Alena Randáková

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.

Cholesterol differentially modulates the activity of opioid and muscarinic receptors via common binding site

This study identifies a shared non-canonical cholesterol-binding site at TM6 in muscarinic and opioid receptors, with significant implications for drug development targeting tissue-specific GPCR modulation.