17 receptor.

8. Secukinumab in plaque psoriasis--results of two phase 3 trials.

Review 9. Macrocycles in new drug discovery.

10. Rationalizing tight ligand binding through cooperative interaction networks.

1. Artificial Macrocycles by Ugi Reaction and Passerini Ring Closure.

Review 2. How RNA modifications regulate the antiviral response.

3. Multicomponent Macrocyclic IL-17a Modifier.

4. Conformation of the Macrocyclic Drug Lorlatinib in Polar and Nonpolar Environments: A MD Simulation and NMR Study.

5. Benchmark of Generic Shapes for Macrocycles.