Results 21 to 30 of about 6,222 (140)
Guanosine 5′-O-(3-Thiotriphosphate) (GTPγS) Stimulation of GLUT4 Translocation is Tyrosine Kinase-dependent [PDF]
Guanosine 5'-O-(3-thiotriphosphate) (GTPgammaS) treatment of permeabilized adipocytes results in GLUT4 translocation similar to that elicited by insulin treatment. However, although the selective phosphatidylinositol 3-kinase inhibitor, wortmannin, completely prevented insulin-stimulated GLUT4 translocation, it was without effect on GTPgammaS ...
J S, Elmendorf, D, Chen, J E, Pessin
openaire +2 more sources
Therapeutic validation of an orphan G protein‐coupled receptor: The case of GPR84
Despite the importance of members of the GPCR superfamily as targets of a broad range of effective medicines many GPCRs remain poorly characterised. GPR84 is an example. Expression of GPR84 is strongly up regulated in immune cells in a range of pro‐inflammatory settings and clinical trials to treat idiopathic pulmonary fibrosis are currently ongoing ...
Sara Marsango +4 more
wiley +1 more source
Gentle handling performed to naïve rats before receiving an aversive stimulus exacerbates fear in a subsequent PA exposure, whereas NORT previous to an aversive stimulus reduces passive avoidance response. Freezing, the main indicator of fear response in PA, is reduced in groups that performed handling or NORT before PA, and it correlates with CB1 ...
Iker Bengoetxea de Tena +8 more
wiley +1 more source
Enzymatic Assays to Explore Viral mRNA Capping Machinery
To escape recognition by the host innate immune system, viruses often incorporate 5′ caps into their mRNAs. The differences in mRNA capping make this process an interesting therapeutic target. Here, we review methods to explore the enzymes involved in cap biosynthesis. Such methods allow inhibitor selection, facilitating antiviral drug discovery, which
Renata Kasprzyk, Jacek Jemielity
wiley +1 more source
In the present study, binding affinities of 5-hydroxytryptamine-4 (5-HT4) ligands for the human 5-HT4d receptor were determined using the agonist [3H]5-HT and the selective 5-HT4 antagonist [3H]GR113,808. We also compared the affinity differences between
Tadayoshi Mikami +5 more
doaj +1 more source
Guanosine 5'-O-(3-thiotriphosphate) inhibits capping of reovirus mRNA.
RNA synthesized by reovirus cores was not capped or methylated when GTP was replaced by guanosine 5'-O-(3-thiotriphosphate) [gamma-S]GTP as a reaction substrate. Full length transcripts were synthesized in the presence of [gamma-S]GTP which indicated that capping could be dissociated from the process of transcription.
A E, Reeve, A J, Shatkin, R C, Huang
openaire +2 more sources
Dimerization of the small GTPase Arf is prerequisite for the scission of COPI‐coated transport vesicles. Here, we quantify the monomer/dimer equilibrium of Arf within the membrane and show that after membrane scission, Arf dimers are restricted to donor membranes.
Petra Diestelkoetter‐Bachert +10 more
wiley +1 more source
Guanosine 5'-O-(3-thiotriphosphate), a potent nucleotide inhibitor of microtubule assembly.
Guanosine 5'-O-(3-thiotriphosphate) (GTP gamma S) and the two diastereoisomers of guanosine 5'-O-(2-thiotriphosphate) (GTP beta S) were prepared enzymatically, and their interactions with tubulin and microtubule-associated proteins (MAPs) in 0.1 M 2-(N-morpholino)ethanesulfonate, 0.5 mM MgCl2 were examined.
E, Hamel, C M, Lin
openaire +2 more sources
Background. Adrenaline quickly inhibits the release of histamine from mast cells. Besides β2‐adrenergic receptors, several in vitro studies also indicate the involvement of α‐adrenergic receptors in the process of exocytosis. Since exocytosis in mast cells can be detected electrophysiologically by the changes in the membrane capacitance (Cm), its ...
Nozomu Abe +7 more
wiley +1 more source
Developmental Potential for Endomorphin Opioidmimetic Drugs
Morphine, which is agonist for μ‐opioid receptors, has been used as an anti‐pain drug for millennia. The opiate antagonists, naloxone and naltrexone, derived from morphine, were employed for drug addiction and alcohol abuse. However, these exogenous agonists and antagonists exhibit numerous and unacceptable side effects.
Yoshio Okada +4 more
wiley +1 more source

