Dietzsch, Simone Prömel, et al. for their work on the Dysfunction of the adhesion GPCR latrophilin 1 am to 12 pm EDT. 22nd to 28th, 2024 Adhesion GPCRs Dysfunction of the adhesion G protein-coupled receptor latrophilin 1 - 17, 2024 | 20th Annual PEGS Boston Summit May 16 - 19, 2024 | ASPET 2024 May 27 - 29, 2024 | SLAS Adhesion GPCR Workshop July 12 - 17, 2026 | 20th World Congress of Basic and Clinical Pharmacology 2026

elevation produced by GCGR activation and promotes expression of phosphoenolpyruvate carboxykinase 1

Furthermore, GRK2-knockdown ablated the sustained phase of endothelin-1 and angiotensin-II-stimulated Conversely, the GRK2 inhibitor compound 101 did not affect vasoconstrictor-driven Akt phosphorylation Moreover, GRK2 knockdown prevented endothelin-1 and angiotensin-II from increasing cyclin D1 expression

by a G protein and constitutively activating mutations Distinct activation mechanisms of β-arrestin-1 February 11 - 14, 2023 | 2024 BPS Annual Meeting March 5 - 7, 2024 | 3rd GPCRs - Targeted Drug Discovery Molecular Gating Seminar March 24 - 29, 2024 | Ligand Recognition and Molecular Gating Conference April 1 5 - 10, 2024 | AACR Annual Meeting April 22 - 23, 2024 | Endocrine Metabolic GPCRs May 13 - 17, 2024 | 20th Annual PEGS Boston Summit May 16 - 19, 2024 | ASPET 2024 May 27 - 29, 2024 | SLAS Europe 2024

TGFβ-mediated antifibrotic GPCR landscape tampering in lung fibroblasts. βHB inhibits glucose-induced GLP-1 - 19, 2023). (June 10 - 11, 2023). (June 11 - 16, 2023). 1, 2023) 19th World Congress of Basic & Clinical Pharmacology 2023.

This week we’ve curated 18 GPCR papers, 1 new event, 9 industry news, and 3 job opportunities! NEW February 11 - 14, 2023 | 2024 BPS Annual Meeting March 5 - 7, 2024 | 3rd GPCRs - Targeted Drug Discovery Molecular Gating Seminar March 24 - 29, 2024 | Ligand Recognition and Molecular Gating Conference April 1 5 - 10, 2024 | AACR Annual Meeting April 22 - 23, 2024 | Endocrine Metabolic GPCRs May 13 - 17, 2024 | 20th Annual PEGS Boston Summit May 16 - 19, 2024 | ASPET 2024 May 27 - 29, 2024 | SLAS Europe 2024

initiating a Phase 2 study with the selective M4 agonist HTL-0016878 in schizophrenia in 2022 and Phase 1

Function Therapeutics has been awarded a Phase 1 SBIR grant from NSF. (May 14 - 19, 2023) 8th and final ERNEST Meeting in Crete. (May 3 - 7, 2023). (June 10 - 11, 2023). (June 11 - 16, 2023). 1, 2023) 19th World Congress of Basic & Clinical Pharmacology 2023.

that associate with different G protein–coupled receptors (GPCRs), including the parathyroid hormone 1

site-independent manner to compounds with therapeutic potential that have even been used safely in phase 1

February 1 | GPCR Forum ECI February 3 - 7, 2024 | SLAS2024 International Conference and Exhibition February 11 - 14, 2024 | 2024 BPS Annual Meeting NEW February 20, 2024 | Career Opportunities in Pharmacology and Drug Discovery March 13 - 15 | 9th German Pharm-Tox Summit March 23 - 24, 2024 | Ligand Recognition Molecular Gating Seminar March 24 - 29, 2024 | Ligand Recognition and Molecular Gating Conference April 1 5 - 10, 2024 | AACR Annual Meeting May 13 - 17, 2024 | 20th Annual PEGS Boston Summit May 16 - 19, 2024

September 2022 "The bioactive lysophospholipid sphingosine-1-phosphate (S1P) acts via five different

molecule) to βarr1 and focal adhesion kinase phosphorylation but not extracellular signal-regulated kinase 1/

