Results 51 to 60 of about 119,228 (259)

Molecular mechanism of Gαi activation by non-GPCR proteins with a Gα-Binding and Activating motif [PDF]

open access: yes, 2017
Heterotrimeric G proteins are quintessential signalling switches activated by nucleotide exchange on Gα. Although activation is predominantly carried out by G-protein-coupled receptors (GPCRs), non-receptor guanine-nucleotide exchange factors (GEFs) have
Baillie, George S.   +14 more
core   +1 more source

The therapeutic potential of allosteric ligands for free fatty acid sensitive GPCRs [PDF]

open access: yes, 2013
G protein coupled receptors (GPCRs) are the most historically successful therapeutic targets. Despite this success there are many important aspects of GPCR pharmacology and function that have yet to be exploited to their full therapeutic potential.
Hudson, Brian D.   +2 more
core   +1 more source

A Web Server for GPCR-GPCR Interaction Pair Prediction

open access: yesFrontiers in Endocrinology, 2022
The GGIP web server (https://protein.b.dendai.ac.jp/GGIP/) provides a web application for GPCR-GPCR interaction pair prediction by a support vector machine. The server accepts two sequences in the FASTA format. It responds with a prediction that the input GPCR sequence pair either interacts or not.
Wataru Nemoto   +7 more
openaire   +3 more sources

Tumour–host interactions in Drosophila: mechanisms in the tumour micro‐ and macroenvironment

open access: yesMolecular Oncology, EarlyView.
This review examines how tumour–host crosstalk takes place at multiple levels of biological organisation, from local cell competition and immune crosstalk to organism‐wide metabolic and physiological collapse. Here, we integrate findings from Drosophila melanogaster studies that reveal conserved mechanisms through which tumours hijack host systems to ...
José Teles‐Reis, Tor Erik Rusten
wiley   +1 more source

ER/K linked GPCR-G protein fusions systematically modulate second messenger response in cells. [PDF]

open access: yes, 2017
FRET and BRET approaches are well established for detecting ligand induced GPCR-G protein interactions in cells. Currently, FRET/BRET assays rely on co-expression of GPCR and G protein, and hence depend on the stoichiometry and expression levels of the ...
Dysthe, Matthew   +4 more
core   +1 more source

Orphan GPCR research [PDF]

open access: yesBritish Journal of Pharmacology, 2008
Orphan G protein‐coupled receptors (GPCRs) are receptors lacking endogenous ligands. Found by molecular biological analyses, they became the roots of reverse pharmacology, in which receptors are attempted to be matched to potential transmitters. Later, when high‐throughput screening technology was applied to reverse pharmacology, dozens of orphan GPCRs
S, Chung, T, Funakoshi, O, Civelli
openaire   +2 more sources

The photoswitchable cannabinoid azo‐HU308 enables optical control of Ca2+ dynamics in INS‐1 β‐cells via off‐target effects on TRPC channels

open access: yesFEBS Open Bio, EarlyView.
Light activation of the photoswitchable cannabinoid ligand azo‐HU308 triggers Ca2+ influx in pancreatic β‐cells through TRPC channels, independent of CB2 cannabinoid receptors. This reveals a non‐GPCR pathway for cannabinoid modulation of β‐cell Ca2+ dynamics and establishes azo‐HU308 as an optical tool to study cannabinoid signaling through TRP ...
Alexander E. G. Viray, James A. Frank
wiley   +1 more source

KLHL12 promotes non-lysine ubiquitination of the dopamine receptors D-4.2 and D-4.4, but not of the ADHD-associated D-4.7 variant [PDF]

open access: yes, 2015
Dopamine D-4 Receptor Polymorphism : The dopamine D-4 receptor has an important polymorphism in its third intracellular loop that is intensively studied and has been associated with several abnormal conditions, among others, attention deficit ...
Lintermans, Béatrice   +3 more
core   +12 more sources

Calcium-independent inhibitory G-protein signaling induces persistent presynaptic muting of hippocampal synapses [PDF]

open access: yes, 2011
Adaptive forms of synaptic plasticity that reduce excitatory synaptic transmission in response to prolonged increases in neuronal activity may prevent runaway positive feedback in neuronal circuits.
Chang, Chun Yun   +3 more
core   +2 more sources

Evaluating the Antiviral Efficacy of Encapsulated PKC Inhibitor BIM‐I against influenza A Virus Infection

open access: yesAdvanced Healthcare Materials, EarlyView.
This study explores nanoparticle delivery of the protein kinase C inhibitor bisindolylmaleimide‐I (BIM‐I) to combat influenza A virus infections. Encapsulation in biodegradable PLGA nanoparticles improved safety while maintaining the compound's strong antiviral activity.
Laura Klement   +12 more
wiley   +1 more source

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