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.

J., Fung, J. J., Pardon, E., Casarosa, P., Chae, P. S., Devree, B. T., Rosenbaum, D. M., Thian, F. 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. (New York, N.Y.), 347(6226), 1113–1117. https://doi.org/10.1126/science.aaa5026 Wu, A., Salom, D., Hong , J.

October 2022 "Systolic heart failure (HF) is a chronic clinical syndrome characterized by the reduction in cardiac function and still remains the disease with the highest mortality worldwide. Despite considerable advances in pharmacological treatment, HF represents a severe clinical and social burden. Chronic human HF is characterized by several important neurohormonal perturbations, emanating from both the autonomic nervous system and the adrenal glands. Circulating catecholamines (norepinephrine and epinephrine) and aldosterone elevations are among the salient alterations that confer significant hormonal burden on the already compromised function of the failing heart. This is why sympatholytic treatments (such as β-blockers) and renin-angiotensin system inhibitors or mineralocorticoid receptor antagonists, which block the effects of angiotensin II (AngII) and aldosterone on the failing heart, are part of the mainstay HF pharmacotherapy presently. The adrenal gland plays an important role in the modulation of cardiac neurohormonal stress because it is the source of almost all aldosterone, of all epinephrine, and of a significant amount of norepinephrine reaching the failing myocardium from the blood circulation. Synthesis and release of these hormones in the adrenals is tightly regulated by adrenal G protein-coupled receptors (GPCRs), such as adrenergic receptors and AngII receptors. In this review, we discuss important aspects of adrenal GPCR signaling and regulation, as they pertain to modulation of cardiac function in the context of chronic HF, by focusing on the 2 best studied adrenal GPCR types in that context, adrenergic receptors and AngII receptors (AT 1 Rs). Particular emphasis is given to findings from the past decade and a half that highlight the emerging roles of the GPCR-kinases and the β-arrestins in the adrenals, 2 protein families that regulate the signaling and functioning of GPCRs in all tissues, including the myocardium and the adrenal gland." Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 Regulator of G Protein Signaling 20 Correlates with Long Intergenic Non-Coding RNA (lincRNAs ; (d) RGS20 was found to be significantly associated with some tumor-related signaling pathways and long

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). Nature communications, 8(1), 443. https://doi.org/10.1038/s41467-017-00357-2 Jong, Y.

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).

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

Sir William Osler Scientists have long sought to discover a “golden bullet” that would cure every disease signal-regulated kinases (ERK), a subset of the mitogen-activated protein kinase (MAPK) family, have long J. (2019). Volmat, V., & Pouysségur, J. (2001). Spatiotemporal regulation of the p42/p44 MAPK pathway. J. (2003).

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

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

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.

emerges with $100M to spark 'second golden age' of prolific drug target GPCR with pioneer as co-founder "J

Robert J Lefkowitz and team's study 'GPCR signal transduction: β-arrestin activates ERK MAPK.' Dr. J. Silvio Gutkind.

What mariachi song are you most likely to shout along to at 3 AM? Mariachi song: I typically do not sing to these since they are dear to Mexican childhood memories, and Don’t be surprised if you find yourself singing Daddy Yankee’s “Gasolina” from the top of your lungs PMID: 38378098 Curated by Sumit J. Bandekar with help from Nathan Zaidman and Abhishek K. Singh

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.

recognized for inhibiting G protein signaling, they also influence specific pathways such as MAPK signaling (Song protein and has evolved to achieve resolutions comparable to X-ray crystallography (García-Nafría, J. H., & Lee, J. , as well as MAPK cascade kinases which can be activated through specific β-arrestin conformations (Song

J Biol Chem, 2018. 293(19): p. 7466-7473. 8.      J Biol Chem, 2007. 282(14): p. 10576-84. 13.   

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.

Structurally they characterize by a long extracellular region of adhesion-like domains which modulate 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.,

., J. García-Nafría, and C.G. Graaf, C., et al., Glucagon-Like Peptide-1 and Its Class B G Protein-Coupled Receptors: A Long March

involved in "short-term memory", whereas cAMP signaling and new protein synthesis are required for "long-term 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. Br J Pharmacol 177, 469–489 (2020). https://bpspubs.onlinelibrary.wiley.com/doi/10.1111/bph.14524/. Robert J.

Robert J Lefkowitz. Join us tomorrow, July 21, in the Dr.

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

trial Salipro Biotech is attending the 3rd Advanced Therapy Showcase in Tokyo, Japan, organized by LINK-J

Extracellular signal-regulated kinases – a potential pathway for GPCR-targeted drug discovery Nicola J

Deadline September 27, 2023 GPCR Events, Meetings, and Webinars October 2 - 3, 2023 | Celebrating Robert J.