G protein-coupled receptors (GPCRs)

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Unique positive cooperativity between the β-arrestin-biased β-blocker Carvedilol and a small molecule positive allosteric modulator of the β2-Adrenergic Receptor
Biswaranjan Pani, Seungkirl Ahn, Paula K Rambarat, Shashank Vege, Alem W. Kahsai, Andrew Liu, Bruno N Valan, Dean P Staus, Tommaso Costa and Robert J. Lefkowitz

Molecular Pharmacology September 27, 2021, MOLPHARM-AR-2021-000363; DOI: https://doi.org/10.1124/molpharm.121.000363
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β-arrestin-biased allosteric modulator potentiates Carvedilol stimulated β adrenergic receptor cardioprotection
Jialu Wang, Biswaranjan Pani, Ilhan Gokhan, Xinyu Xiong, Alem W. Kahsai, Haoran Jiang, Seungkirl Ahn, Robert J. Lefkowitz and Howard A Rockman

Molecular Pharmacology September 24, 2021, MOLPHARM-AR-2021-000359; DOI: https://doi.org/10.1124/molpharm.121.000359
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High-content single-cell FRET imaging of cultured striatal neurons reveals novel cross-talk in the regulation of nuclear signalling by PKA and ERK1/2
Jace Jones-Tabah, Ryan D. Martin, Jason C. Tanny, Paul B.S. Clarke and Terence E. Hebert

Molecular Pharmacology September 9, 2021, MOLPHARM-AR-2021-000290; DOI: https://doi.org/10.1124/molpharm.121.000290
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Pharmacological characterization of the imipridone anti-cancer drug ONC201 reveals a negative allosteric mechanism of action at the D₂ dopamine receptor
R. Benjamin Free, Caroline A Cuoco, Bing Xie, Yoon Namkung, Varun V. Prabhu, Blair K.A. Willette, Marilyn M. Day, Marta Sanchez-Soto, J. Robert Lane, Stephane A. Laporte, Lei Shi, Joshua E. Allen and David R. Sibley

Molecular Pharmacology August 5, 2021, MOLPHARM-AR-2021-000336; DOI: https://doi.org/10.1124/molpharm.121.000336
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CPL207280 - a novel GPR40/FFA1-specific agonist shows a favorable safety profile and exerts anti-diabetic effects in type 2 diabetic animals.
Katarzyna Bazydlo-Guzenda, Pawel Buda, Mikolaj Matloka, Mateusz Mach, Filip Stelmach, Radoslaw Dzida, Damian Smuga, Joanna Hucz-Kalitowska, Malgorzata Teska-Kaminska, Varvara Vialichka, Krzysztof Dubiel, Bozena Kaminska, Maciej Wieczorek and Jerzy Pieczykolan

Molecular Pharmacology August 4, 2021, MOLPHARM-AR-2021-000260; DOI: https://doi.org/10.1124/molpharm.121.000260
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Membrane-facilitated receptor access and binding mechanisms of long-acting β2-adrenergic receptor (β2-AR) agonists
Christopher T. Szlenk, Jeevan B. GC and Senthil Natesan

Molecular Pharmacology August 1, 2021, MOLPHARM-AR-2021-000285; DOI: https://doi.org/10.1124/molpharm.121.000285
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Acylation of the incretin peptide exendin-4 directly impacts GLP-1 receptor signalling and trafficking
Maria Lucey, Tanyel Ashik, Amaara Marzook, Yifan Wang, Joelle Goulding, Atsuro Oishi, Johannes Broichhagen, David J Hodson, James Minnion, Yuval Elani, Ralf Jockers, Steven J Briddon, Stephen R Bloom, Alejandra Tomas and Ben Jones

Molecular Pharmacology July 27, 2021, MOLPHARM-AR-2021-000270; DOI: https://doi.org/10.1124/molpharm.121.000270

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