The activation of mTOR complex 1 (mTORC1) is typically observed in human disease and continues to be

Retinitis pigmentosa (RP) is a group of hereditary degenerative diseases affecting 1 of 4000 people worldwide

Two β3 -AR agonists are used clinically: mirabegron 1 and vibegron 2, which are indicated for overactive

Kooistra & Gáspár Pándy-Szekeres ) will present and demonstrate the newest resources of the GPCRdb: 1)

Relative to control, 10μM THC and 10μM CBD reduced mRNA levels of milk proteins (CSN2 and WAP) , lipid synthesizing and glucose transport markers (GLUT 1 , HK2 , FASN , FABP4 , PLIN2 and LPL) , as well In conclusion, 10μM THC and CBD altered the differentiation of HC11 cells, in part via the CB2 receptor

the 2 best studied adrenal GPCR types in that context, adrenergic receptors and AngII receptors (AT 1

What challenges will researchers overcome in the next 10 years? AB: One of the big challenges that the field will have to face in the next 10 years is deciphering the PMID: 38311610 Member Dimitris Placantonakis’s identifies extended synaptotagmin 1 as an intracellular PMID: 38758649 Member Simone Prömel’s lab shows that the nematode (C. elegans) homolog of CELSR, FMI-1,

which includes lysergic acid diethylamide (LSD), psilocybin, mescaline and the substituted amphetamine 1- female as compared to male C57BL/6J mice, a sex-specific exacerbated behavior that was not observed in 129S6

deactivation of the alpha subunit contributing to the termination of the G protein-mediated signaling cascades[1, understanding the mechanisms of these complex molecules is crucial for developing effective therapies. 1. 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.

membrane directly and remains attached to the same receptor until they reach clathrin-coated pits (CCPs)1. clathrin-coated pits (CCPs) without solely relying on the initial and short-lived receptor-β-arrestin complexes 1. Cell, 186(10), 2238–2255.e20. https://doi.org/10.1016/j.cell.2023.04.018 Janetzko, J., Kise, R., Barsi-Rhyne Toxicol. 52, 179–197. https://doi.org/10. 1146/annurev.pharmtox.010909.105800 Tsao, P. Pharmacology & therapeutics, 89(2), 139–147. https://doi.org/10.1016/s0163-7258(00)00107-8

The mambaquaretin-1 (MQ1) peptide identified from the Dendroaspis angusticeps venom is the most selective

and physiological output in the hormone receptor-negative MDA-MB-231 and BT-20 cell lines after KP-10 We show that both cell lines express KISS1R mRNA and respond to KP-10 by elevating calcium mobilisation However, KP-10 stimulation induced migration of MDA-MB-231, but not BT-20 cells, in a calcium-dependent Moreover, only BT-20 cells responded to KP-10 by increasing ERK phosphorylation in a β-arrestin-dependent Interestingly, both cell lines displayed different complements of β-arrestin 1 and 2 expression.

selectively reduces CaV 3.2 and CaV 3.3 currents GPCR Binders, Drugs, and more LP2, a cyclic angiotensin-(1- Deadline February 12, 2023. GEM2023 (14-17 March 2023). 8th and final ERNEST Meeting May 3-7, 2023 in Crete. June 10 - 11. June 11-16, 2023. 19th World Congress of Basic & Clinical Pharmacology 2023. July 2 - 7.

Submit a logo design by Nov 1st on the Logo Contest page. -Adrenergic Receptor determined by NMR via Methyl Relaxation Structural determinants of sphingosine-1- 3rd Annual Meeting IRN I-GPCRNet November 2 - 4, 2023 | GPCR Retreat- Registration Closed November 15 - 17, 2023 | MPGPCR Conference November 20 - 23, 2023 | ASCEPT Annual Scientific Meeting February 3 , 2024 | AACR Annual Meeting May 13 - 17, 2024 | 20th Annual PEGS Boston Summit May 16 - 19, 2024 | ASPET

Cell surface expression was severely reduced to ≤18% of wild-type (WT) for 11, modestly reduced to 66% Of the 11 with severely reduced cell surface expression, restoration to ≥57% of WT levels was achieved for 6 by treatment with 1 µM CAN1404 for 24 h, and a corresponding increase in FSH-induced signaling