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

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Standard

A Photoswitchable Ligand Targeting the β1‐Adrenoceptor Enables Light‐Control of the Cardiac Rhythm. / Duran-Corbera, Anna; Faria, Melissa; Ma, Yuanyuan; Prats, Eva; Dias, Andre; Catena, Juanlo; Martinez, Karen L.; Raldua, Demetrio; Llebaria, Amadeu; Rovira, Xavier.

I: Angewandte Chemie International Edition, Bind 61, Nr. 30, 202203449, 2022.

Publikation: Bidrag til tidsskrift › Tidsskriftartikel › Forskning › fagfællebedømt

Harvard

Duran-Corbera, A, Faria, M, Ma, Y, Prats, E, Dias, A, Catena, J, Martinez, KL, Raldua, D, Llebaria, A & Rovira, X 2022, 'A Photoswitchable Ligand Targeting the β1‐Adrenoceptor Enables Light‐Control of the Cardiac Rhythm', Angewandte Chemie International Edition, bind 61, nr. 30, 202203449. https://doi.org/10.1002/ange.202203449, https://doi.org/10.1002/anie.202203449

APA

Duran-Corbera, A., Faria, M., Ma, Y., Prats, E., Dias, A., Catena, J., Martinez, K. L., Raldua, D., Llebaria, A., & Rovira, X. (2022). A Photoswitchable Ligand Targeting the β1‐Adrenoceptor Enables Light‐Control of the Cardiac Rhythm. Angewandte Chemie International Edition, 61(30), [202203449]. https://doi.org/10.1002/ange.202203449, https://doi.org/10.1002/anie.202203449

Vancouver

Duran-Corbera A, Faria M, Ma Y, Prats E, Dias A, Catena J o.a. A Photoswitchable Ligand Targeting the β1‐Adrenoceptor Enables Light‐Control of the Cardiac Rhythm. Angewandte Chemie International Edition. 2022;61(30). 202203449. https://doi.org/10.1002/ange.202203449, https://doi.org/10.1002/anie.202203449

Author

Duran-Corbera, Anna ; Faria, Melissa ; Ma, Yuanyuan ; Prats, Eva ; Dias, Andre ; Catena, Juanlo ; Martinez, Karen L. ; Raldua, Demetrio ; Llebaria, Amadeu ; Rovira, Xavier. / A Photoswitchable Ligand Targeting the β1‐Adrenoceptor Enables Light‐Control of the Cardiac Rhythm. I: Angewandte Chemie International Edition. 2022 ; Bind 61, Nr. 30.

Bibtex

@article{c7a497b753164eaab11c377c20b7bc1e,
title = "A Photoswitchable Ligand Targeting the β1‐Adrenoceptor Enables Light‐Control of the Cardiac Rhythm",
abstract = "Catecholamine-triggered beta-adrenoceptor (beta-AR) signaling is essential for the correct functioning of the heart. Although both beta(1)- and beta(2)-AR subtypes are expressed in cardiomyocytes, drugs selectively targeting beta(1)-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 beta(1)-AR activation by means of photoswitchable drugs with a high level of beta(1)-/beta(2)-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 enables a dynamic cardiac rhythm management on living zebrafish larvae using light, thus highlighting the therapeutic and research potential of the developed photoswitches. Overall, this work provides the first proof of precise control of the therapeutic target beta(1)-AR in native environments using light.",
keywords = "Azobenzene, Beta-1 Adrenoceptors, Drug Design, Light-Regulated Ligands, Photochromism, BETA-ADRENERGIC-RECEPTORS, PHARMACOLOGY, SELECTIVITY, ANTAGONISTS, DISRUPTION, AGONISTS",
author = "Anna Duran-Corbera and Melissa Faria and Yuanyuan Ma and Eva Prats and Andre Dias and Juanlo Catena and Martinez, {Karen L.} and Demetrio Raldua and Amadeu Llebaria and Xavier Rovira",
year = "2022",
doi = "10.1002/ange.202203449",
language = "English",
volume = "61",
journal = "Angewandte Chemie International Edition",
issn = "1433-7851",
publisher = "Wiley-VCH Verlag GmbH & Co. KGaA",
number = "30",

}

RIS

TY - JOUR

T1 - A Photoswitchable Ligand Targeting the β1‐Adrenoceptor Enables Light‐Control of the Cardiac Rhythm

AU - Duran-Corbera, Anna

AU - Faria, Melissa

AU - Ma, Yuanyuan

AU - Prats, Eva

AU - Dias, Andre

AU - Catena, Juanlo

AU - Martinez, Karen L.

AU - Raldua, Demetrio

AU - Llebaria, Amadeu

AU - Rovira, Xavier

PY - 2022

Y1 - 2022

N2 - Catecholamine-triggered beta-adrenoceptor (beta-AR) signaling is essential for the correct functioning of the heart. Although both beta(1)- and beta(2)-AR subtypes are expressed in cardiomyocytes, drugs selectively targeting beta(1)-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 beta(1)-AR activation by means of photoswitchable drugs with a high level of beta(1)-/beta(2)-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 enables a dynamic cardiac rhythm management on living zebrafish larvae using light, thus highlighting the therapeutic and research potential of the developed photoswitches. Overall, this work provides the first proof of precise control of the therapeutic target beta(1)-AR in native environments using light.

AB - Catecholamine-triggered beta-adrenoceptor (beta-AR) signaling is essential for the correct functioning of the heart. Although both beta(1)- and beta(2)-AR subtypes are expressed in cardiomyocytes, drugs selectively targeting beta(1)-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 beta(1)-AR activation by means of photoswitchable drugs with a high level of beta(1)-/beta(2)-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 enables a dynamic cardiac rhythm management on living zebrafish larvae using light, thus highlighting the therapeutic and research potential of the developed photoswitches. Overall, this work provides the first proof of precise control of the therapeutic target beta(1)-AR in native environments using light.

KW - Azobenzene

KW - Beta-1 Adrenoceptors

KW - Drug Design

KW - Light-Regulated Ligands

KW - Photochromism

KW - BETA-ADRENERGIC-RECEPTORS

KW - PHARMACOLOGY

KW - SELECTIVITY

KW - ANTAGONISTS

KW - DISRUPTION

KW - AGONISTS

U2 - 10.1002/ange.202203449

DO - 10.1002/ange.202203449

M3 - Journal article

C2 - 35608051

VL - 61

JO - Angewandte Chemie International Edition

JF - Angewandte Chemie International Edition

SN - 1433-7851

IS - 30

M1 - 202203449

ER -

ID: 309204006