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We recently have shown that fluorescently labeled Hst1 (F-Hst1) targets and activates mitochondria, presenting

CRCM Must-read publications : AlphaFold3 benchmarking for GPCRs; new structural insights into peptide ligand At first glance, when a ligand binds at two different affinities in the same system, it seems logical conditions, what appears to be a second high-affinity site may simply reflect kinetic factors—such as ligand-receptor-G

Heydenreich, Michel Bouvier, Brian Kobilka, M Madan Babu, and their team's work on Molecular determinants of ligand GPCRs) Associated with Lambda-Cyhalothrin Detoxification in Cydia pomonella Molecular determinants of ligand autophagy-mediated NLRP3 degradation Methods & Updates in GPCR Research Direct Binding Methods to Measure Receptor-Ligand Annual Meeting March 5 - 7, 2024 | 3rd GPCRs - Targeted Drug Discovery Summit March 23 - 24, 2024 | Ligand Recognition and Molecular Gating Seminar March 24 - 29, 2024 | Ligand Recognition and Molecular Gating

Ligands must first partition into the surrounding membrane and take lipid paths to these sites. Remarkably, a significant part of the bound ligands appears exposed to the membrane lipids. experimental structures do not usually account for the surrounding lipids, and their apparent contribution to ligand

metadynamics-enhanced conformational sampling are used here to determine the different interactions of these two ligands The endogenous peptide ligand endomorphin-1 (EM-1) underwent almost no significant conformational changes This finding reveals a dynamic mechanism for the response of MOR to different ligands and provides a basis for the discovery of new ligands for MOR at the atomic level."

by a chemerin-derived agonist Functional profiling of the G protein-coupled receptor C3aR1 reveals ligand-mediated biased agonism GPCR Binders, Drugs, and more Design and structural validation of peptide-drug conjugate ligands Annual Meeting March 5 - 7, 2024 | 3rd GPCRs - Targeted Drug Discovery Summit March 23 - 24, 2024 | Ligand Recognition and Molecular Gating Seminar March 24 - 29, 2024 | Ligand Recognition and Molecular Gating

High-throughput screening for receptor ligands was booming, and Sokhom was at the center of it.

Brendan Creemer, Thomas Gardella, and Ross Cheloha for their work on Highly biased agonism for GPCR ligands GPCR Activation and Signaling Highly biased agonism for GPCR ligands via nanobody tethering Mechanistic deficits GPCRs in Cardiology, Endocrinology, and Taste The full-length TSH receptor is stabilized by TSH ligand orientation using a neurotensin receptor 1 peptide Illuminating the neuropeptide Y4 receptor and its ligand

Fast-forward a few thousand years, and we’re talking beta receptors, receptor theory, and AI-generated ligands

 (e.g., 14-3-3) Heterodimerization Endogenous vs. overexpressed systems Orphan GPCR deorphanization Ligand

sees a future where this system is not just used for detection, but for functional screening : add ligands

the immune system ORs are expressed in different blood cells where aroma compounds from butter, known ligands In the GI tract OR ligands drive an intracellular cascade that results in enhanced serotonin release antagonists, where the starting point can be using licensed drugs (for drug repurposing) and endogenous ligands Odorants, the natural ligands, could potentially be used as ligands and particular forms of odorant delivery ORs research to advance drug discovery include the deorphanization and characterization of relevant ligands

Neurotensin Receptor Allosterism Revealed in Complex with a Biased Allosteric Modulator. α1-adrenoceptor ligands A small molecule ligand for the novel pain target, GPR171, produces minimal reward in mice. Monitoring the Reversibility of GPCR Signaling by Combining Photochromic Ligands with Label-free Impedance , Endocrinology, and Taste Structure-based design of novel melanin-concentrating hormone receptor-1 ligands New paradigms in purinergic receptor ligand discovery.

therapy Rational design of highly stabilized and selective adrenomedullin analogs Novel multi-target ligands scaffolds-synthesis, biological activity, and structural evaluation Flavonoids as G Protein-coupled Receptors Ligands Annual Meeting March 5 - 7, 2024 | 3rd GPCRs - Targeted Drug Discovery Summit March 23 - 24, 2024 | Ligand Recognition and Molecular Gating Seminar March 24 - 29, 2024 | Ligand Recognition and Molecular Gating

