Perspective for Discovery of Small Molecule IL-6 Inhibitors through Study of Structure-Activity Relationships and Molecular Docking

Hossam Nada, Aneesh Sivaraman, Qili Lu, Kyoungho Min, Sungdo Kim, Ja Il Goo, Yongseok Choi, Kyeong Lee

Research output: Contribution to journalReview articlepeer-review

20 Scopus citations

Abstract

Interleukin-6 (IL-6) is a proinflammatory cytokine that plays a key role in the pathogenesis and physiology of inflammatory and autoimmune diseases, such as coronary heart disease, cancer, Alzheimer’s disease, asthma, rheumatoid arthritis, and most recently COVID-19. IL-6 and its signaling pathway are promising targets in the treatment of inflammatory and autoimmune diseases. Although, anti-IL-6 monoclonal antibodies are currently being used in clinics, huge unmet medical needs remain because of the high cost, administration-related toxicity, lack of opportunity for oral dosing, and potential immunogenicity of monoclonal antibody therapy. Furthermore, nonresponse or loss of response to monoclonal antibody therapy has been reported, which increases the importance of optimizing drug therapy with small molecule drugs. This work aims to provide a perspective for the discovery of novel small molecule IL-6 inhibitors by the analysis of the structure-activity relationships and computational studies for protein-protein inhibitors targeting the IL-6/IL-6 receptor/gp130 complex.

Original languageEnglish
Pages (from-to)4417-4433
Number of pages17
JournalJournal of Medicinal Chemistry
Volume66
Issue number7
DOIs
StatePublished - 13 Apr 2023

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