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Results found for "Franziska M Heydenreich"
- 📰 GPCR Weekly News, December 18 to 31, 2023
Franziska M Heydenreich, Michel Bouvier, Brian Kobilka, M Madan Babu, and their team's work on Molecular
- Disentangling bias between G q, GRK2, and arrestin3 recruitment to the M 3 muscarinic acetylcholine
G protein-coupled receptors (GPCRs) transmit extracellular signals to the inside by activation of intracellular effector proteins. Different agonists can promote differential receptor-induced signaling responses - termed bias - potentially by eliciting different levels of recruitment of effector proteins. As activation and recruitment of effector proteins might influence each other, thorough analysis of bias is difficult. Here, we compared the efficacy of seven agonists to induce G protein, G protein-coupled receptor kinase 2 (GRK2), as well as arrestin3 binding to the muscarinic acetylcholine receptor M3 by utilizing FRET-based assays. In order to avoid interference between these interactions, we studied GRK2 binding in the presence of inhibitors of Gi and Gq proteins and analyzed arrestin3 binding to prestimulated M3 receptors to avoid differences in receptor phosphorylation influencing arrestin recruitment. We measured substantial differences in the agonist efficacies to induce M3R-arrestin3 versus M3R-GRK2 interaction. However, the rank order of the agonists for G protein- and GRK2-M3R interaction was the same, suggesting that G protein and GRK2 binding to M3R requires similar receptor conformations, whereas requirements for arrestin3 binding to M3R are distinct. Read full article
- Targeted Drug Design through GPCR Mutagenesis: Insights from β2AR
To achieve this, the work of Heydenreich et al. (2023) will be analysed to demonstrate how mutagenesis www.ecosystem.drgpcr.com/post/decoding-gpcr-function-the-role-of-mutagenesis-in-rational-drug-discovery Heydenreich M., Marti-Solano, M., Sandhu, M., Kobilka, B. K., Bouvier, M., & Babu, M. M. (2023). Howard, M. K., Hoppe, N., Huang, X. P., Macdonald, C. B., Mehrota, E., Grimes, P.
- Decoding GPCR Function: The Role of Mutagenesis in Rational Drug Discovery
For instance, Heydenreich et al. (2023) developed a data science framework that combined mutagenesis Heydenreich, F. M., Marti-Solano, M., Sandhu, M., Kobilka, B. K., Bouvier, M., & Babu, M. Kosar, M., Sarott, R. C., Sykes, D. A., Viray, A. E., Vitale, R. M., Tomašević, N., ... & Carreira, E. M. (2024). M., Christopoulos, A., & May, L. T. (2016).
- 📰 GPCR Weekly News, February 5 to 11, 2024
Magdalena M Scharf, Antonella Di Pizio, Ines Liebscher, Hannes Schihada, and Gunnar Schulte et al. on Franziska Heydenreich, Sudarshan Rajagopal, Graham Ladds, Cesare Orlandi and Michel Bouvier.
- 📰 GPCR Weekly News, February 12 to 18, 2024
Nayara Braga Emidio, Ross Cheloha, Laura M Wingler, et al. for their work on Nanobody-Mediated Dualsteric Franziska Heydenreich, Sudarshan Rajagopal, Graham Ladds, and Michel Bouvier.
- 📰 GPCR Weekly News, March 4 to 10, 2024
Franziska Heydenreich, Sudarshan Rajagopal, Graham Ladds, Cesare Orlandi, Simone Prömel and Michel Bouvier
- 📰 GPCR Weekly News, February 26 to March 3, 2024
Franziska Heydenreich, Sudarshan Rajagopal, Graham Ladds, Cesare Orlandi, Simone Prömel and Michel Bouvier
- 📰 GPCR Weekly News, January 22 to 28, 2024
Franziska Heydenreich, Sudarshan Rajagopal, Graham Ladds, and Michel Bouvier We will also have a poster
- Unlocking Cell's Secrets: Spontaneous β-Arrestin-Membrane Preassociation Drives Receptor-Activation
M., Medel-Lacruz, B., Baidya, M., Makarova, M., Mistry, R., Goulding, J., Drube, J., Hoffmann, C., Owen M., Shukla, A. K., Selent, J., Hill, S. J., & Calebiro, D. (2023). H., Heydenreich, F. M., Kawakami, K., Masureel, M., Maeda, S., Garcia, K. C., von Zastrow, M., Inoue, A., & Kobilka, B. K. (2022). I., & von Zastrow, M. (2001).
