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Updated: Jan 19, 2026
Covalent Binding of BMP-2 on Surfaces Using a Self-assembled Monolayer Approach
Published on: August 26, 2013
One-step Heck Reaction Generates Nonimmunosuppressive FK506 Analogs for Pharmacological BMP Activation
Yuefan Wang1, Brandon J Peiffer1, Qi Su2
1Department of Pharmacology and Molecular Sciences, Johns Hopkins School of Medicine and the SJ Yan and HJ Mao Laboratory of Chemical Biology, Johns Hopkins School of Medicine, Baltimore, Maryland 21205, United States.
Abstract:
FKBP12 ligands such as FK506 have been shown to activate the BMP signaling pathway and facilitate tissue regeneration. However, the immunosuppressive activity of FK506 limits its clinical application. Using Heck reaction, we generated nonimmunosuppressive analogs of FK506 by fusing heterocycles to the calcineurin (CN) binding domain of FK506. Structure-activity relationships provided novel mechanistic insights into the FK506-CN interaction that can be exploited for rational design of future analogs.
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