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Structural Biology of the TNFα Antagonists Used in the Treatment of Rheumatoid Arthritis

Department of Chemistry, Konkuk University, 120 Neungdong-ro, Gwangjin-gu, Seoul 05029, Korea
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Int. J. Mol. Sci. 2018, 19(3), 768; https://doi.org/10.3390/ijms19030768
Received: 8 February 2018 / Revised: 6 March 2018 / Accepted: 6 March 2018 / Published: 7 March 2018
(This article belongs to the Special Issue Research of Pathogenesis and Novel Therapeutics in Arthritis)
The binding of the tumor necrosis factor α (TNFα) to its cognate receptor initiates many immune and inflammatory processes. The drugs, etanercept (Enbrel®), infliximab (Remicade®), adalimumab (Humira®), certolizumab-pegol (Cimzia®), and golimumab (Simponi®), are anti-TNFα agents. These drugs block TNFα from interacting with its receptors and have enabled the development of breakthrough therapies for the treatment of several autoimmune inflammatory diseases, including rheumatoid arthritis, Crohn’s disease, and psoriatic arthritis. In this review, we describe the latest works on the structural characterization of TNFα–TNFα antagonist interactions related to their therapeutic efficacy at the atomic level. A comprehensive comparison of the interactions of the TNFα blockers would provide a better understanding of the molecular mechanisms by which they neutralize TNFα. In addition, an enhanced understanding of the higher order complex structures and quinary structures of the TNFα antagonists can support the development of better biologics with the improved pharmacokinetic properties. Accumulation of these structural studies can provide a basis for the improvement of therapeutic agents against TNFα for the treatment of rheumatoid arthritis and other autoimmune inflammatory diseases in which TNFα plays an important role in pathogenesis. View Full-Text
Keywords: TNFα; etanercept; infliximab; adalimumab; certolizumab pegol; golimumab; rheumatoid arthritis; therapeutic antibody; structure TNFα; etanercept; infliximab; adalimumab; certolizumab pegol; golimumab; rheumatoid arthritis; therapeutic antibody; structure
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MDPI and ACS Style

Lim, H.; Lee, S.H.; Lee, H.T.; Lee, J.U.; Son, J.Y.; Shin, W.; Heo, Y.-S. Structural Biology of the TNFα Antagonists Used in the Treatment of Rheumatoid Arthritis. Int. J. Mol. Sci. 2018, 19, 768.

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