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To further investigate if GPR was the
2022-05-23
To further investigate if GPR40 was the functional target of these phenylpropiolic 5720 analogs, GW-1100, a selective antagonist of GPR40-mediated Ca2+ elevations in HEK293 cells with an IC50 value equal to 1 μM, was used to inhibit agonist-induced intracellular calcium flux [15]. HEK293-GPR40 cell
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However it is unclear whether the parent and transition meta
2022-05-23
However, it is unclear whether the parent and transition metal substitution in Keggin-type phosphomolybdic DAPI hydrochloride receptor will reveal the best effects on α-glucosidase. Therefore, the Keggin-type H3PMo12O40 (abbreviated as PMo12) and three transition metal-substituted POMs (Na4PMo11VO40
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Nuclear export of GK has been reported to
2022-05-23
Nuclear export of GK has been reported to be dependent on a GK nuclear export signal (NES), mapped to residues 300–310 (Shiota et al., 1999). The assignment of a nuclear export signal common to both the liver and pancreatic GK isoform sequence suggests a possible reversible translocation of GK acros
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During the tests in vitro SHP showed the beneficial effect
2022-05-23
During the tests in vitro, SHP289-04 showed the beneficial effect on both two important aspects. In human liver carcinoma cell line HepG2, it was found to improve glucose consumption significantly. Otherwise, in pancreas cell line NIT1, it could only promote insulin secretion significantly at high g
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Recently several dual GLP GIP receptor
2022-05-23
Recently, several dual GLP-1/GIP receptor agonists have been developed as a treatment of type II diabetes. These peptides can activate both the GLP-1 and the GIP receptor. Such dual receptor agonists are superior compared to single GLP-1 analogues such as liraglutide (Finan et al., 2013). Previously
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br Conclusion Our experiments have confirmed
2022-05-23
Conclusion Our experiments have confirmed the effects of fasting, DIO, and E2 on the expression of Ghsr, Npy, and Agrp in the ARC (Briggs et al., 2013, Briggs et al., 2010, Brown and Clegg, 2010, Coppola et al., 2007, Palou et al., 2009, Roepke et al., 2008, Verhulst et al., 2012). However, gene
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ARCA Cy5 EGFP mRNA br Introduction Ghrelin is a amino acid p
2022-05-23
Introduction Ghrelin is a 28-amino ARCA Cy5 EGFP mRNA peptide mainly produced in the stomach and small intestines with the kidneys, placenta, and pancreas contributing to miniscule amounts of circuiting ghrelin [1]. Ghrelin exists in circulation in two major forms: acyl ghrelin (AG) and desacyl g
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Piezo channels can be activated by
2022-05-23
Piezo channels can be activated by many mechanical stimuli . While some of these stimulations directly mimic physiological forces experienced by ON-01910 , such as shear stress applied in a microfluidic chamber, the most commonly used modes of stimulation consist of stretching the membrane by appl
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Many investigators have noted structural similarities betwee
2022-05-23
Many investigators have noted structural similarities between certain flavonoids and benzodiazepines, such as diazepam, that are the most widely studied positive modulators of GABAA receptors. Benzodiazepines can act on these receptors via ‘two distinct and separable mechanisms’ (Walters, Hadley, Mo
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Introduction Osteoclasts are large multinuclear cells
2022-05-23
Introduction Osteoclasts are large, multinuclear Spectinomycin hydrochloride hydrate that are responsible for the resorption (breakdown) of bone [1]. Together with osteoblasts, the bone forming cell, they maintain the integrity of the skeleton through constant resorption and repair of bone. Osteocl
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In vitro studies have described
2022-05-23
In vitro studies have described the kinetic parameters of the KDM4A catalytic site (cKDM4A) (Figure 1C) (23); the kcat/KM (kcat as the catalytic constant and KM as the Michaelis constant) values represent how fast the enzyme reacts with the substrate once it encounters the substrate, where the value
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Arena Pharmaceutical introduced a biaryl sulfone derivative
2022-05-23
Arena Pharmaceutical introduced a biaryl sulfone derivative with antagonistic activity at H3Rs known as APD-916, ((R)-1-(2-(4'-(3-methoxypropylsulfonyl)biphenyl-4-yl)ethyl)-2-methylpyrrolidine), which was rationally designed from corresponding sulfonamides in order to yield compounds with short dura
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br Methods br Acknowledgements We are
2022-05-23
Methods Acknowledgements We are grateful to Eric Olson for providing Yap/Taz floxed mice, and to members of the Epstein lab for helpful comments and advice. This work was supported by NIH R01 HL118768, R35 HL140018, the Cotswold Foundation and the WW Smith Endowed Chair to J.A.E. The Hippo
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It is not established if ONOO also
2022-05-23
It is not established if ONOO− also induces tyrosine nitration of ANT and affects VDAC1 and ANT interaction, as well as the interaction of VDAC1 with HK II, all of which are events that may lead to altered mitochondrial and cellular function. Thus, in this study we examined tyrosine nitration of bot
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It is acknowledged that mitochondrial outer membrane permeab
2022-05-23
It is acknowledged that mitochondrial outer membrane permeabilisation is a pivotal signal for apoptosis, which leads to the liberation of pro-apoptotic molecule such as cytochrome c and post-caspase activation [37]. As a consequence of the protection of mitochondrial integrity, AIV improved mitochon
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