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Early maternal obesity shapes offspring development through immune mechanisms: a systematized review. [PDF]

Front Immunol
Zhang J, Chen Y, Hu Z, Ding C, Chen J, Chen Y.   +5 more
europepmc   +1 more source

Gintonin as a Lysophosphatidic Acid-Enriched GPCR Ligand System: Molecular Architecture and Receptor Pharmacology in <i>Panax ginseng</i>. [PDF]

Biomolecules
Kim KH, Yoo BC.
europepmc   +1 more source

Bile acids and bile acid modification in health and disease: from novel modifications to therapeutic interventions. [PDF]

Front Endocrinol (Lausanne)
Yu C, Ye X, Zhao H, Qian S, Xie F, Liu Q.   +5 more
europepmc   +1 more source

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Flavors of GPCR signaling bias

Neuropharmacology
GPCRs are inherently flexible molecules existing in an equilibrium of multiple conformations. Binding of GPCR agonists shifts this equilibrium. Certain agonists can increase the fraction of active-like conformations that predispose the receptor to coupling to a particular signal transducer or a select group of transducers.
Vsevolod Gurevich, Mohammad Seyedabadi
exaly   +4 more sources

Signaling bias in drug discovery

Expert Opinion on Drug Discovery, 2017
The availability of different functional pharmacological assays has revealed that agonists for receptors that are pleiotropically coupled to multiple signaling pathways in the cell can emphasize signals to some pathways over others, i.e. can be biased toward certain signals.
T. Kenakin
exaly   +4 more sources

Measurement of Receptor Signaling Bias

Current Protocols in Pharmacology, 2016
AbstractG protein–coupled receptors (GPCRs) are often pleiotropically linked to numerous cellular signaling mechanisms in cells, and it is now known that many agonists differentially activate some signaling pathways at the expense of others. The mechanism for this effect is the stabilization of different active receptor states by different agonists ...
T. Kenakin
exaly   +4 more sources

Determining signaling bias

Science, 2018
GPCR Signaling G protein–coupled receptors (GPCRs) can mediate signaling through the G protein or β-arrestin pathways. Drugs that selectively activate one of these pathways provide effective treatment without side effects. GPCRs must undergo phosphorylation mediated by the GPCR kinase (GRK) family of kinases to recruit β-arrestins.
J. Foley
openaire   +2 more sources

The Measurement of Receptor Signaling Bias

Methods in molecular biology, 2015
This chapter describes a method to quantify biased signaling effects of agonists; this approach can furnish a scale for medicinal chemists to optimize biased profiles. Biased ligands have different pharmacological properties on a molecular level (stabilization of different receptor active states) and thus can have different pharmacological profiles ...
T. Kenakin
openaire   +3 more sources

Synthesis, biological, and structural explorations of a series of μ-opioid receptor (MOR) agonists with high G protein signaling bias.

European journal of medicinal chemistry, 2021
Biased agonism refers to the ability of compounds to drive preferred signaling pathways and avoid adverse signaling pathways in a ligand-dependent manner for some G-protein-coupled receptors. It is thought that the separation of therapeutic efficacy (e.g.
Yifei Yang, Yonghai Wang, Aixia Zuo, Chunmei Li, Wenyan Wang, Wanglin Jiang, Xiaochen Zhang, Xin Che, Yang Zhang, Wentao Wu, X. Cen, Hongbo Wang, Jingwei Tian   +12 more
semanticscholar   +1 more source

Phase retrieval with signal bias

Journal of the Optical Society of America A, 2009
The effect of a uniform measurement bias, due to background light, stray light, detector dark current, or detector offset, on phase retrieval wavefront sensing algorithms is analyzed. Simulation results indicate that the root-mean-square error of the retrieved phase can be more sensitive to an unaccounted-for signal bias than to random noise in ...
Samuel T, Thurman, James R, Fienup
openaire   +2 more sources