A Photoswitchable Ligand Targeting the β₁ -Adrenoceptor Enables Light-Control of the Cardiac Rhythm.

ABSTRACT: Catecholamine-triggered β-adrenoceptor (β-AR) signaling is essential for the correct functioning of the heart. Although both β₁ - and β₂ -AR subtypes are expressed in cardiomyocytes, drugs selectively targeting β₁ -AR have proven this receptor as the main target for the therapeutic effects of beta blockers in the heart. Here, we report a new strategy for the light-control of β₁ -AR activation by means of photoswitchable drugs with a high level of β₁ -/β₂ -AR selectivity. All reported molecules allow for an efficient real-time optical control of receptor function in vitro. Moreover, using confocal microscopy we demonstrate that the binding of our best hit, pAzo-2, can be reversibly photocontrolled. Strikingly, pAzo-2 also ena

SUBMITTER: Duran-Corbera A 

PROVIDER: S-EPMC9401038 | biostudies-literature | 2022 Jul

REPOSITORIES: biostudies-literature