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SP 141 Compound was synthesized in a racemic fashion
2021-09-23
Compound was synthesized in a racemic fashion with this study and plans for an enantioselective synthesis could be developed based on the activity of racemic . Synthesis of compound followed a slightly different synthetic route due to the ineffectuality of the S2 reaction on the secondary position
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Pirfenidone br Materials and methods br Results
2021-09-23
Materials and methods Results and discussion Conflict of interest Introduction In the presence of continuous and excessive levels of nutrients, adipocytes become hypertrophic and release several pro-inflammatory adipocytokines such as interleukin-6 (IL-6), monocyte chemoattractant protei
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GPR A a G protein coupled receptor located
2021-09-23
GPR109A, a G-protein-coupled receptor located mainly on adipocyte cell membranes, has been identified as the molecular target for nicotinic RO4987655 [[5], [6], [7]] and mediator of NEFA reduction [5]. As a mechanism of NEFA-lowering, it is recognized that activation of GPR109A leads to Gi-mediated
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Mapping and separation of the
2021-09-23
Mapping and separation of the anti-GlyT1C epitopes allowed us to verify the existence of calpain cleavage sites in isolated mouse synaptosomes. In order to allow calcium to enter the intrasynaptosomal compartment and activate endogenous calpain, we incubated synaptosomes in hypoosmotic high (200μM)
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br Materials and methods br Results
2021-09-23
Materials and methods Results Discussion The GO system is an important mechanism for maintaining the integrity of genetic material in many eukaryotic organisms. This is demonstrated by the high conservation, across different evolutionary lineages, of the sequences of the proteins that compo
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The GlyR is pentameric with each subunit consisting of an
2021-09-23
The GlyR is pentameric, with each subunit consisting of an extracellular ligand binding domain (LBD), four transmembrane (TM) segments, and a large intracellular loop between TM3 and TM4. Binding of neurotransmitter produces conformational changes that are rapidly transmitted to the membrane-spannin
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br Materials animals and methods br Results br Discussion Th
2021-09-23
Materials, animals and methods Results Discussion This study presents mice with a missense point mutation in R258 of FFAR1 that has functional consequences. Firstly, in islets of Ffar1R258W/R258W mice, both the physiological agonist palmitate and the synthetic agonist TUG-469 were unable to
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To get a broader view of the interplay
2021-09-23
To get a broader view of the interplay between glycolysis and Hippo signaling, we tested the involvement of YAP1 in the regulation of C-MYC and GLUT1 expression. We were able to detect a YAP1-TEAD1 interaction in the nuclear fraction of Jurkat Phos-tag synthesis and confirm the inhibition of this in
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However it is unclear whether the parent and
2021-09-23
However, it is unclear whether the parent and transition metal substitution in Keggin-type phosphomolybdic AMG-900 will reveal the best effects on α-glucosidase. Therefore, the Keggin-type H3PMo12O40 (abbreviated as PMo12) and three transition metal-substituted POMs (Na4PMo11VO40, Na6PMo11FeO40 and
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br Materials and methods br
2021-09-23
Materials and methods Results and discussion Conclusion Altogether, our data provide an unexpected insight into Cx26 trafficking pathway and gap junction assembly in the cochlea. Since many of the disease-causing mutations in GJB2 impair the trafficking and delivery of Cx26 to the cell surf
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FFAs are essential nutritional molecules that can also modul
2021-09-22
FFAs are essential nutritional molecules that can also modulate numerous cellular functions. Fatty Penciclovir derivatives like prostaglandins, leukotrienes lysophosphatidic acid, spinhgosine-1-phosphate and others are well documented to carry out signal transduction via G-protein coupled receptors
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Hydrocortisone The minimal segment of the
2021-09-22
The minimal segment of the SIM appears to be a core of Hydrocortisone residues, which frequently matches the consensus sequences ΨΨΨΨ, ΨxΨΨ, or ΨΨxΨ (where Ψ is V, I, or L and x is typically D, E, S, or T) [29,31,32]. In a subset of SIMs, this hydrophobic core is flanked by serine residues and a st
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br Materials and methods br
2021-09-22
Materials and methods Results Discussion Several histamine H3 receptor antagonists have progressed into clinical development for indications including Alzheimer's disease, schizophrenia, pain and narcolepsy. Each of the compounds studied herein has been extensively characterized in its own
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Although the presence of histamine
2021-09-22
Although the presence of histamine-secreting bacteria has been well documented in foods, their presence within the human gut microbiota has not been investigated in detail. We recently performed an analysis of fecal samples from 161 volunteers to quantify the presence of bacterial HDC, using primers
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The relationship between the attention
2021-09-22
The relationship between the attention deficit hyperactivity disorder (ADHD) and H3Rs is supported by several reports (Berlin et al., 2011; Passani, Bacciottini, Mannaioni, & Blandina, 2000; Vohora & Bhowmik, 2012). ADHD is a neurobehavioral disorder with high prevalence in children, with hyperactiv
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