Carbohydrate-Small Molecule Hybrids as Lead Compounds Targeting IL-6 Signaling.

ABSTRACT: In the past 25 years, a number of efforts have been made toward the development of small molecule interleukin-6 (IL-6) signaling inhibitors, but none have been approved to date. Monosaccharides are a diverse class of bioactive compounds, but thus far have been unexplored as a scaffold for small molecule IL-6-signaling inhibitor design. Therefore, in this present communication, we combined a structure-based drug design approach with carbohydrate building blocks to design and synthesize novel IL-6-signaling inhibitors targeting glycoprotein 130 (gp130). Of this series of compounds, LS-TG-2P and LS-TF-3P were the top lead compounds, displaying IC₅₀ values of 6.9 and 16 µM against SUM159 cell lines, respectively, while still retaining preferential activity against the

SUBMITTER: Schultz DC 

PROVIDER: S-EPMC9861960 | biostudies-literature | 2023 Jan

REPOSITORIES: biostudies-literature