Next on the Dr. GPCR Podcast, we have Dr. Nicola Smith, Molecular Pharmacologist, lab head, and senior lecturer at UNSW Sydney. Subscribe to the podcast today and get notified when new episodes are released! Please share! https://www.ecosystem.drgpcr.com/dr-gpcr-podcast/ #gpcr #drgpcr #podcast

March 2022 "Congratulations to Richard J. Law, our newly named Chief Business Officer.

of receptor activity-modifying proteins in obesity and diabetes mellitus Maleesha Ubhayarathna , Christopher Langmead , Gregory Stewart , et al. for their fantastic review on Molecular and structural insights into the 5-HT2C receptor as a therapeutic target for substance use disorders Leigh Walker , Christopher Langmead , Andrew Lawrence , et al. for their remarkable analysis on Targeting muscarinic receptors

.; Tuisku, J. M.; Hirvonen, J. E. S.; Vahlberg, T.; Lahdenpohja, S.; Rinne, J. O.; Brück, A. E. J. Med. Der Wel, T.; Mandhair, H.; Honer, M.; Fingerle, J.; Scheffel, J.; Broichhagen, J.; Gawrisch, K.; Romero , J.; Hillard, C. .; Hénichart, J.-P.

.; Boström, J. J. Med. Chem.   2016 , 59  (10), 4443–4458. https://doi.org/10.1021/acs.jmedchem.5b01409 . .; Salvador Andresa, J.; Allongue, P.; Chazalviel, J.-N.; Gouget-Laemmel, A.   (3) Fan, J.; Toth, I.; Stephenson, R. J.

J.; Goulding, J.; Robers, M. B.; Machleidt, T.; Wood, K. V.; Hill, S. J.; Pfleger, K. D. G. J. Med. Chem. 2000, 43 (23), 4359–4362. https://doi.org/10.1021/jm0009843 . (4) Jacobson, K. T.; Carlsson, J. Adenosine A2A Receptor Antagonists: From Caffeine to Selective Non‐xanthines. British J Pharmacology 2022, 179 (14), 3496–3511. https://doi.org/10.1111/bph.15103 . (5) Borrmann, T J. Med. Chem. 2009, 52 (13), 3994–4006. https://doi.org/10.1021/jm900413e . (6) Klotz, K.-N.

Christopher Langmead and colleagues' work on the 5-HT2C receptor as a therapeutic target for substance

Wouters OJ, McKee M, Luyten J. J Health Econ. 2016;47:20-33. 8.            Lu S, He X, Ni D, Zhang J. Changeux J-P, Christopoulos A. J Phys Chem B. 2016;120(11):2878-85. 36.        

Che for their analysis of GPCR-G protein selectivity revealed by structural pharmacology Yao Lu, Drs Christopher Langmead,  Gregory Stewart, et al. for their study on Molecular insights into orphan G protein-coupled

excellent study on Molecular glues as potential GPCR therapeutics Sabrina Rahman , Arthur Christopoulos , Christopher Langmead , et al. for their outstanding work on Ligand-directed biased agonism at human histamine H3

Reference   Bikker, J. A., Trumpp-Kallmeyer, S., & Humblet, C. (1998). Carlsson, J., Yoo, L., Gao, Z. G., Irwin, J. J., Shoichet, B. K., & Jacobson, K. A. (2010). T., Baltos, J.-A., Thomas, T., Nguyen, T. D., Muñoz, L. L., Gregory, K. J., White, P. J., Sexton, P. M., Christopoulos, A., & May, L. T. (2016).

J., Fung, J. J., Pardon, E., Casarosa, P., Chae, P. S., Devree, B. T., Rosenbaum, D. M., Thian, F. H., Pautsch, A., Steyaert, J., Weis, W. I., & Kobilka, B. K. (2011). M., Manglik, A., Hu, J., Hu, K., Eitel, K., Hübner, H., Pardon, E., Valant, C., Sexton, P. C., Gmeiner, P., Steyaert, J., Weis, W. I., Garcia, K. C., Wess, J., & Kobilka, B. K. (2013). Nature, 504(7478), 101–106. https://doi.org/10.1038/nature12735 Burg, J. S., Ingram, J.

trial Salipro Biotech is attending the 3rd Advanced Therapy Showcase in Tokyo, Japan, organized by LINK-J Christopher Prior, as CEO and Reports Recent Drug Discovery Highlights Call for GPCR Papers GPCRs: Signal