Activation: GAIN Domain Unfolding and Dissociation in Adhesion GPCRs Molecular sensing of mechano- and ligand-dependent receptor GPR81 drives breast cancer growth and invasiveness through regulation of ECM properties and Notch ligand Annual Meeting March 5 - 7, 2024 | 3rd GPCRs - Targeted Drug Discovery Summit March 23 - 24, 2024 | Ligand Recognition and Molecular Gating Seminar March 24 - 29, 2024 | Ligand Recognition and Molecular Gating

Drugs, and more Nanobody-Mediated Dualsteric Engagement of the Angiotensin Receptor Broadens Biased Ligand impacts on metabolism of polyamines, mRNA splicing, regulation of RAS by GAPs, neddylation and GPCR ligand in Pharmacology and Drug Discovery March 13 - 15 | 9th German Pharm-Tox Summit March 23 - 24, 2024 | Ligand Recognition and Molecular Gating Seminar March 24 - 29, 2024 | Ligand Recognition and Molecular Gating

Impact of membrane lipid polyunsaturation on dopamine D2 receptor ligand binding and signaling GPCR Binders Application of computational methods for class A GPCR Ligand discovery. Methods & Updates in GPCR Research GPCRLigNet: rapid screening for GPCR active ligands using machine Insights into GPCR Function Structure-based design of novel melanin-concentrating hormone receptor-1 ligands Studentship - Integrated Approaches In Pharmacology, Computer Simulations And Machine Learning To Predict Ligand

isoforms, a case for functionally Gs protein-selective GPCRs, and new methods for detecting simultaneous ligand Learn how his research aims to develop models that can distinguish between active and inactive ligands , paving the way for computational ligand discovery even where experimental data is scarce.

Just her, radioactive ligands, and steady hands. could make or break the result, The pace and precision of GPCR research today — from high-throughput ligand

is the removal of the inhibitory GAIN domain and the dipping of the cleaved stalk peptide into the ligand-binding The structures reveal unique ligand-engaging mode, distinctive activation conformation, and key mechanisms

employed optical assays in living cells to thoroughly profile both GPR35 isoforms for constitutive and ligand-induced activation and signaling of 10 different heterotrimeric G proteins, ligand-induced arrestin recruitment and mechanistic insights of our study provide clues for the future design of isoform-specific GPR35 ligands

2022 "As the only member of the CX3C chemokine receptor subfamily, CX3CR1 binds to its sole endogenous ligand Here, we present two cryo-electron microscopy structures of CX3CR1-Gi1 complexes in ligand-free and CX3CL1

through Transcriptomics and Single-Cell Technologies Methods & Updates in GPCR Research ThermoBRET: A Ligand-Engagement Meeting February 3 - 7, 2024 | SLAS2024 International Conference and Exhibition March 23 - 24, 2024 | Ligand Recognition and Molecular Gating Seminar March 24 - 29, 2024 | Ligand Recognition and Molecular Gating

Synaptamide suppressed osteoclastogenesis induced by receptor activator of nuclear factor-kappa B ligand Our study suggested that ligands of GPR110, such as synaptamide, might be a useful drug for osteoporotic

These structures reveal an agonist binding site for the oxysterol and a potential ligand entrance site Together, these findings provide new insight into how EBI2 is activated by an oxysterol ligand and will

Ross Cheloha's research involves semi-synthetic nanobody-ligand conjugates with enhanced transcriptional complex unravels the biased signaling mechanism GPCR Binders, Drugs, and more Semi-synthetic nanobody-ligand Annual Meeting March 5 - 7, 2024 | 3rd GPCRs - Targeted Drug Discovery Summit March 23 - 24, 2024 | Ligand Recognition and Molecular Gating Seminar March 24 - 29, 2024 | Ligand Recognition and Molecular Gating

dual contrasting functional feature of CBD, that is, displaying antagonistic and (possible) agonistic ligand From microsecond-length unbiased molecular dynamics simulations, we found that the presence of the CBD ligand These results are in agreement with the proposed modulatory function of each ligand, showing that the In contrast to the CBD/CB1 complex, when the CB1 receptor is simulated in complex with the ligand antagonist

During Drosophila embryonic salivary gland (SG) invagination, the GPCR ligand Folded gastrulation (Fog Our data support a model wherein Smog regulates distinct myosin pools and actin cytoskeleton in a ligand-dependent

Dual control: not just brightness but fluorescence lifetime, with drastic shifts as pH drops.

During Drosophila embryonic salivary gland (SG) invagination, the GPCR ligand Folded gastrulation (Fog Our data support a model wherein Smog regulates distinct myosin pools and actin cytoskeleton in a ligand-dependent