Results 61 to 70 of about 187,893 (285)

The planar cell polarity protein Vangl2 interacts with the PDZ‐domains of Scribble but not with a unique PDZ‐like domain in Inturned

FEBS Letters, EarlyView.
Structural and biochemical characterisations show that the planar cell polarity (PCP) protein Inturned harbours a unique PDZ‐like domain that does not bind canonical PDZ‐binding motifs (PBMs) like that of another PCP protein Vangl2. In contrast, the apical‐basal polarity protein Scribble contains four PDZ domains that bind Vangl2, but one PDZ domain ...
Stephan Wilmes, Jan Brysch, Carmen Gelze, Lilli Meier, Daniel Kümmel   +4 more
wiley   +1 more source

Ligand bias underlies differential signaling of multiple FGFs via FGFR1

eLife
The differential signaling of multiple FGF ligands through a single fibroblast growth factor (FGF) receptor (FGFR) plays an important role in embryonic development.
Kelly Karl, Nuala Del Piccolo, Taylor Light, Tanaya Roy, Pooja Dudeja, Vlad-Constantin Ursachi, Bohumil Fafilek, Pavel Krejci, Kalina Hristova   +8 more
doaj   +1 more source

Deciphering Complex Interactions in Bioactive Lipid Signaling

Molecules, 2023
Lipids are usually viewed as metabolic fuel and structural membrane components. Yet, in recent years, different families of lipids able to act as authentic messengers between cells and/or intracellularly have been discovered. Such lipid signals have been
Mauro Maccarrone
doaj   +1 more source

Multidisciplinary Consideration of Potential Pathophysiologic Mechanisms of Paradoxical Erythema with Topical Brimonidine Therapy. [PDF]

, 2016
Rosacea is a chronic inflammatory disease with transient and non-transient redness as key characteristics. Brimonidine is a selective α2-adrenergic receptor (AR) agonist approved for persistent facial erythema of rosacea based on significant efficacy and
Detmar, Michael, Di Nardo, Anna, Docherty, James R, Holmes, Anna, Lorton, Dianne, Schäfer, Gregor, Steinhoff, Martin   +6 more
core   +2 more sources

Tuning Biased GPCR Signaling for Physiological Gain [PDF]

Cell, 2017
Effective and safe doses of opiate painkillers, like morphine, can be limited by respiratory depression. Schmid et al. (2017) now present a quantitative method to design ligands and correlate GPCR signaling bias to the dose separation between therapeutic and adverse effects in animals.
Skylar, Spangler, Michael R, Bruchas
openaire   +2 more sources

Calpain small subunit homodimerization is robust and calcium‐independent

FEBS Letters, EarlyView.
Calpains dimerize via penta‐EF‐hand (PEF) domains. Using single‐molecule force spectroscopy, we measured the strength and kinetics of PEF–PEF homodimer binding. The interaction is robust, shows a transient conformational step before dissociation, and remains largely insensitive to Ca2+.
Nesha May O. Andoy, Trina Dykstra‐MacPherson, Mathias A. Bell, Peter L. Davies, Ruby May A. Sullan   +4 more
wiley   +1 more source

Biased agonism of GLP-1R and GIPR enhances glucose lowering and weight loss, with dual GLP-1R/GIPR biased agonism yielding greater efficacy

Cell Reports Medicine
Summary: Glucagon-like peptide-1 receptor (GLP-1R) and glucose-dependent insulinotropic polypeptide receptor (GIPR) agonists have recently been shown to play a significant role in the treatment of diabetes and obesity.
Ruben Rodriguez, Anne Hergarden, Shyam Krishnan, Marikris Morales, Davina Lam, Ted Tracy, Teresa Tang, Avalon Patton, Craig Lee, Asmita Pant, Daniel A. Erlanson, Johan Enquist, Derek Bone, Ray Fucini, Damian Bialonczyk, Stig K. Hansen, Jian Luo, Manu V. Chakravarthy   +17 more
doaj   +1 more source

Pharmacological Characterization of µ-Opioid Receptor Agonists with Biased G Protein or β-Arrestin Signaling, and Computational Study of Conformational Changes during Receptor Activation

Molecules, 2020
In recent years, G protein vs. β-arrestin biased agonism at opioid receptors has been proposed as an opportunity to produce antinociception with reduced adverse effects.
Justyna Piekielna-Ciesielska, Roberto Artali, Ammar A. H. Azzam, David G. Lambert, Alicja Kluczyk, Luca Gentilucci, Anna Janecka   +6 more
doaj   +1 more source

Structural Insights into CB1 Receptor Biased Signaling. [PDF]

Int J Mol Sci, 2019
The endocannabinoid system has emerged as a promising target for the treatment of numerous diseases, including cancer, neurodegenerative disorders, and metabolic syndromes. Thus far, two cannabinoid receptors, CB1 and CB2, have been discovered, which are found predominantly in the central nervous system (CB1) or the immune system (CB2), among other ...
Al-Zoubi R, Morales P, Reggio PH.
europepmc   +5 more sources

Diversity and complexity in neural organoids

FEBS Letters, EarlyView.
Neural organoid research aims to expand genetic diversity on one side and increase tissue complexity on the other. Chimeroids integrate multiple donor genomes within single organoids. Self‐organising multi‐identity organoids, exogenous cell seeding, or enforced assembly of region‐specific organoids contribute to tissue complexity.
Ilaria Chiaradia, Madeline A. Lancaster
wiley   +1 more source