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Compounds and were evaluated for their pharmacokinetic
2021-11-04
Compounds and were evaluated for their pharmacokinetic properties in rats and the results are summarized in . Following intravenous (IV) administration, both compounds displayed low clearance (CL), short half-lives (t) and low volumes of distribution (V). When dosed orally as a solution, exposure
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DDD107498 br Materials and methods br Results br Discussion
2021-11-04
Materials and methods Results Discussion The major findings of the present study are that: 1) the response to inverse agonists may be crossregulated by the activation of either DDD107498 H1 or H2 receptors, 2) histamine H1 and H2 receptor inverse agonists crossdesensitize the receptor´s re
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In our previous study we designed
2021-11-03
In our previous study, we designed and synthesized compounds of A series from the starting material 4-hydroxy-3-methoxycinnamic Estradiol Benzoate receptor (ferulic acid). These compounds with R group being amino acid residues, fatty acyl group and sulfuryl group showed moderate HDAC inhibition and
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Biological evaluations of the compounds were done
2021-11-03
Biological evaluations of the compounds were done both using HCV protease and replicon assays. Results are shown in . The protease inhibitory IC’s were determined using a FRET assay with HCV NS3/4A 1a protease domain. The replicon EC’s were determined using a replicon luciferase cell-based assay. Th
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Urinary As species monomethylated MMAV percentage might incr
2021-11-03
Urinary As species monomethylated (MMAV) percentage might increase and As species dimethylated (DMAV) percentage might decrease with increasing As exposure dosage (Lindberg et al., 2008). The limited methylation capacity associated with increased of As exposure dosage might probably explained throug
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niclosamide The endocytic inhibitors MDC and CPZ and dynamin
2021-11-03
The endocytic inhibitors MDC and CPZ and dynamin GTPase blocker (dynamin mutant) have been shown to significantly decrease the intracellular accumulation of cGMP. Moreover, earlier reports suggested that G-protein-coupled receptor (GPCRs) continue to signal by generating cAMP throughout internalizat
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Initial structural and biochemical work showed that Get form
2021-11-03
Initial structural and biochemical work showed that Get3 forms an obligate dimer whose conformation is regulated by the bound nucleotide. Analogous to SRP and SR, Get3 contains a P-loop nucleotide hydrolase domain in which the bound ATPs face one another at the dimer interface (Figure 3A, top right
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br Acknowledgements This work was supported by a grant from
2021-11-03
Acknowledgements This work was supported by a grant from the BBSRC (BB/D011809/1) to GJL and The Royal Society to SHS (Uf090321). SIM and AH were the recipients of scholarships from HEC Pakistan. Introduction Iron (Fe) is the fourth most abundant element in the earth’s crust. However, Fe is o
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br Methods and materials br Results Overall free glutamate
2021-11-03
Methods and materials Results Overall, free glutamate intakes in US children and adults are shown in Table 1. The sample-weighted mean intake of crude free glutamate was 258 mg/d for children and 322 mg/d for adults. Furthermore, the corresponding energy-adjusted value was 136 mg/1000 kcal and
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br Introduction L Glutamate is
2021-11-03
Introduction L-Glutamate is one of the most prevalent excitatory signaling molecules in the central nervous system (CNS) (Salazar et al., 2016) and plays a crucial role in a variety of folate analogue functions such as memory and learning (Danbolt, 2001, Nedergaard et al., 2002). At elevated conc
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Acknowledgments br Introduction The gut derived hormone oxyn
2021-11-03
Acknowledgments Introduction The gut-derived hormone oxyntomodulin (OXM) is a naturally occurring dual agonist of both the glucagon receptor (GCGr) and glucagons-like peptide 1 receptor (GLP-1r). Structurally OXM is the 29 Safingol of glucagon with a C-terminal octapeptide tail. Administration
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Analysis of the GHSR screening data for
2021-11-03
Analysis of the GHSR screening data for inactive library members indicated that the prolinol-derived secondary amine and α-substituted phenoxyacetamide moieties described in were critical for activity. As a result, we initiated the synthesis of follow-up libraries utilizing the solid-phase chemistr
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Ipratropium Bromide sale br Conclusions GPCRs are versatile
2021-11-03
Conclusions GPCRs are versatile signaling molecules regulating almost all physiological processes, including energy homeostasis and glucose homeostasis.105, 106 They also prove to be important therapeutic targets. Drugs targeting GPCRs account for 30% of current pharmaceutical sales. GPR40 is a m
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Macroautophagy hereafter referred to as autophagy
2021-11-03
Macroautophagy (hereafter referred to as autophagy) depends on an intracellular lysosome-dependent degradation system that maintains cellular metabolism and homeostasis [11]. Genes involved in these processes are termed autophagy-related genes (ATGs), which regulate autophagosome formation and compl
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Mammals and birds are sensitive
2021-11-03
Mammals and birds are sensitive either to hypo or hyper glycemia. In contrary some frogs when freezing/thawing experience very high glycemia (Storey and Storey, 1986). Nevertheless when the effect of temperature on Fru-2,6P2 concentration was investigated, the constant glucose level in frogs kept at
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