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204 items found for "cryo-EM structure"
- 📰 GPCR Weekly News, May 6 to 12, 2024
We have postponed our symposium on Structural Insights into GPCR Activation to a later date. Generation of comprehensive GPCR-transducer-deficient cell lines to dissect complexity of GPCR signaling Structural and Molecular Insights into GPCR Function Membrane mimetic-dependence of GPCR energy landscapes Structural
- 📰 GPCR Weekly News - January 2 to 8, 2023
Structural and Molecular Insights into GPCR Function Structural and functional analyses of a GPCR-inhibited
- High hedgehog signaling is transduced by a multikinase-dependent switch controlling the...
transducer of the hedgehog (HH) morphogen, which plays an essential role in the patterning of epithelial structures
- Therapeutic validation of an orphan G protein-coupled receptor: The case of GPR84
consider the physiological and pathological expression profile of GPR84 and, in the absence of direct structural
- Molecular insights into regulation of constitutive activity by RNA editing 5HT2C serotonin receptor
responsible for these effects of RNA editing, we present four active-state 5HT2C-transducer-coupled structures
- Isoform-and ligand-specific modulation of adhesion GPCR ADGRL3/Latrophilin3 by a synthetic binder
The LK30/ADGRL3 complex structure revealed that the LK30 binding site on ADGRL3 overlaps with the binding
- Discovery and In Vivo Evaluation of ACT-660602: A Potent and Selective Antagonist of the Chemokine..
The careful structural modifications during the lead optimization phase led to a compound with high biological
- Allosteric Effect of Nanobody Binding on Ligand-Specific Active States of the β2 Adrenergic Receptor
Dimensionality reduction analysis shows that Nb80 stabilizes structural features of the β2AR with an intracellular binding partners on the GPCR activation mechanism, which should be taken into account in structure-based
- GPCR kinases generate an APH1A phosphorylation barcode to regulate amyloid-β generation
Collectively, these studies provide insight into the molecular and structural determinants of the APH1A-βarr2
- 📰 GPCR Weekly News, May 20 to 26, 2024
adipocyte differentiation through ERK activation GPCR Binders, Drugs, and more Flipping the GPCR Switch: Structure-Based Under' Apelin receptor dimer: Classification, future prospects, and pathophysiological perspectives Structural
- Nanobodies as Probes and Modulators of Cardiovascular G Protein-Coupled Receptors
Here, we review how nanobodies have been adopted to elucidate the structure, pharmacology, and signaling
- 📰 GPCR Weekly News, May 1 to 7, 2023
Structural and Molecular Insights into GPCR Function Structural insight into an anti-BRIL Fab as a G-protein-coupled
- Finding needles in haystacks: Omass unveils pipeline aimed at tough-to-drug targets
2021 "Nov. 15, 2021 LONDON – There’s not yet proof of the pudding, but Omass Therapeutics Ltd.’s new structure-based
- Fluorescent Ligands Targeting Intracellular Allosteric Binding Site of the Chemokine Receptor CCR2
Here, we report the structure-based development of fluorescent ligands targeting the intracellular allosteric
- Opioid Receptors and Protonation-Coupled Binding of Opioid Drugs
In this review, we discuss the relationship between structure, function, and dynamics of opioid receptors
- Unlocking the Therapeutic Potential of Previously Undruggable GPCRs
In general, signaling occurs when agonists engage key microswitch structures located in the TM domain Spurred on by new scientific and technological advances related to the understanding of structure and Screening directly identifies leads, and the structure-activity data obtained for the ensemble of candidate Available structural data across the GPCR superfamily is increasing at an exponential rate, alongside Sci Adv, 7. https://doi.org/10.1126/sciadv.abg8685 · Structural explanation of the binding and
- Odorant receptors – a bit of smell for drug discovery
Selective screening assays for ectopic ORs as well as investment on the structural characterization of function of ORs in vivo, development of in vitro systems for functional assays and the availability of structural information for structure-based drug design.
- 📰 GPCR Weekly News, February 5 to 11, 2024
Reviews, GPCRs, and more The dark sides of the GPCR tree - research progress on understudied GPCRs Structural and Molecular Insights into GPCR Function GPR161 structure uncovers the redundant role of sterol-regulated
- Functional modulation of PTH1R activation and signaling by RAMP2
Employing homology modeling, we describe the putative structural molecular basis underlying our functional
- A broad look into the future of systemic sclerosis
The authors provide a hierarchical structure into the studies of the pathogenesis of SSc starting with
- Pepducin-mediated G Protein-Coupled Receptor Signaling in the Cardiovascular System
We will discuss the historic context of pepducin development for each receptor, as well as the structural
- New Resources in GPCRdb
present and demonstrate the newest resources of the GPCRdb: 1) the new G protein resources and 2) the structural
- Mechanistic Understanding of the Palmitoylation of Go Protein in the Allosteric Regulation of...
Structural and energetic analyses indicated that the palmitoylation of Go can allosterically stabilize
- Targeted Therapies to Reduce Side Effects in Modern Drug Development
Modern drug development approaches include a range of techniques leveraging structural biology, immunology
- Discovery of 3(2-aminoethyl)-thiazolidine-2,4-diones as a novel chemotype of sigma-1 receptor ligand
hydrophobic groups of different sizes on both sides of the five-membered ring scaffold guided by the crystal structure
- To probe the activation mechanism of the Delta opioid receptor by an agonist ADL5859 started from...
Although the high-resolution crystal structures of the DOR with both agonist and antagonist have recently
- Lysine 101 in the CRAC Motif in Transmembrane Helix 2 Confers Cholesterol-Induced Thermal...
We envision that our results could have potential implications in structural biological advancements
- Neuropeptide S Encodes Stimulus Salience in the Paraventricular Thalamus
PVT NPSR1 neurons recruit the nucleus accumbens shell and structures in the prefrontal cortex and amygdala