- 📰 GPCR Weekly News, February 19 to 25, 2024
Franziska Heydenreich, Sudarshan Rajagopal, Graham Ladds, Cesare Orlandi, Simone Prömel and Michel Bouvier
- 📰 GPCR Weekly News, January 29 to February 4, 2024
Franziska Heydenreich, Sudarshan Rajagopal, Graham Ladds, and Michel Bouvier.
- A robust and Efficient FRET-Based Assay for Cannabinoid Receptor Ligands Discovery.
M.; Compton, D. R.; Martin, B. R.; Abood, M. E. , M. C.; Westphal, M. V.; Mostinski, Y.; Mach, L.; Wasinska-Kalwa, M.; Weise, M.; Hoare, B. .; Maccarrone, M.; Veprintsev, D. B.; Carreira, E. M.; Grether, U.; Nazaré, M. F.; Nicolotti, O.; Perrone, M. G.; Brea, J.; Loza, M. I.; Infantino, V.; Abate, C.; Contino, M.
- An overview of the compartmentalized GPCR Signaling: Relevance and Implications
E., Healy, M. D., & Collins, B. M. (2019). , Gonçalves-Monteiro, S., Vieira-Rocha, M. M., & Lefkowitz, R. J. (2003). B., Conti, M., & von Zastrow, M. (2017). M., & Murray, F. (2018).
- Fluorescence based HTS compatible ligand binding assays for dopamine D3 receptors in baculovirus preparations and live cells
M.; Bucolo, C.; Platania, C. B. M.; Salomone, S.; Drago, F. W.; Högl, B.; Bainbridge, J.; Buchfuhrer, M.; Hadjigeorgiou, G.; Inoue, Y.; Manconi, M.; Oertel, W.; -J.; Kopanchuk, S.; Laasfeld, T.; Weinhart, M.; Schollmeyer, D.; Betschart, M. .; Keller, M. H.; Bates, M.; Zhuang, X.
- From DNA day to GPCR genomics
G., Frielle, T., Bolanowski, M. A., Bennett, C. D., Rands, E., Diehl, R. E., Mumford, R. S., Caron, M. G., Lefkowitz, R. J., & Strader, C. D. (1986). Nature, 321(6065), 75–79. https://doi.org/10.1038/321075a0 Fredriksson, R., Lagerström, M. M., Pérez-Hernández, G., Batebi, H., Gao, Y., Eskici, G., Seven, A. B., Panova, O., Hilger, D., Casiraghi, M., He, F., Maul, L., Gmeiner, P., Kobilka, B.
- 📰 GPCR Weekly News, April 24 to 30, 2023
Galien Foundation Announces 2023 Prix Galien UK Award Candidates Exscientia Appoints Harvard Professor Franziska
- The Perils and Guardrails of Modifying Signalling Proteins in Bioassays
Butlen-Ducuing F, Pétavy F, Guizzaro L, Zienowicz M, Salmonson T, Haas M, et al. Wouters OJ, McKee M, Luyten J. Schlander M, Hernandez-Villafuerte K, Cheng CY, Mestre-Ferrandiz J, Baumann M. Yamaguchi S, Kaneko M, Narukawa M. Persechino M, Hedderich JB, Kolb P, Hilger D.
- Harnessing Deep Mutational Scanning for Enhanced Drug Discovery
M. (2011). Deep mutational scanning: assessing protein function on a massive scale. M., Stephany, J. J., & Fields, S. (2014). Nature Protocols , 9 (9), 2267–2284. https://doi.org/10.1038/nprot.2014.153 Howard, M. M., Trinidad, D. D., English, J. G., Coyote-Maestas, W., & Aashish Manglik. (2024).
