The conformation-selective antibody, Fab30, promotes partially activated βarr into the activated-like

heterotrimeric G protein activity biosensors Marta Lopez-Balastegui , Antonella Di Pizio , Jiafei Mao , Jana Selent Principles of Pharmacology in Drug Discovery II -   Advanced Methods for the Optimization of Candidate Selection

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

serum lipid profile, attenuation of the damage following ischemia-reperfusion, the regulation of blood pressure

serum lipid profile, attenuation of the damage following ischemia-reperfusion, the regulation of blood pressure

on Highly biased agonism for GPCR ligands via nanobody tethering Elk Kossatz, Michel Bouvier, Jana Selent pancreatic polypeptide from a structural, functional, and therapeutic perspective Structural basis for selectivity

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

Propranolol, initially prescribed for high blood pressure, irregular heart rate, essential tremor, and

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

However, these drugs show adverse effects, including increased blood pressure in mirabegron patients.

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

GPR3 knockout mice were vulnerable to neural death during aging without affecting high intraocular pressure

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

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

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