How Carvedilol activates β2-adrenoceptors

Autor: Tobias Benkel, Mirjam Zimmermann, Julian Zeiner, Sergi Bravo, Nicole Merten, Victor Jun Yu Lim, Edda Sofie Fabienne Matthees, Julia Drube, Elke Miess-Tanneberg, Daniela Malan, Martyna Szpakowska, Stefania Monteleone, Jak Grimes, Zsombor Koszegi, Yann Lanoiselée, Shannon O’Brien, Nikoleta Pavlaki, Nadine Dobberstein, Asuka Inoue, Viacheslav Nikolaev, Davide Calebiro, Andy Chevigné, Philipp Sasse, Stefan Schulz, Carsten Hoffmann, Peter Kolb, Maria Waldhoer, Katharina Simon, Jesus Gomeza, Evi Kostenis

Publikováno v: Nature Communications, Vol 13, Iss 1, Pp 1-20 (2022)

Abstract Carvedilol is among the most effective β-blockers for improving survival after myocardial infarction. Yet the mechanisms by which carvedilol achieves this superior clinical profile are still unclear. Beyond blockade of β1-adrenoceptors, ar

Externí odkaz: https://doaj.org/article/31913551d70443ecbc6be0521f89476a

Lack of beta-arrestin signaling in the absence of active G proteins

Autor: Manuel Grundmann, Nicole Merten, Davide Malfacini, Asuka Inoue, Philip Preis, Katharina Simon, Nelly Rüttiger, Nicole Ziegler, Tobias Benkel, Nina Katharina Schmitt, Satoru Ishida, Ines Müller, Raphael Reher, Kouki Kawakami, Ayumi Inoue, Ulrike Rick, Toni Kühl, Diana Imhof, Junken Aoki, Gabriele M. König, Carsten Hoffmann, Jesus Gomeza, Jürgen Wess, Evi Kostenis

Publikováno v: Nature Communications, Vol 9, Iss 1, Pp 1-16 (2018)

Arrestins terminate signaling from GPCRs, but several lines of evidence suggest that they are also able to transduce signals independently of G proteins. Here, the authors systematically ablate G proteins in cell lines, and show that arrestins are un

Externí odkaz: https://doaj.org/article/e038d4ec42a84fe0b5f232ccf68a180d

The atypical chemokine receptor ACKR3/CXCR7 is a broad-spectrum scavenger for opioid peptides

Autor: Jochen Ohnmacht, Vincent Seutin, Evi Kostenis, Max Marc Roger Meyrath, Markus Ollert, Julian Zeiner, Katharina Simon, Rejko Krüger, Martyna Szpakowska, Andy Chevigné, Myriam P. Merz, Laurent Massotte, Jonathan D. Turner, Tobias Benkel

Publikováno v: Nature Communications, Vol 11, Iss 1, Pp 1-16 (2020)
Nature Communications
Meyrath, M, Szpakowska, M, Zeiner, J, Massotte, L, Merz, M P, Benkel, T, Simon, K, Ohnmacht, J, Turner, J D, Krüger, R, Seutin, V, Ollert, M, Kostenis, E & Chevigné, A 2020, ' The atypical chemokine receptor ACKR3/CXCR7 is a broad-spectrum scavenger for opioid peptides ', Nature Communications, vol. 11, 3033 . https://doi.org/10.1038/s41467-020-16664-0

Endogenous opioid peptides and prescription opioid drugs modulate pain, anxiety and stress by activating opioid receptors, currently classified into four subtypes. Here we demonstrate that ACKR3/CXCR7, hitherto known as an atypical scavenger receptor

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8e3b6474cc994903ceec0b560bf4f575
http://link.springer.com/article/10.1038/s41467-020-16664-0

Deciphering Specificity Determinants for FR900359-Derived Gqα Inhibitors Based on Computational and Structure-Activity Studies

Autor: Charlotte A. Bäuml, Evi Kostenis, Daniel Tietze, Tobias Benkel, Desireé Kaufmann, Max Crüsemann, Toni Kühl, Stefan Kehraus, Raphael Reher, Justin Patrick Odhiambo, Britta Nubbemeyer, Suvi Annala, Diana Imhof, Gabriele M. König, Pascal Heimer

Publikováno v: ChemMedChem. 13:1634-1643

Direct targeting of intracellular Gα subunits of G protein-coupled receptors by chemical tools is a challenging task in current pharmacological studies and in the development of novel therapeutic approaches. In this study we analyzed novel FR900359-

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::05eccf1f87ce43469c8c7aa866a539f1
https://doi.org/10.1002/cmdc.201800304

BIM-46174 fragments as potential ligands of G proteins

Autor: Evi Kostenis, Suvi Annala, Jim Küppers, Michael Gütschow, Gregor Schnakenburg, Tobias Benkel

Publikováno v: Medchemcomm

The 5,6,7,8-tetrahydroimidazo[1,2-a]pyrazine derivative BIM-46174 has received attention as Gα(q) inhibitor. We conducted structural reductions to monocyclic and bicyclic substructures to explore the chemical space of BIM fragments and to gain insig

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a40a2e3f5b1188a1e4dca7b7706b59a3
https://pubmed.ncbi.nlm.nih.gov/32180917