- Dynamic GPCR activation revealed through time-resolved Cryo-EM
A recent breakthrough study published in Nature by Makaía M. Papasergi-Scott, M. M. et al. Time-resolved cryo-EM of G-protein activation by a GPCR.
- Nanobodies: New Dimensions in GPCR Signaling Research
K., Odongo, S., Radwanska, M., & Magez, S. (2023). M., Thian, F. S., Kobilka, T. S., Schnapp, A., Konetzki, I., Sunahara, R. K., Gellman, S. M., Manglik, A., Hu, J., Hu, K., Eitel, K., Hübner, H., Pardon, E., Valant, C., Sexton, P. M., Christopoulos, A., Felder, C. C., Gmeiner, P., Steyaert, J., Weis, W. I., Garcia, K. M., Dukkipati, A., Feinberg, E. N., Angelini, A., Waghray, D., Dror, R. O., Ploegh, H.
- Advantages of Fluorescent Probes in GPCR Assays
References Barbazán J, Majellaro M, Martínez AL, Brea JM, Sotelo E, Abal M. Soave M, Briddon SJ, Hill SJ, Stoddart LA.
- Applications of Fluorescent Probes in Confocal Imaging of GPCRs: From Live to Fixed Cells
References Fessl T, Majellaro M, Bondar A. Navarro G, Sotelo E, Raïch I, Loza MI, Brea J, Majellaro M.
- Feeder or trigger – CCR2 as a scavenger and regulator of cell migration
M. Aragay et al. 1998). Removal of G proteins by using CRISPR KO of Gαi (Gαi KO) or KO of all Gα subtypes (Gα_all KO) (M. constitutively internalize through clathrin-coated pits independently of phosphorylation and β-arrestin (M. M. Paing et al. 2022; J. L. Sapmaz et al. 2019, M. N. J. Seaman 2012).
- The sixth transmembrane region of a pheromone G-protein coupled receptor, Map3, is implicated in ...
The fission yeast Schizosaccharomyces pombe has two mating types, Plus (P) and Minus (M). investigated the stringency of the two GPCRs, Mam2 and Map3, for their respective pheromones, P-factor and M-factor acid residues of Map3, F214 and F215, are key residues important for discrimination of closely related M-factors
- Transmembrane domains of GPCR dimers – a novel hot spot for drug discovery
M. et al. 2018; Manglik, A. et al. 2012). the formation of dimers and alter their function by destroying the interface between two receptors (M. structure of CB1R–5HT2AR heterodimers, preventing cognitive impairment while preserving analgesia in vivo (M.
- Optimizing HTRF Assays with Fluorescent Ligands: Time-Resolved Fluorescence in GPCR Research
Source: Navarro G, Sotelo E, Raïch I, Loza MI, Brea J, Majellaro M. References Navarro G, Sotelo E, Raïch I, Loza MI, Brea J, Majellaro M.
- Targeting GPCRs in the CNS: Advances in Drug Discovery Strategies
Biomed Pharmacother. 2018 Feb;98:222-232. doi: 10.1016/j.biopha.2017.12.056 Azam S, Haque ME, Jakaria M, ):11646-11664. doi: 10.3390/cimb46100691 Navarro G, Sotelo E, Raïch I, Loza MI, Brea J, Majellaro M.
- Decoding β-Arrestins: from Structure to function
H. 2020, Casiraghi, M. et al. 2019), double electron-electron resonance (DEER) spectroscopy for high-resolution M. et al. 2019), and hydrogen-deuterium exchange (HDX) mass spectrometry for time-dependent conformational M. et al. 1999), while dual knockout is lethal (Schmid, C. L., & Bohn, L. M. 2009).
- Hop in the Time Machine with GPCR: Unraveling the Future of Research! ⦿ Nov 24 - Dec 1, 2024
David Reiner-Link , Alessandro Berghella , Brinda K Rana , G Enrico Rovati , Valerie Capra , Caroline M Abigail Alwin , Campbell Krusemark , Ezequiel Marron Fernandez de Velasco , Steven H Olson , Lauren M