Adapted from: Zhang Y, Tang H, Chen W, Zhang J. Int J Mol Sci. 2022 Aug 3;23(15):8625 . Miranda-Pastoriza D, Bernárdez R, Azuaje J, Prieto-Díaz R, Majellaro M, Tamhankar AV, Koenekoop L, González A, Gioé-Gallo C, Mallo-Abreu A, Brea J, Loza MI, García-Rey A, García-Mera X, Gutiérrez-de-Terán H,

British J Pharmacology 2007 , 152 (4), 429–448. https://doi.org/10.1038/sj.bjp.0707332 . (4) Barbazán , J.; Majellaro, M.; Brea, J. https://doi.org/10.1016/j.biopha.2022.113408 . (5) Raïch, I.; Rivas-Santisteban, R.; Lillo, A.; Lillo, J. 105970. https://doi.org/10.1016/j.phrs.2021.105970 . (6) Miranda-Pastoriza, D.; Bernárdez, R.; Azuaje, J. V.; Koenekoop, L.; González, A.; Gioé-Gallo, C.; Mallo-Abreu, A.; Brea, J.; Loza, M.

S., Sousa, J. B., Gonçalves, J., & Diniz, C. (2019). N., Castro, M., Wang, B., Bouley, R., Potts, J. T., Gardella, T. J., & Vilardaga, J. P. (2009). J. (2003). J., & Calebiro, D. (2016). J., & Calebiro, D. (2017).

Nichola J Smith's investigation: Gene expression of TAS1R taste receptors for cardiometabolic disease Christophe Arbet-Engels to Join as Chief Medical Officer GPCR Events, Meetings, and Webinars ONCORNET2.0

Int J Mol Sci. 2014 Feb 13;15(2):2554-72. 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. Int J Mol Sci. 2014 Feb 13;15(2):2554-72. doi: 10.3390/ijms15022554.

, J. H.; Winkelman, J. , J.; Allen, R. J. J. Med.

References: Lyu, J. et al. AlphaFold2 structures guide prospective ligand discovery. Science https://doi.org/10.1126/science.adn6354 (2024) Abramson, J., Adler, J., Dunger, J. et al.

J.; Graham, G. J., 2013). J., et al. 2010), which may ultimately compete with receptor antagonists, thereby decreasing the efficacy

antihistamines: A clinical trial is needed Jillian G Baker ,  Erica K Sloan ,   Kevin Pfleger ,  Peter J Trung Duong Nguyen ,  Ziaurrehman Tanoli ,  Saad Hassan , Umut Onur Özcan ,   Jimmy Caroli ,   Albert J physiological ligand complexes Luis P Taracena Herrera , Søren N Andreassen ,   Jimmy Caroli ,   Albert J a human bitter taste GPCR Lior Peri ,  Donna Matzov ,  Dominic R Huxley ,   Peter Gmeiner ,  Peter J

Source: Kim J, Choi C. Cells. 2020 Feb 23;9(2):506. doi: 10.3390/cells9020506   Kim J, Choi C. Oct 19;46(10):11646-11664. doi: 10.3390/cimb46100691   Navarro G, Sotelo E, Raïch I, Loza MI, Brea J,

in-depth-molecular-profiling-of-an-intronic-gnao1-mutant-as-the-basis-for-personalized-high-throughput-drug-screening References Grimes, J. M., Medel-Lacruz, B., Baidya, M., Makarova, M., Mistry, R., Goulding, J., Drube, J., Hoffmann, C., Owen K., Selent, J., Hill, S. J., & Calebiro, D. (2023). Cell, 186(10), 2238–2255.e20. https://doi.org/10.1016/j.cell.2023.04.018 Janetzko, J., Kise, R., Barsi-Rhyne

References Barbazán J, Majellaro M, Martínez AL, Brea JM, Sotelo E, Abal M. Br J Pharmacol. 2020 Mar;177(5):978-991. doi: 10.1111/bph.14953. Sridharan R, Zuber J, Connelly SM, Mathew E, Dumont ME.

using the known structure of a homologous protein as a template to model the target protein ( Carlsson, J. References: Carlsson, J.  et al.  

Br J Pharmacol. 2023 Dec 12. doi: 10.1111/bph.16297.  Navarro G, Sotelo E, Raïch I, Loza MI, Brea J, Majellaro M.

J. (2019). Volmat, V., & Pouysségur, J. (2001). Spatiotemporal regulation of the p42/p44 MAPK pathway. J. (2003).

M., Stephany, J. J., & Fields, S. (2014). D., English, J. G., Coyote-Maestas, W., & Aashish Manglik. (2024).

J., Benovic, J. L., Dohlman, H. G., Frielle, T., Bolanowski, M. A., Bennett, C. J., & Strader, C. D. (1986).