Democratized Discovery of Microsclerodermin F as an Immunophilin Ligand Article Swipe

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Computational biology Drug discovery Medicine Chemistry Biology Bioinformatics

Manfred Auer , Malcolm D. Walkinshaw , Jacqueline Dornan , Nhan T. Pham , Xinru Xue , Miaomiao Liu , Ronald J. Quinn , Eric J. Ross , Abimael D. Rodrı́guez , James J. La Clair ·

YOU? · · 2025 · Open Access · · DOI: https://doi.org/10.3390/md23090336 · OA: W4413480462

While immunophilins are well-recognized therapeutic targets, several members of this family of peptidyl-proline isomerases (PPIases) have yet to be subjected to ligand discovery efforts. In this study, we demonstrate a cost-effective means to identify ligands to the insufficiently investigated two-domain PPIase human Cyclophilin40 (Cyp40). Central to this effort was the use of beads, wherein a confocal nanoscanning (CONA) approach was used to rapidly probe candidates. Here, we describe how one can adapt the physical nature of microsized beads as a means to strategically reduce cost and ultimately make the discovery of small molecule hit and lead compounds more accessible to everyone irrespective of financial status (democratization).