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Updated: Aug 11, 2026

Structure-Guided Design and Development of Novel Cyclophilin A Inhibitors and Ganoderiol-F Derivatives: An In-Silico Approach
Published on: June 23, 2026
Screening, synthesis and structural characterization of a novel bicyclic peptide inhibiting α7 nicotinic
Xichu Yang1, Kele Cui1, Xiuxiu Cao1
1Hefei National Laboratory for Physical Sciences at the Microscale, Department of Clinical Laboratory, The First Affiliated Hospital of USTC, Division of Life Sciences and Medicine, Anhui Provincial Engineering Laboratory of Peptide Drugs, University of Science and Technology of China (USTC), Hefei 230026, China. dmsun@ustc.edu.cn.
Abstract:
Peptides targeting the α7 nicotinic acetylcholine receptor (α7-nAChR) represent promising candidates for therapeutic and chemical probe development. Here, we identified a novel bicyclic peptide KP1877 via phage-displayed peptide library screening followed by chemical synthesis of active analogs. Structural characterization reveals KP1877 adopts a unique bicyclic conformation distinct from known natural α7-nAChR-targeting peptides, and exerts potent inhibitory effect by stabilizing the closed, non-conducting state of the receptor via orthosteric binding.
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