Results 71 to 80 of about 818,382 (379)

Agonist and antagonist TRUPATH assays for G protein-coupled receptors

open access: yesSTAR Protocols, 2022
Summary: TRUPATH is a bioluminescence resonance energy transfer-based platform for quantifying G protein-coupled receptor activity via dissociation of heterotrimeric G protein biosensors.
Jeffrey F. DiBerto   +3 more
doaj   +1 more source

By dawn or dusk—how circadian timing rewrites bacterial infection outcomes

open access: yesFEBS Letters, EarlyView.
The circadian clock shapes immune function, yet its influence on infection outcomes is only beginning to be understood. This review highlights how circadian timing alters host responses to the bacterial pathogens Salmonella enterica, Listeria monocytogenes, and Streptococcus pneumoniae revealing that the effectiveness of immune defense depends not only
Devons Mo   +2 more
wiley   +1 more source

Fusion protein strategies for cryo-EM study of G protein-coupled receptors

open access: yesNature Communications, 2022
Here, Zhang et al. explore fusion protein strategies to facilitate cryo-EM structural studies of GPCRs alone- without signal transducers- in ligand bound or unliganded form.
Kaihua Zhang   +4 more
doaj   +1 more source

Multiple endocytic pathways of G protein-coupled receptors delineated by GIT1 sensitivity. [PDF]

open access: yes, 2000
Recently, we identified a GTPase-activating protein for the ADP ribosylation factor family of small GTP-binding proteins that we call GIT1. This protein initially was identified as an interacting partner for the G protein-coupled receptor kinases, and ...
Achiriloaie, M   +6 more
core   +1 more source

Phosphatidylinositol 4‐kinase as a target of pathogens—friend or foe?

open access: yesFEBS Letters, EarlyView.
This graphical summary illustrates the roles of phosphatidylinositol 4‐kinases (PI4Ks). PI4Ks regulate key cellular processes and can be hijacked by pathogens, such as viruses, bacteria and parasites, to support their intracellular replication. Their dual role as essential host enzymes and pathogen cofactors makes them promising drug targets.
Ana C. Mendes   +3 more
wiley   +1 more source

Stabilization of G protein-coupled receptors by point mutations

open access: yesFrontiers in Pharmacology, 2015
G protein-coupled receptors (GPCRs) are flexible integral membrane proteins involved in transmembrane signaling. Their involvement in many physiological processes makes them interesting targets for drug development.
Franziska eHeydenreich   +7 more
doaj   +1 more source

Allostery of atypical modulators at oligomeric G protein-coupled receptors

open access: yesScientific Reports, 2021
Many G protein-coupled receptors (GPCRs) are therapeutic targets, with most drugs acting at the orthosteric site. Some GPCRs also possess allosteric sites, which have become a focus of drug discovery.
Rabindra V. Shivnaraine   +7 more
doaj   +1 more source

Molecular bases of circadian magnesium rhythms across eukaryotes

open access: yesFEBS Letters, EarlyView.
Circadian rhythms in intracellular [Mg2+] exist across eukaryotic kingdoms. Central roles for Mg2+ in metabolism suggest that Mg2+ rhythms could regulate daily cellular energy and metabolism. In this Perspective paper, we propose that ancestral prokaryotic transport proteins could be responsible for mediating Mg2+ rhythms and posit a feedback model ...
Helen K. Feord, Gerben van Ooijen
wiley   +1 more source

G-Protein–Coupled Receptors in Heart Disease

open access: yesCirculation Research, 2018
GPCRs (G-protein [guanine nucleotide-binding protein]–coupled receptors) play a central physiological role in the regulation of cardiac function in both health and disease and thus represent one of the largest class of surface receptors targeted by drugs.
Jialu Wang, C. Gareri, H. Rockman
semanticscholar   +1 more source

Ligand-guided homology modeling drives identification of novel histamine H3 receptor ligands [PDF]

open access: yes, 2019
In this study, we report a ligand-guided homology modeling approach allowing the analysis of relevant binding site residue conformations and the identification of two novel histamine H3 receptor ligands with binding affinity in the nanomolar range.
Hagenow, Stefanie   +3 more
core   +2 more sources

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