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- Exscientia welcomes Richard J. Law, as their new Chief Business Officer
March 2022 "Congratulations to Richard J. Law, our newly named Chief Business Officer. Richard is the architect behind nearly all of Exscientia's partnerships and collaborations across pharma
- Dr. Nicola J. Smith - Dr. GPCR Podcast
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
- A robust and Efficient FRET-Based Assay for Cannabinoid Receptor Ligands Discovery.
.; 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. ; Richert, L.; Le, H.
- Conjugation Strategies for Probe Development
.; 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.
- The Perils and Guardrails of Modifying Signalling Proteins in Bioassays
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.
- Nanobodies: New Dimensions in GPCR Signaling Research
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.
- Decoding GPCR Function: The Role of Mutagenesis in Rational Drug Discovery
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).
- An overview of the compartmentalized GPCR Signaling: Relevance and Implications
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).
- Fluorescence Polarization in GPCR Research
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,
- Ode to GPCRs
The 2004 Nobel Prize in Physiology or Medicine went to Richard Axel and Linda Brown Buck for their work Dowling, J. E. Nobel Prize: Three Named for Medicine, Physiology Award. McGrath, J. C. & Bond, R. A. Sir James Whyte Black OM. 14 June 192422 March 2010. Press release: The 2004 Nobel Prize in Physiology or Medicine to Richard Axel and Linda B. Robert J.
- Do You Believe AI Could Accelerate Drug Discovery?
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.
- Optimizing HTRF Assays with Fluorescent Ligands: Time-Resolved Fluorescence in GPCR Research
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.
- Fluorescence based HTS compatible ligand binding assays for dopamine D3 receptors in baculovirus preparations and live cells
, J. H.; Winkelman, J. , J.; Allen, R. J. J. Med.
- Canonical chemokine receptors as scavenging “decoys”
J.; Graham, G. J., 2013). J., et al. 2010), which may ultimately compete with receptor antagonists, thereby decreasing the efficacy
- 🤯Mind-blowing GPCR Scoops! Discover the Latest Breakthroughs! ⦿ Nov 18 - 24, 2024
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
- Unlocking Cell's Secrets: Spontaneous β-Arrestin-Membrane Preassociation Drives Receptor-Activation
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
- Targeting GPCRs in the CNS: Advances in Drug Discovery Strategies
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,
- AlphaFold’s Breakthrough in GPCR Research: Revolutionizing Discovery, Yet Awaiting Experimental Proof
using the known structure of a homologous protein as a template to model the target protein ( Carlsson, J. References: Carlsson, J. et al.
- Advantages of Fluorescent Probes in GPCR Assays
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.
- Extracellular signal-regulated kinases – a potential pathway for GPCR-targeted drug discovery
J. (2019). Volmat, V., & Pouysségur, J. (2001). Spatiotemporal regulation of the p42/p44 MAPK pathway. J. (2003).
- Applications of Fluorescent Probes in Confocal Imaging of GPCRs: From Live to Fixed Cells
Br J Pharmacol. 2023 Dec 12. doi: 10.1111/bph.16297. Navarro G, Sotelo E, Raïch I, Loza MI, Brea J, Majellaro M.
- From DNA day to GPCR genomics
J., Benovic, J. L., Dohlman, H. G., Frielle, T., Bolanowski, M. A., Bennett, C. J., & Strader, C. D. (1986).
- Harnessing Deep Mutational Scanning for Enhanced Drug Discovery
M., Stephany, J. J., & Fields, S. (2014). D., English, J. G., Coyote-Maestas, W., & Aashish Manglik. (2024).
- Feeder or trigger – CCR2 as a scavenger and regulator of cell migration
J. B. Nibbs et al. 2013). Paing et al. 2022; J. L. J. Seaman 2012). J. al 2010) which may ultimately compete with receptor antagonists, thereby decreasing the efficacy (J.
- 📰 GPCR Weekly News, October 16 to 22, 2023
Robert J Lefkowitz and team's study 'GPCR signal transduction: β-arrestin activates ERK MAPK.' Dr. J. Silvio Gutkind.
- 📰 GPCR Weekly News, September 25 to October 1, 2023
Michel Bouvier, J Silvio Gutkind, and team found that Gαs is essential for GRK selectivity and gene regulation cardiometabolic diseases GPCR Events, Meetings, and Webinars October 2 - 3, 2023 | Celebrating Robert J.
- Illuminating GPCR Research: FRET and BRET-Based Sensors Shed Light on Cellular Signaling
J Biol Chem, 2018. 293(19): p. 7466-7473. 8. J Biol Chem, 2007. 282(14): p. 10576-84. 13.
- Regulators of G-protein signaling: essential players in GPCR signaling
J Biol Chem, 2009. 284(27): p. 18357-67. https://pubmed.ncbi.nlm.nih.gov/19416973/ 5. J Neurosci, 2019. 39(42): p. 8291-8304. https://pubmed.ncbi.nlm.nih.gov/31308097/ 8.
- Radioligands vs. Fluorescent Ligands: Binding Assays
Br J Pharmacol. 2020 Mar;177(5):978-991. doi: 10.1111/bph.14953.
- Overview of adhesion GPCRs self-activation
Embo j, 2012. 31(6): p. 1364-78. 2. Qian, Y., Ma, Z., Liu, C., Li, X., Zhu, X., Wang, N., Xu, Z., Xia, R., Liang, J., Duan, Y., Yin, H.,















