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- 📰 GPCR Weekly News, January 30 to February 5, 2023
(May 14 - 19, 2023) 8th and final ERNEST Meeting in Crete. (May 3 - 7, 2023). (June 11 - 16, 2023). 19th World Congress of Basic & Clinical Pharmacology 2023.
- The Perils and Guardrails of Modifying Signalling Proteins in Bioassays
Circ Res. 2024;135(1):174-197. 17. Kenakin TP. Journal of Medicinal Chemistry. 2019;62(14):6405-6421. 19. Fenton AW. J Biol Chem. 2018;293(19):7466-7473. 45. Am J Psychoanal. 1987;47(4):342-57. 57. Lowe D.
- An overview of the compartmentalized GPCR Signaling: Relevance and Implications
Proceedings of the National Academy of Sciences of the United States of America, 100(19), 10782–10787 Endocrinology, 157(4), 1613–1621. https://doi.org/10.1210/en.2015-1945 Irannejad, R., Pessino, V., Mika
- Feeder or trigger – CCR2 as a scavenger and regulator of cell migration
The chemokine receptor family comprises 19 canonical chemokine receptors together with 4 atypical chemokine Aragay et al. 1998).
- Ode to GPCRs
pathway, one of the two principal signal transduction pathways associated with GPCRs mediated signaling.[19 /1967/summary/. 12. /1970/summary/. 18. Mayo Clinic 68, 262 (1993). https://doi.org/10.1016/S0025-6196(12)60046-9/. 19. -1994/. 44.
- Decoding Schild Analysis: The Pharmacologist’s Lens on Competitive Antagonism
Analysis Schild analysis was born from an elegantly simple equation published by Sir John Gaddum in 1937 Its purpose extends far beyond its 1930s origin: It teaches equilibrium thinking—recognizing when binding
- From Failed Experiments to Predictive GPCR Models
When he moved to Uppsala in the late 1990s to study engineering, it was biotechnology—then on the rise—that
- Transformative GPCR Insights: Unleash New Horizons in Science | Sep 9 - 15, 2024
GPCR Event Spotlight Discovery on Target’s 19th Annual GPCR-Based Drug Discovery Targeting G Protein-Coupled
- Targeting GPCRs in the CNS: Advances in Drug Discovery Strategies
Curr Issues Mol Biol. 2024 Oct 19;46(10):11646-11664. Curr Issues Mol Biol. 2024 Oct 19;46(10):11646-11664. doi: 10.3390/cimb46100691 Navarro G, Sotelo E
- Fluorescence Polarization in GPCR Research
Heliyon. 2023 Dec 19;10(1):e23864. doi: 10.1016/j.heliyon.2023.e23864.
- Advantages of Fluorescent Probes in GPCR Assays
ACS Chem Biol. 2014 Sep 19;9(9):1918-28. doi: 10.1021/cb5004042.
- Differential binding of Δ9-tetrahydrocannabinol derivatives to type 1 cannabinoid receptors (CB1)
This interest has been driving efforts to understand their pharmacology since the 1980s.
- Radioligands vs. Fluorescent Ligands: Binding Assays
Methods Cell Biol. 2016;132:191-215. doi: 10.1016/bs.mcb.2015.11.004.
- 📢 Early Bird Registration Ends Tomorrow! | Sep 16 - 22, 2024
GPCR Event Spotlight Discovery on Target’s 19th Annual GPCR-Based Drug Discovery Targeting G Protein-Coupled
- Unlock the Future of GPCR Science: Breakthroughs and Courses Await | Sep 2 - Sep 8, 2024
GPCR Event Spotlight Discovery on Target’s 19th Annual GPCR-Based Drug Discovery Targeting G Protein-Coupled
- GPCR Updates: Celebrating Breakthroughs, New Course Launches Soon, and Exclusive Discounts! | Aug 26 - Sep 1, 2024
GPCR Event Spotlight Discovery on Target’s 19th Annual GPCR-Based Drug Discovery Targeting G Protein-Coupled The 19th Annual GPCR-Based Drug Discovery conference (October 2-3, 2024, in Boston and online) gathers
- Decoding GPCR Function: The Role of Mutagenesis in Rational Drug Discovery
(Bikker et al., 1998) Quantitative studies of how drugs modulate their targets have been instrumental A., Trumpp-Kallmeyer, S., & Humblet, C. (1998).
