Ján Jakubík

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.

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.

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.

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.