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Two typical properties of Gi o protein coupled receptors nam
2021-10-03
Two typical properties of Gi/o protein-coupled receptors, namely an increase in 35S-GTPγS binding (Strange, 2010) and an inhibition of exocytotic noradrenaline release (Schlicker and Göthert, 1998), were not shared by H4 receptor activation on cortical membranes (guinea-pig and mouse) and cortical s
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The crystal structures of plant class ADH GSNOR from
2021-10-02
The crystal structures of plant class ADH3/GSNOR from Arabidopsis thaliana (AtGSNOR) and Solanum lycopersicum cv. Amateur (SlGSNOR) with bound substrates and cofactors revealed important differences between plant and human enzyme, namely within the substrate-binding pocket. GSNOR are unusually homod
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While published data around the
2021-10-02
While published data around the functional significance of GPR84 are quite sparse, details of signaling pathways initiated by the receptor are even more limited, including in recombinant systems. In recombinant cells, GPR84 activation reportedly leads to Gi pathway activation, resulting in pertussis
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br TGR agonists current developments and future landscape Th
2021-10-02
TGR5 agonists: current developments and future landscape The amphipathic nature of bile acids is crucial in aiding the digestion and Z-VDVAD-FMK of vitamins and fats. With the emerging roles of bile acids in the regulation of energy and glucose homeostasis through TGR5, the pharmaceutical indust
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Hepatic drug metabolizing enzymes and transporters expressio
2021-10-02
Hepatic drug-metabolizing ci-1033 and transporters expression were regulated by nuclear receptors [19], [20], [21]. The effects of HFD-induced fatty liver on drug metabolizing enzymes in mice were recently studied, and the results provided a systematic evaluation of the changes of nuclear receptors
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KPT-276 Binding of FGFs to FGFRs
2021-10-01
Binding of FGFs to FGFRs leads to receptor dimerization, resulting in the transphosphorylation of a tyrosine in the activation loop of the kinase domain. Subsequently, the activated FGFRs phosphorylate their intracellular receptor substrates, particularly FGFR substrate 2 (FRS2) and phospholipase Cγ
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Introduction Type diabetes T D has been seriously affecting
2021-10-01
Introduction Type 2 diabetes (T2D) has been seriously affecting the health life of 415 million people and 193 million undiagnosed people [1]. Importantly, this disease was found to cause death at least 1.5 million annually, and has brought about an extensive health concern throughout the world [2,3
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Not only has the cortical actin network been found
2021-10-01
Not only has the cortical Penciclovir Sodium network been found to influence plasma membrane properties but also to interact with exo- and endocytic vesicles (Gormal et al., 2015, Tomatis et al., 2013). The interplay between actin and membranes is integrally regulated by the phosphoinositide compos
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We also demonstrated that inhibition
2021-10-01
We also demonstrated that inhibition of NAAG hydrolysis to suppress glutamate production through a GCPII inhibitor is a viable target for cancer therapy. GCPII is also known as N-acetyl-L-aspartyl-L-glutamate peptidase I (NAALADase I) or NAAG peptidase (Pinto et al., 1996), and its increased express
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L Family Leguminosae widely distributed in
2021-10-01
L. (Family Leguminosae) widely distributed in tropical and subtropical regions of the world. As a medicinal and edible plant, it is widely used in Asia, especially in China, Korea, Japan and India. It was first recorded in Shen Nong Ben Cao Jing (神农本草经), and was described having the effect of cleari
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br GR Is a Transcriptional Activator How GR activates
2021-10-01
GR Is a Transcriptional Activator How GR activates some genes while repressing others remains unsettled after decades of study. While significant controversy exists regarding GR-mediated repression, a consensus model for transcriptional activation has emerged: GR activates transcription through s
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Animal studies have shown that various antidepressant treatm
2021-10-01
Animal studies have shown that various antidepressant treatment are capable of upregulating GR protein and mRNA in key ruthenium red australia regions including the hippocampus and decreasing basal and/or stress-induced glucocorticoid secretion [37]. Changes in the level or function of GR regulate t
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The experiments indicate that a major
2021-10-01
The experiments indicate that a major component of the vasodilatation is due to antagonism of α 1-adrenoceptors. Evidence for α1-adrenoceptor antagonism is that vasodilatation was observed in pentylenetetrazol preconstricted with α1-adrenoceptor agonists, phenylephrine or methoxamine, but not in ves
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The absence of differences between GalR knockout and wild
2021-10-01
The absence of differences between GalR1 knockout and wild type mice in kainic acid-induced seizures suggests that GalR1 do not interfere with the seizure-inducing action of kainic acid. Postsynaptic kainate receptors are excitatory ionotropic glutamate receptors and their activation leads to seizur
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Moreover studies on subcellular localization of
2021-09-30
Moreover, studies on subcellular localization of FBPase in carp heart and smooth muscle revealed nuclear localization of the enzyme. Previously, we have unequivocally demonstrated the presence of FBPase in the nuclei of mammalian cardiomyocytes (Gizak and Dzugaj, 2003) and myocytes (Gizak et al., 20
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