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br Experimental br Results and discussion
2022-06-27

Experimental Results and discussion One of the major challenges of oral drug delivery via nanocarriers is the fairly low efficiency of crossing the intestinal barrier. While there is the possibility of a paracellular transport for polar substances below 1000 Dalton [26], the key mechanism of o
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br Acknowledgments I thank Takeshi Sakaba
2022-06-27

Acknowledgments I thank Takeshi Sakaba for critical reading of the manuscript and helpful comments. This work was supported by JSPS/MEXT KAKENHI Grant Numbers 17K19466, 17H03548. Introduction The oral route of drug application is the main route in pharmacology since it is easy to handle and o
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Liposomes that are less than nm in diameter are necessary
2022-06-27

Liposomes that are less than 200nm in diameter are necessary to optimize uptake of liposomes by Ifosfamide (Oesterling et al., 2014). The liposomes constructed in these experiments were found to be sufficiently small in diameter for use in in vivo and in vitro experiments. Even smaller diameters are
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The variants all occurred at residues
2022-06-27

The 17 variants all occurred at residues conserved among vertebrates (Figure 1B) and in regions depleted in missense variants in gnomAD. Indeed, when we assessed missense tolerance ratios for TRRAP, we observed that most of the 17 variants were in regions intolerant to missense variants (Figure 2B).
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br Discussion Our results showed
2022-06-27

Discussion Our results showed that the histamine H1 receptor antagonist/inverse agonists, pyrilamine and cetirizine, attenuated not only NMDAR-mediated synaptic current but also LTP in Shaffer collateral-CA1 pyramidal neuron synapses. The H1 receptor antagonist/inverse agonist-induced attenuation
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MK cyclobutylpiperidin yl oxyphenyl methyl trifluoromethyl q
2022-06-27

MK-3134 (3-[4-(1-cyclobutylpiperidin-4-yl)oxyphenyl]-2-methyl-5-(trifluoromethyl)quinazolin-4-one) was synthesized by Merck, as the structurally constrained analogue of MK-0249 (Nagase et al., 2008). This H3R inverse agonist has MW 457.49, seven HBA, and MLogP 4.58, with one violation in terms of dr
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The site of metastasis in
2022-06-27

The site of metastasis in breast cancer often contributes to the patient’s OS. Patients with bone metastasis from their breast cancer often have a notably increased survival over patients with visceral or ikk pathway metastasis. In this analysis, ER+/HER2+ patients were noted to have a higher rate
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Treatment and control for IBD are targeted to
2022-06-27

Treatment and control for IBD are targeted to identify and eliminate the cause if possible, decrease intestinal inflammation, reduce diarrhea and vomiting, improve appetite, and promote weight gain. Methods include dietary manipulation with or without concurrent medical therapy such as corticosteroi
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It is extremely difficult to predict a
2022-06-27

It is extremely difficult to predict a plausible conformer of hsGCαβ heterodimer with right orientation of multiple domains. Even though the template identities in case of dimeric domains were not high enough but still we modelled the entire heterodimeric structure of hsGCαβ with a reasonable and ju
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br Conclusion and future perspectives
2022-06-27

Conclusion and future perspectives The nicotinic RGFP966 receptor GPR109A and its close relatives GPR109B and GPR81 are primarily expressed in adipocytes and are coupled to Gi-type G proteins. Recently, the ketone body β-hydroxy-butyrate, the β-oxidation intermediate 3-hydroxy octanoic acid and l
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br Glycoengineering br The Omics perspective The publication
2022-06-24

Glycoengineering The « Omics » perspective The publication of the CHO-K1 genome sequence in 2011, followed by the publication of two Chinese hamster and six CHO cell line genomes in 2013, bring new opportunities in developing and engineering CHO FPS-ZM1 for improved glycoprotein production (X
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In this study we examined whether zebrafish ionocytes might
2022-06-24

In this study, we examined whether zebrafish ionocytes might also share other types of similarity in transport function with kidney cells. In addition to ion transport, mammalian kidney c1v1 c2v2 calculator also play key roles in xenobiotic elimination, through the action of ATP-Binding Cassette (A
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br Vesicular glutamate transporters VGLUTs br Conclusions Du
2022-06-24

Vesicular glutamate transporters (VGLUTs) Conclusions Due to the molecular cloning of EAAT and VGLUT subtypes, a better understanding of the functional properties of these carriers has been elucidated over the last few years. In the case of the EAATs, specific blockers, such as trans-2,4-PDC,
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A number of anti diabetic drugs are available that inhibit
2022-06-24

A number of anti-diabetic drugs are available that inhibit α-glucosidase activity, including acarbose, voglibose and miglitol [6,7]. These inhibitors, however, also exhibit undesirable side effects, such as adverse gastrointestinal symptoms and liver toxicity [8,9]. For diabetics, it would therefore
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There are two ways to
2022-06-24

There are two ways to transport FFAs into cells. First by passive diffusion. Second as the putative long-chain fatty AZ191 transporters are proposed, CD36 the plasma membrane-associated fatty acid-binding protein (FABPpm) and fatty acid transport proteins (FATP) [11], where CD36 is responsible for
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