Eva Dolejší

Dualsteric and dual-acting modulation of muscarinic receptors by antagonist KH-5

This study investigates KH-5's dualsteric and dual-acting modulation of muscarinic receptors, finding it acts as a dualsteric antagonist at M1 receptors and competitive antagonist at M2 receptors.

Steroid-based Tide Quencher 1 probes enable real-time mapping of novel non-canonical cholesterol sites on the M1 muscarinic receptor

This paper introduces TQ1 probes to map non-canonical cholesterol-binding sites on the M1 muscarinic receptor, showing improved quenching and binding specificity compared to Dabcyl.

Balancing Rigidity and Flexibility: Optimised 4-(Hexyloxy)benzoate Antagonists with Enhanced Affinity and Tuneable Duration at Muscarinic Receptors

This study synthesizes and evaluates 4-(hexyloxy)benzoate derivatives to optimize muscarinic receptor antagonists, finding that rigid groups increase affinity but reduce duration, while flexible analogues balance potency and residence time.