Continuing Study Addex Therapeutics in the 23rd BioEquity Europe Conference Simon Bekker-Jensen and Mette M Rosenkilde received two proof of concept grants from European Research Council (ERC) Addex Reports Placebo in Participants Diagnosed with WHIM Syndrome GPCR Events, Meetings, and Webinars ASPET 2023 - (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.

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

August 2022 "GPCRs in Medicinal Chemistry Event 8th RSC / SCI symposium on GPCRs in Medicinal Chemistry Dates Wednesday-Friday, 5th-7th October 2022 Place Evotec Campus Levi-Montalcini, Verona, Italy Downloads and Links Registration closing dates: 6th September – registration against invoice (bank transfers): Tuesday, 6th September 30th September – online registration (card payments)" Read more at the source #DrGPCR #GPCR #IndustryNews

Hybrid meeting.

August 2022 "Join Us in Boston for Discovery On Target 2022! Discovery on Target (DOT) highlights advances in current and emerging “hot” targets and technologies, as well as target validation strategies for the discovery and development of novel therapeutic agents ranging from biologics to small molecules." Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 "WELCOME 4GPCRnet meeting bringing together four of the biggest GPCR networks in Europe for a joint meeting in Leipzig. Rise and ERNEST plus DFG-funded SFB1423 and FOR2372) have joined forces to organize an international meeting

August 2022 "We are happy to announce you our 2nd IRN i-GPCRnet meeting that will be held at the University

December 2021 "Meet Peter McNamara , Ph.D., Tectonic ’s SVP, Head of Research.

M., & Fields, S. (2014). Deep mutational scanning: a new style of protein science. 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).

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.

., Vieira-Rocha, M. S., Vojtek, M., Sousa, J. B., & Diniz, C. (2021). E., Healy, M. D., & Collins, B. M. (2019). M., & Lefkowitz, R. J. (2003). B., Conti, M., & von Zastrow, M. (2017). M., & Murray, F. (2018).

., Bolanowski, M. A., Bennett, C. D., Rands, E., Diehl, R. E., Mumford, R. A., Slater, E. 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. ., Casiraghi, M., He, F., Maul, L., Gmeiner, P., Kobilka, B. K., Hildebrand, P.

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).

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.

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).

., 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

Franziska M Heydenreich, Michel Bouvier, Brian Kobilka, M Madan Babu, and their team's work on Molecular GPCR Ecosystem Premium memberships 30-minute one-on-one meeting with Dr. License Agreement and Strategic Collaboration with Novartis to Advance Novel Gene Therapies GPCR Events, Meetings 7, 2024 | SLAS2024 International Conference and Exhibition February 11 - 14, 2024 | 2024 BPS Annual Meeting Discovery Chemistry April 4 - 7, 2024 | American Physiology Summit April 5 - 10, 2024 | AACR Annual Meeting

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).

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.

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).

Kathleen M Caron and her team studied the GPER/GPR30 complex with β1-adrenergic receptor and AKAP5 in $299 and includes: All 4 live Zoom sessions ( 4x 1 hour lecture + 30 mins Q&A) 30-minute one-on-one meeting Concludes in Largest-Ever Phase 2b Clinical Trial for Cannabis Addiction Treatment AEF0117 GPCR Events, Meetings 7, 2024 | SLAS2024 International Conference and Exhibition February 11 - 14, 2024 | 2024 BPS Annual Meeting Discovery Chemistry April 4 - 7, 2024 | American Physiology Summit April 5 - 10, 2024 | AACR Annual Meeting

Devki D Sukhtankar and Pina M Cardarelli's research: Burixafor Hydrobromide (GPC-100) effects on hematopoietic Christophe Arbet-Engels to Join as Chief Medical Officer GPCR Events, Meetings, and Webinars ONCORNET2.0 Targets: Allosteric Function and Biased Signaling" at the DOT (September 27 - 28, 2023) 3rd Annual Meeting GPCR Retreat (November 2 - 4, 2023) MPGPCR Conference (November 15 -17, 2023) ASCEPT Annual Scientific Meeting

This week's highlight includes congrats to: Makaía M Papasergi-Scott, Peter Gmeiner, Brian K Kobilka, development in Drosophila Karuna Therapeutics announces that is now part of Bristol Myers Squibb GPCR Events, Meetings Discovery Chemistry April 4 - 7, 2024 | American Physiology Summit April 5 - 10, 2024 | AACR Annual Meeting

Magdalena M Scharf, Antonella Di Pizio, Ines Liebscher, Hannes Schihada, and Gunnar Schulte et al. on Industry Veterans Bernard Coulie, M.D., Ph.D., and Shalini Sharp to its Board of Directors GPCR Events, Meetings Discovery Chemistry April 4 - 7, 2024 | American Physiology Summit April 5 - 10, 2024 | AACR Annual Meeting

M, et al. 2023).

SMOOTHENED-PKA signaling in the Hedgehog cascade Elita Yuliantie , Arthur Christopoulos , Patrick M. Under Nasdaq Listing Rule 5635(c)(4) Unlocking New Possibilities in GLP-1R Drug Discovery GPCR Events, Meetings

Nayara Braga Emidio, Ross Cheloha, Laura M Wingler, et al. for their work on Nanobody-Mediated Dualsteric Cracking Cellular Communication Code Aelis Farma will be at Bio Europe Spring in Barcelona GPCR Events, Meetings Discovery Chemistry April 4 - 7, 2024 | American Physiology Summit April 5 - 10, 2024 | AACR Annual Meeting