The structures reveal unique ligand-engaging mode, distinctive activation conformation, and key mechanisms The structures also reveal the uncharted structural information of GPCR/G12 coupling.

Receptor conformational sampling in advance of docking or receptor conformational adjustment after docking

August 2022 "G-protein-coupled receptors (GPCR) are present at the cell surface in different conformational

enhance GPCR subtype-selectivity, it also presents a significant challenge when it comes to detecting and confirming the following pharmacological characteristics: 1) affinity modulation where the resulting change in conformation Additionally, considering conformational kinetics for coupling preference with downstream signaling components

Structural analysis revealed that the introduced thiophene modification restricted receptor conformational

It provided a fundamental understanding of how genetic information is stored and transferred between like X-ray crystallography and cryo-electron microscopy, have allowed us to understand the structural dynamics Additionally, there have been recent discoveries of the conformational changes that occur during G-protein

GPCR, was featured as Superluminal Medicines Launches to Drug Protein Conformations in a Flash. make digital therapeutics for substance use disorders Superluminal Medicines Launches to Drug Protein Conformations and G-CLIPS join forces to revolutionize transmembrane proteins characterization in drug discovery Confo 3rd Annual Meeting IRN I-GPCRNet November 2 - 4, 2023 | GPCR Retreat November 15 - 17, 2023 | MPGPCR Conference 20th Annual PEGS Boston Summit May 16 - 19, 2024 | ASPET 2024 May 27 - 29, 2024 | SLAS Europe 2024 Conference

WNT stimulation induces dynamic conformational changes in the Frizzled-Dishevelled interaction. SLAS Europe 2023 Conference and Exhibition. (May 22 - 26, 2023) 2nd LEAPS Meets Life Sciences Conference. The Illuminating the Understudied Druggable Proteome Conference.

The structures reveal distinctive ligand engaging model and activation conformations of GPR110. Taken together, our study fills the missing information of GPCR/G-protein engagement and provides a framework

acid release), assays to monitor β-arrestin recruitment or signaling, and assays to monitor receptor conformational

molecules biasedly modulating the TLR4 signaling axis not only provide probes to fine-tune receptor conformation

Dynamic spatiotemporal determinants modulate GPCR:G protein coupling selectivity and promiscuity. Computational study of the conformational ensemble of CX3C chemokine receptor 1 (CX3CR1) and its interactions Lysine 101 in the CRAC Motif in Transmembrane Helix 2 Confers Cholesterol-Induced Thermal Stability to The Illuminating the Understudied Druggable Proteome Conference.

between PTHrP1-36 and properties of native PTHrP1-141 are caused by the stabilization of a singular PTHR conformation

Despite decades of research on the signaling consequences of molecule-receptor interactions, conformational

chemokine and the extracellular loops and transmembrane domains of the receptor (CRS2), which will trigger conformational Further research will be needed to boost our understanding on the dynamics and biological relevance of

Confirmed speakers include Drs. GPCR Volunteers Join our dynamic team as a volunteer! You'll share your contributor articles with the community, stay updated with GPCR literature, join a dynamic the brain-genetically encoded single wavelength fluorescent biosensors to unravel neurotransmitter dynamics 20th Annual PEGS Boston Summit May 16 - 19, 2024 | ASPET 2024 May 27 - 29, 2024 | SLAS Europe 2024 Conference

Co-immunoprecipitation and pull-down assays confirmed interaction between NFα1/CPE and 5-HTR1E and 125I Molecular dynamics studies revealed that NF-α1/CPE interacts with 5-HTR1E via 3 salt bridges, stabilized

Structural and Molecular Insights into GPCR Function Thermodynamic architecture and conformational plasticity SLAS2023 International Conference and Exhibition (February 25 - March 1). (April 20-21, 2023) SLAS Europe 2023 Conference and Exhibition. The Illuminating the Understudied Druggable Proteome Conference.

including amino acid sequences or structural data (from X-ray crystallography, cryoEM or molecular dynamics properties of GPCRs, such as ligand binding sites (orthosteric, allosteric), activation mechanisms, and conformational Birolo, Montanucci, Turina, Capriotti & Fariselli, 2020) with intrinsic limitations (e.g. using sequence information facilitate the development of personalized treatments by analyzing patient data, including genomic information

Confirmed speakers include Drs.  GPCR Volunteers Join our dynamic team as a volunteer! You'll share your contributor articles with the community, stay updated with GPCR literature, join a dynamic Recognition and Molecular Gating Seminar March 24 - 29, 2024 | Ligand Recognition and Molecular Gating Conference 20th Annual PEGS Boston Summit May 16 - 19, 2024 | ASPET 2024 May 27 - 29, 2024 | SLAS Europe 2024 Conference

fluorescence fluctuation spectroscopy Structural and Molecular Insights into GPCR Function Monitoring GPCR conformation

Confirmed speakers include Drs. GPCR Volunteers Join our dynamic team as a volunteer! phosphodiesterases in aortic aneurysm and dissection GPCRs in Oncology and Immunology Molecular docking and dynamics February 1 | GPCR Forum ECI February 3 - 7, 2024 | SLAS2024 International Conference and Exhibition February 20th Annual PEGS Boston Summit May 16 - 19, 2024 | ASPET 2024 May 27 - 29, 2024 | SLAS Europe 2024 Conference

We work tirelessly to bring you informative and exciting news about the world of GPCR every Thursday. Intermediate-state-trapped mutants pinpoint G protein-coupled receptor conformational allostery. (April 20 - 21, 2023) SLAS Europe 2023 Conference and Exhibition. (May 22 - 26, 2023) 2nd LEAPS Meets Life Sciences Conference. The Illuminating the Understudied Druggable Proteome Conference.

Conformational specificity of opioid receptors is determined by subcellular location irrespective of

Stay tuned for more information coming soon. Interested in showcasing your research? between renin-angiotensin system receptors Arrestin-centred interactions at the membrane and their conformational Recognition and Molecular Gating Seminar March 24 - 29, 2024 | Ligand Recognition and Molecular Gating Conference 20th Annual PEGS Boston Summit May 16 - 19, 2024 | ASPET 2024 May 27 - 29, 2024 | SLAS Europe 2024 Conference

to peptide and non-peptide ligands have been elucidated, providing new opportunities to examine the dynamic This review covers the new data elucidating the structural dynamics of AngII receptors and how structural

Activation and Signaling PACAP key interactions with PAC1, VPAC1, and VPAC2 identified by molecular dynamics cells Profiling the proximal proteome of the activated μ-opioid receptor Computational modelling of dynamic for patent granted for somatostatin modulators for treating hormone-related conditions Sosei Heptares Confirms Clinical Study Evaluating Effects of NBI-1065890, a Second-Generation VMAT2 Inhibitor, in Healthy Adults Confo 20th Annual PEGS Boston Summit May 16 - 19, 2024 | ASPET 2024 May 27 - 29, 2024 | SLAS Europe 2024 Conference

Interactions in G Protein-Coupled Receptor Allosteric Sites at the Membrane Interface from Molecular Dynamics allosteric sites of the PAR2, C5aR1, and GCGR receptors in three lipid compositions using molecular dynamics