Democratized Discovery of Microsclerodermin F as an Immunophilin Ligand

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Auer, Manfred
Walkinshaw, Malcolm D
Dornan, Jacqueline
Pham, Nhan T
Xue, Xinru
Liu, Miaomiao
Quinn, Ronald J
Ross, Eric M
Rodríguez, Abimael D
La Clair, James J
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2025
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Abstract

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).

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Marine Drugs

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23

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9

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© 2025 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).

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Chemical oceanography

Pharmacology and pharmaceutical sciences

Physical chemistry

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Auer, M; Walkinshaw, MD; Dornan, J; Pham, NT; Xue, X; Liu, M; Quinn, RJ; Ross, EM; Rodríguez, AD; La Clair, JJ, Democratized Discovery of Microsclerodermin F as an Immunophilin Ligand, Marine Drugs, 2025, 23 (9), pp. 336

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