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functional specificity at C-X-C chemokine receptor 5 (CXCR5) Panjamaporn Sangwung , Alejandra Tomas , Kyle Sloop , et al. for their outstanding study on Class B1 GPCRs: insights into multireceptor pharmacology

Greetings, GPCR Colleague! Prepare to be amazed! Shocking GPCR revelations await you. Explore the newest breakthroughs and thrilling research findings in this week's update! This Week’s Highlights: Celebrating Excellence:   Patrick Sexton  and Arthur Christopoulos  Named Among Top 1% of Scientists in Pharmacology and Toxicology for 2024 ! High-affinity agonists reveal recognition motifs for the MRGPRD GPCR Chunyu Wang ,  Yongfeng Liu ,  Marion Lanier ,   Brian K Shoichet ,  Esther Martinborough ,  Jonathan F Fay ,  Can Cao ,   Bryan L Roth , et al. Pancreatic ductal adenocarcinoma, β-blockers and antihistamines: A clinical trial is needed Jillian G Baker ,  Erica K Sloan ,   Kevin Pfleger ,  Peter J McCormick , Cristina Salmerón ,   Paul A Insel PGxDB: an interactive web-platform for pharmacogenomics research Trinh Trung Duong Nguyen ,  Ziaurrehman Tanoli ,  Saad Hassan , Umut Onur Özcan ,   Jimmy Caroli ,   Albert J Kooistra ,   David E Gloriam ,   Alexander S Hauser GPCRdb in 2025: adding odorant receptors, data mapper, structure similarity search and models of physiological ligand complexes Luis P Taracena Herrera , Søren N Andreassen ,   Jimmy Caroli ,   Albert J Kooistra , Gáspár Pándy-Szekeres ,   David E Gloriam , et al. A bitter anti-inflammatory drug binds at two distinct sites of a human bitter taste GPCR Lior Peri ,  Donna Matzov ,  Dominic R Huxley ,   Peter Gmeiner ,  Peter J McCormick ,  Dorothee Weikert ,  Masha Y Niv ,  Moran Shalev-Benami , et al. Dr. GPCR Kicked Off as a Podcast... 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Phenylalanine 193 in Extracellular Loop 2 of the β 2-Adrenergic Receptor Coordinates β-Arrestin Interaction This single point mutation in extracellular loop 2 of the β2AR is sufficient to intrinsically bias the intracellular response to stimuli and suggests a previously undescribed role for the extracellular loops We characterized the effects of extracellular loop mutations on agonist-promoted interactions of GPCRs Our studies reveal that F193 in extracellular loop 2 in the β2-adrenergic receptor mediates interactions

, three anti-parallel β-strands connected by 30s- and 40s-loops, and a C-terminal α-helix. bridges, which connect the N-loop to the 30s-loop and the β3-strand, thereby anchoring the distal N-terminus β3-strand align well, although the position of the disulfide bridges between the N-loop and the 30s-loop The 30s-loop of chemokines can bind either on top of the extracellular loop 2 (ECL2) or inside the major (ICLs 1-3) and three extracellular loops (ECLs 1-3).

phosphorylation of the G protein subunit Gαi at specific residues within three strategic hotspots: the P loop Key findings include: Phosphorylation Hotspots: P Loop (Ser44, Ser47, Thr48): Impairs ligand-stimulated Signaling Pathway Segregation: Phosphorylation events in the interdomain cleft and P loop uncouple G

Significantly, we show that GRKs generate distinct phosphorylation barcodes in intracellular loop 2 ( Further molecular dynamics simulation studies reveal an interaction between the βarr2 finger loop domain

As GTP stabilizes and migrates towards the P loop, it causes the TCAT motif to shift, a key movement The AHD transitioning to a closed conformation prompts the β2–β3 loop to move away from the α5 helix,

highlighted five positions, among which four are involved in V2R interaction and belong to the two large MQ1 loops We finally determined that eight positions, part of these two loops, interact with the V2R.

The teaser question How could you design your next lead to recruit the body’s own feedback loops in your Ligands come and go, feedback loops kick in, and what you see in vitro rarely tells the whole story.

triphosphatase (GTPase)-activating protein for the Rag GTPases, through a conserved cytoplasm-facing loop

assemblies, associated with an original V2R/β-arrestin1 interface involving all receptor intracellular loops

The interface indicates a strong involvement of the connecting loop.

Collectively, these findings reveal a unique hydrogen-bonding network located on intracellular loop 2

Decoding PTH1R Gq Signaling Cryo-EM structures of Gq-bound PTH1R uncover glycan and loop-based mechanisms

Denise Wootten and colleagues has highlighted the importance of extracellular loop 2 (ECL2) in stabilizing oxyntomodulin that preferentially activate ERK1/2 signaling interact more significantly with extracellular loop

Besides, ligand-specific subtle differences in the conformations assumed by intracellular loop 2 and extracellular loop 2 are captured from the trajectories of various ligand-bound receptors in the presence

key conserved amino acids for GPR116 activation in the tethered agonist sequence and in extracellular loops

Employing GRK knockout cells and β-arrestins lacking the finger-loop-region, we show that the two isoforms

October 2022 "Pepducins are small-lipidated peptides designed from the intracellular loops of G protein-coupled

Major conformational differences were located on transmembrane (TM) 5 and 6, as well as intracellular loop

Our findings suggest a positive feedback loop in which Wnt-stimulated local PI(4,5)P2 production enhances

The larger RMSD values generated by the NN-based methods were primarily due to the differences in loop

We found that a proposed disulfide bridge between the N-terminus and extracellular loop 3, present in

catalyzes β-arrestin activation, including β-arrestin inter-domain rotation and extension of the finger loop Following dissociation from the receptor, the interaction of the extended finger loop with the lipid

It shortens feedback loops. It reveals flaws early. It stops wasted experiments.

interactions of kurarinone with the key residues of the deep orthosteric binding pocket and the extracellular loops

Not from polished plans—but from patterns of curiosity, risk-taking, and mentorship loops.

Furthermore, after phosphorylating the C-terminal tail and intracellular loop 3 (ICL3) of NF-α1/CPE-5

vivo from indole‐3‐carbinol, which is present at high levels in some vegetables including broccoli and kale

. & Kyle, R. A. Sir Bernard Katz--winner of Nobel Prize in physiology or medicine.