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Author

Jeffrey Aubé

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Open access Aug 2026

Dynamic view of an allosteric intermediate in a positively cooperative dimer

Positive cooperativity in ligand binding is a hallmark of allosteric oligomers, yet how the first binding event enhances the second remains obscure, because the pivotal singly-bound intermediate (lig₁) is thermodynamically disfavored and rarely accumulates. Distinguishing concerted (MWC) from sequential (KNF) mechanism...

P. J. Sapienza, T. Mileur, M. S. Khan et al. · 0 citations
Open access Aug 2026

Discovery of Highly Potent G Protein-Biased Bisamide Kappa Opioid Receptor Agonists.

Kappa opioid receptor (KOR) agonists are used clinically to treat chronic itch and are promising candidates for the treatment of pain and other maladies. Unfortunately, adverse effects have hampered the widespread clinical development of KOR agonists. Preferentially stimulating the G protein activation pathway over the...

Kimberly S. Taylor, Kerri M. Czekner, Aubrie A. Harland et al. · 0 citations

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