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Elizabeth Johnstone were awarded one of the 2022 Diabetes Research Grants at the World Diabetes Day Breakfast "Congratulations to Perkins Professor Kevin Pfleger and Dr Elizabeth Johnstone who were awarded one of

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

Genome-wide identification of 216 G protein-coupled receptor (GPCR) genes from the marine water flea Here, we identified a total 216 full-length GPCR genes in the marine water flea Diaphanosoma celebensis In this study, these results may provide a better understanding on the evolution of GPCRs, and expand

Targeted mutagenesis may miss broader functional regions, while random mutagenesis generates extensive M., Marti-Solano, M., Sandhu, M., Kobilka, B. K., Bouvier, M., & Babu, M. M. (2023). 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).

For example, the lipid composition of intracellular membranes may influence GPCR dynamics and signaling ., Vieira-Rocha, M. S., Vojtek, M., Sousa, J. B., & Diniz, C. (2021). E., Healy, M. D., & Collins, B. M. (2019). B., Conti, M., & von Zastrow, M. (2017). M., & Murray, F. (2018).

This suggests that conserved residues across species may be ideal drug targets, ensuring consistent efficacy 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.

Also, ongoing research may discover new GPCRs or refine existing data, which could lead to adjustments provide a large database of genetic variations (including single nucleotide polymorphisms or SNPs) that may S., Caron, M. G., Lefkowitz, R. J., & Strader, C. D. (1986). M., Pérez-Hernández, G., Batebi, H., Gao, Y., Eskici, G., Seven, A. ., Casiraghi, M., He, F., Maul, L., Gmeiner, P., Kobilka, B. K., Hildebrand, P.

physical barrier this lipid bilayer creates is dynamic and interactive, becoming the foundation for many 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). M., Kawakami, K., Masureel, M., Maeda, S., Garcia, K. C., von Zastrow, M., Inoue, A., & Kobilka, B. I., & von Zastrow, M. (2001).

combines high-throughput DNA sequencing with systematic mutagenesis to create and assess the impact of many 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).

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.

., 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.

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

M. Aragay et al. 1998). M. Paing et al. 2022; J. L. Sapmaz et al. 2019, M. N. J. Seaman 2012). Namkung et al. 2016), and avoid depletion may also contribute to its ability to efficiently scavenge Scavenging may allow cells to continuously migrate by remaining responsive to chemokines (S.

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.

The hypothesis arises that GPCR and β-arrestin-centered effector complexes vary based on subcellular 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). In certain cancer types, only one β-arrestin isoform's expression may be altered, while the other remains

Franziska M Heydenreich, Michel Bouvier, Brian Kobilka, M Madan Babu, and their team's work on Molecular Physiology Summit April 5 - 10, 2024 | AACR Annual Meeting April 22 - 23, 2024 | Endocrine Metabolic GPCRs May 13 - 17, 2024 | 20th Annual PEGS Boston Summit May 16 - 19, 2024 | ASPET 2024 May 27 - 29, 2024 | SLAS

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 GPCR Events Mark your glittery calendar with dates in 2025 ! April 24 - 27, 2025 | American Physiology Summit 2025 April 25 - 30, 2025 | AACR Annual Meeting 2025 May 12 - 15, 2025 | PEGS 2025 May 20 - 22, 2025 | SLAS Europe 2025 June 16 - 19, 2025 | BIO International

M, et al. 2023). migrate by remaining responsive to chemokines, it dampens the inflammatory response when needed; and it may J., et al. 2010), which may ultimately compete with receptor antagonists, thereby decreasing the efficacy into the contribution of scavenging to homeostatic maintenance and the pathological consequences that may

., Ghassemian, M., Kufareva, I., & Ghosh, P. (2024).

Devki D Sukhtankar and Pina M Cardarelli's research: Burixafor Hydrobromide (GPC-100) effects on hematopoietic cells in mice and humans Mark your calendar! with single molecule sensitivity and high selectivity Reviews, GPCRs, and more GPR84 in physiology - many functions in many tissues Bispecific Monoclonal Antibodies in Multiple Myeloma: Data from ASH 2022:

include chronic cough, in addition to the rights to develop certain retained compounds for Charcot-Marie-Tooth

where different ligands acting on the same receptor trigger distinct signaling pathways, leading to varied Cary, B.P., et al., New Insights into the Structure and Function of Class B1 GPCRs.   Anson, M., et al., Incidence of new onset type 2 diabetes in adults living with obesity treated with

Recent studies suggest that class B1 GPCRs can form both homodimers and heterodimers, which may play These dimeric interactions may contribute to the phenomenon of biased agonism, where ligands produce dimerization is critical for regulating GPCR function, particularly with respect to biased agonism, which may Bouvier, M., Oligomerization of G-protein-coupled transmitter receptors.  

SMOOTHENED-PKA signaling in the Hedgehog cascade Elita Yuliantie , Arthur Christopoulos , Patrick M.

This emphasis may have caused other signaling pathways to be overlooked due to a need for adequate assay M., & Lefkowitz, R. J. (2003).

Remember to join us tomorrow, May 19th, for the highly anticipated Dr. Below is your Classified GPCR News at a glance for May 8th to 14th, 2023. Continuing Study Addex Therapeutics in the 23rd BioEquity Europe Conference Simon Bekker-Jensen and Mette M (May 22 - 26, 2023) 2nd LEAPS Meets Life Sciences Conference. (May 14 - 19, 2023) PEGS Boston (May 15 - 19, 2023) 8th and final ERNEST Meeting in Crete.

This week's highlight includes congrats to: Makaía M Papasergi-Scott, Peter Gmeiner, Brian K Kobilka, GPCR University Save the date for our upcoming workshop, starting May 9th, 2024, featuring Dr.  Discovery Chemistry April 4 - 7, 2024 | American Physiology Summit April 5 - 10, 2024 | AACR Annual Meeting May 13 - 17, 2024 | 20th Annual PEGS Boston Summit May 16 - 19, 2024 | ASPET 2024 May 27 - 29, 2024 | SLAS

Some studies have suggested that VAMP2 may be involved in regulating dopamine D2 receptor signaling by K ´ onigstorfer, M. Mozhayeva, Y. Sara, T.C. Südhof, and ¨ E.T. Kavalali. 2001.