called promising candidates in G protein-coupled receptor (GPCR) drug development by displaying subtype selectivity

Endogenous l- to d-amino acid residue isomerization modulates selectivity between distinct neuropeptide Structural and Molecular Insights into GPCR Function Structural basis of selective cannabinoid CB2 receptor

Our results suggest that strategies to selectively target OGR1 expression may represent a novel therapeutic

GPCR Activation and Signaling Coupling between GPR143 and dopamine D2 receptor is required for selective D2 receptor ligand binding and signaling GPCR Binders, Drugs, and more Discovery of the Potent and Selective

protein-biased GPR3 mouse model to investigate the physiological and pathophysiological consequences of selective

Pc(4-4), a lead backbone cyclic peptide, was selected out of a mini-library, directed toward PAR2&4 PH-binding

available to study the contribution of PKC isozymes have considerable limitations, including a lack of selectivity

mechanistic insights of our study provide clues for the future design of isoform-specific GPR35 ligands that selectively

Individual cancer types were enriched for highly impactful, recurrent mutations at selected cognate positions

targets Constitutive activity of the dopamine receptor D5R, highly expressed in CA1 hippocampal neurons, selectively

Cannabinoid 1 (CB1 ) receptor arrestin subtype-selectivity and phosphorylation dependence. GPCR Binders, Drugs, and more Ligands selectively tune the local and global motions of neurotensin receptor

β -arrestin interaction and demonstrates altered regulatory outcomes downstream of this functional selectivity

GPCR Binders, Drugs, and more Rational design of highly stabilized and selective adrenomedullin analogs

Synthetic signaling platforms permitting precise and selective Ca2+ signal transduction can improve dissection

The impact of ACEA is inhibited by the selective CB1 receptor antagonist, rimonabant.

determined by NMR via Methyl Relaxation Structural determinants of sphingosine-1-phosphate receptor selectivity

The potent BECN2-ATG14 coiled-coil interaction is selectively critical for endolysosomal degradation

GPCRs in Neuroscience Conformationally Selective 2-Aminotetralin Ligands Targeting the alpha2A- and alpha2C-Adrenergic

Industry News Arcoscreen selected by START Lausanne to pitch at the START Global summit on the 23-24th

In contrast, when the GPR55 receptor is simulated in complex with the selective agonist ML186, agonist-like

Submit your abstracts for poster presentation using this form - short talks will be selected from these

Traditionally, it was believed that GPCRs selectively activate only their cognate G protein subtypes,

Methods & Updates in GPCR Research Development and Characterization of a Highly Selective Turn-On Fluorescent

Selection of the libraries typically leads to the isolation of several hundred candidate hits, enriched initial search for potent target receptor modulators is agnostic towards signaling activity because it selects While the native ligand conjugate exhibited poor selectivity for CCR5-expressing cells and was less effective unconjugated MMAE, the Orion CCL5 superagonist analog significantly increased both the potency and selectivity

While some receptors selectively activate specific G protein families, others are more versatile, yielding resonance energy transfer (BRET), and multi-color fluorescence microscopy assays employ conformation-selective

analysis restricted to variants impacting gene function Interaction modes of human orexin 2 receptor with selective

dimerization of GLP-1R results in decreased high-affinity binding to its natural ligand, GLP-1, while selectively

Hexahydroquinoline Derivatives are Selective Agonists for the Adhesion G Protein-Coupled Receptor ADGRG1