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S., Hunyady, L., Luttrell, L. M., & Lefkowitz, R. J. (2003).

Therapy Research Structure Therapeutics Receives R&D Achievement of the Year Award for GPCR Research Bryan Roth, Natural Products, and the John Daly Legacy Sosei Heptares’ Partner, Pfizer, Progresses Its GLP

mGlu5 receptor is activated by the main excitatory neurotransmitter of the nervous central system, L-glutamate

mGlu5 receptor is activated by the main excitatory neurotransmitter of the nervous central system, L-glutamate

Moreover, due to the ratiometric nature of the assay, the FA signal depends on the concentration of both Therefore, both assays can be used for fundamental D3 receptor-ligand binding studies as well as for Sleep Medicine   2016 , 21 , 1–11. https://doi.org/10.1016/j.sleep.2016.01.017 . (5)         Tõntson, L. E.; Miller, L. J. Neuroscience Letters   2001 , 302  (1), 5–8. https://doi.org/10.1016/S0304-3940(01)01568-3 . (15)      Grätz, L.

we have demonstrated that both radioligands and FP assays using CELT-228 A3AR fluorescent antagonist Miranda-Pastoriza D, Bernárdez R, Azuaje J, Prieto-Díaz R, Majellaro M, Tamhankar AV, Koenekoop L, González

Point mutations are in the C-tail of PAR4 PH-binding domain; F347 L and D349A, but not E346A, abrogate

previously developed to bind Gαs in complex with active GPCRs, enabled detection of GLP-1R activation both Freeman BB, 3rd, Yang L, Rankovic Z. Butlen-Ducuing F, Pétavy F, Guizzaro L, Zienowicz M, Salmonson T, Haas M, et al. Manchanda Y, ElEid L, Oqua AI, Ramchunder Z, Choi J, Shchepinova MM, et al. González-Maeso J, Weisstaub NV, Zhou M, Chan P, Ivic L, Ang R, et al.

to the US to attend the ACSMEDI-EFMC Medicinal Chemistry Frontiers 2025 , a conference organized by both the EFMC and the ACSMEDI, in an effort to share the most novel medicinal chemistry advancements in both This joint effort by both associations is repeated every year, with 2026’s being in Dublin, Ireland. Brian K. Shoichet, Dr. Luc Van Hijfte and Dr. Wendy Young. The talks given targeted both traditional GPCRs such as the serotoninergic receptor 5HT1A, but also newer

cilium initiate SMOOTHENED-PKA signaling in the Hedgehog cascade Allatotropin (AT) related peptides L-ATRP

kinases – a potential pathway for GPCR-targeted drug discovery Nicola J Smith, Lauren T May, and Natasha L

Structural and Molecular Insights into GPCR Function Endogenous l- to d-amino acid residue isomerization

CCR2 is an example of a dual-function receptor that directly regulates both cell migration and scavenging Recruitment of both β-arrestin1 and β-arrestin2 was significantly diminished iin Gαi KO and Gα_all KO Moreover, HEK293 cells with CRISPR KO of both β-arrestin1 and β-arrestin2 only led to a small but measurable L.

Zhang, and L. Ma. 2008.

Binding of Stalk-derived Peptide Agonists GPCR Binders, Drugs, and more In silico exploration of 4(α-l-rhamnosyloxy

L., & Fowler, D. M. (2011).

Sakmar, Debbie L. Hay, Lukas Grätz, and more. Check out some of the latest GPCR discoveries below!

Endogenous l- to d-amino acid residue isomerization modulates selectivity between distinct neuropeptide

and dopamine D2 receptor is required for selective potentiation of dopamine D2 receptor function by L-

L., & Garcia, K. C. (2015). Structural biology.

L., Stepniewski, T.

Signalling 4 (RGS4) negatively modulates nociceptin/orphanin FQ opioid receptor signalling: Implication for l-Dopa-induced

In the skin, OR51E2 was shown to play a role in human melanocyte homeostasis (Gelis L. et. al 2016) and

was performed highlighted a new hydrophobic conserved motif composed of phenylalanine (F)/leucine (L)

Brian Arey is doing. https://www.ecosystem.drgpcr.com/dr-gpcr-virtual-cafe/ #gpcr #drgpcr #virtualcafe

article Class B1 GPCR Dimerization: Unveiling Its Role in Receptor Function and Signaling Sonja Peter , Brian

It wasn’t until his postdoctoral years at UCSF—under Brian Shoichet—that GPCRs entered his scientific This scarcity made the field both exciting and high-risk. asked whether a compound is twice as potent as another, he’s quick to point out the limitations in both

Antonella Di Pizio’s lab , there was almost nothing—no team, no culture, not even proper desks. Over the years you see the lab establishing, and for both of us, of course, growing.”  

article Class B1 GPCR Dimerization: Unveiling Its Role in Receptor Function and Signaling Sonja Peter , Brian

Brian Arey, and Dr. J. Silvio Gutkind.