- From DNA day to GPCR genomics
the month of DNA Day, a special day commemorating the discovery of the DNA double helix structure in 1953 Another example is the cannabinoid receptor 1 with a total of 248 SNPs, where 190 missense mutations D. (1986).
- GPCRs are not simple on-off switches: deep dive into GPCR-ligand interactions
demonstration of spontaneous or "constitutive" receptor activity was reported for the β2-adrenergic receptor in 1984 (Cerione et al. 1984), where reconstitution of purified β2-adrenergic receptors from guinea pig lung constitutively activate Gi proteins in a membrane preparation without the need for an agonist (Costa and Herz 1989
- Chemokine receptor-targeted drug discovery: progress and challenges
different patterns of receptor recycling where CCR5 recycles back to the cell surface (Mack et al. 1998 restored to the cell surface and partially targeted to lysosomes (Zimmermann, Conkright, and Rothenberg 1999 only interact with the extracellular domain of the receptor ((Zimmermann, Conkright, and Rothenberg 1999
- Decoding β-Arrestins: from Structure to function
A., et al. 1997, Bohn, L. M. et al. 1999), while dual knockout is lethal (Schmid, C. L., & Bohn, L.
- 📰 GPCR Weekly News, June 26 to July 2, 2023
GPCR Events, Meetings, and Webinars NEW ERNEST ECI Zoominar (July 6, 2023) 19th World Congress of Basic
- Structural landscape of the Chemokine Receptor system
follows a common pattern which is generally described by the classic “two-site” model (Crump, Gong et al. 1997
- Unlocking Cell's Secrets: Spontaneous β-Arrestin-Membrane Preassociation Drives Receptor-Activation
Toxicol. 52, 179–197. https://doi.org/10. 1146/annurev.pharmtox.010909.105800 Tsao, P.
- Regulators of G-protein signaling: essential players in GPCR signaling
Cell, 1997. 89(2): p. 251-61. https://pubmed.ncbi.nlm.nih.gov/9108480/ 2. J Biol Chem, 2009. 284(27): p. 18357-67. https://pubmed.ncbi.nlm.nih.gov/19416973/ 5. Immunopharmacol Immunotoxicol, 2018. 40(3): p. 187-192. https://pubmed.ncbi.nlm.nih.gov/29433403/ 7.
- New role of β-arrestins in MOR signaling
regulating the response to nociception, i.e. the response of the nervous system to painful stimuli; the 1970s Proc Natl Acad Sci U S A. 1993 Jun 15;90(12):5391-3. doi: 10.1073/pnas.90.12.5391.
- Unlocking the Therapeutic Potential of Previously Undruggable GPCRs
protein GPCR ligands Paolini-Bertrand, M. et al. (2018) The Journal of Biological Chemistry, 293(49), 19092 –19100. https://doi.org/10.1074/jbc.RA118.004370 · New technology to rapidly synthesize candidate Journal of Infectious Diseases, 199, 1525-1527. https://doi.org/10.1086/598685 · Demonstration
- 📰 GPCR Weekly News - January 9 to 15, 2023
(June 11-16, 2023). 19th World Congress of Basic & Clinical Pharmacology 2023. (July 2 - 7).
- 📰 GPCR Weekly News - January 2 to 8, 2023
June 11-16, 2023. 19th World Congress of Basic & Clinical Pharmacology 2023. July 2 - 7.
- 📰 GPCR Weekly News
June 11-16, 2023. 19th World Congress of Basic & Clinical Pharmacology 2023. July 2 - 7.














