Drug intelligence / Profile preview

gaillardin

Development stage: Preclinical
Modality: Small Molecules

Overview

Gaillardin is a sesquiterpene lactone phytochemical that functions as a structural and functional modulator of tumor necrosis factor-alpha (TNF-alpha). It interacts with TNF-alpha through hydrogen bonding and van der Waals contacts (specifically involving residues GLN47 and ASP45), which stabilizes the protein's beta-sheet architecture and enhances its resistance to unfolding. In preclinical models of colorectal cancer, gaillardin has been shown to significantly increase the apoptotic activity of TNF-alpha, effectively lowering the IC50 and potentially addressing TNF-alpha hyporesponsiveness in tumor cells.

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