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Recently a receptor for nicotinic
2021-09-23

Recently, a receptor for nicotinic acid, named GPR109A (also known as HM74a in man or PUMA-G in the mouse) has been identified (Lorenzen et al., 2001, Lorenzen et al., 2002, Soga et al., 2003, Tunaru et al., 2003, Wise et al., 2003). This receptor, a member of the 7 transmembrane G-protein coupled f
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TGR is a class A
2021-09-23

TGR5 is a class A GPCR, transducing signal through Gs-protein mediated cAMP accumulation, and was recently reclassified as the founder member of the bile–acid receptor subclass of GPCRs [22]. The cAMP-mediated signaling of TGR5 activation has been implicated in a range of cellular physiological acti
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br Introduction Cell surface receptors are central to the in
2021-09-23

Introduction Cell surface receptors are central to the interaction of cells with their surroundings and play an important role in determining functional responses. These receptors are integral membrane proteins responsible for the binding of extracellular signaling molecules and transduction into
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br Discussion The present study showed that the
2021-09-23

Discussion The present study showed that glut1 the factors of pre-exposure and glutamate drug injections might affect the total latency time. However, the factor of sex did not affect the total latency time. The results indicate that the glutamate system and pre-exposure, but not sex, influence
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The rapid actions of glucocorticoids range
2021-09-23

The rapid actions of glucocorticoids range from the production of endocannabinoid as a retrograde messenger [9], to regulation of ion channels [10], [11], to inhibitory effects on immune K-252c [12], [13], [14]. Many different kinase signaling pathways have been implicated in the rapid actions of gl
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Besides its established insulinotropic actions GIP has been
2021-09-23

Besides its established insulinotropic actions, GIP has been shown to possess other direct beneficial effects on the beta cell, including stimulation of growth, differentiation, proliferation and survival.21, 22, 23 It has also been shown to stimulate proinsulin gene transcription and translation. M
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br Conflict of interest br Transparency document
2021-09-23

Conflict of interest Transparency document Acknowledgements We acknowledge our funding sources from the American Heart Association (13EIA4480016) and the National Institute of Health/National Heart, Lung, and Blood Institute (RO1 HL094414). We are very grateful to Dr. Shaohua Xiao and Dr. S
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Many investigators have noted structural similarities betwee
2021-09-23

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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Herein we describe the design and optimization
2021-09-22

Herein, we describe the design and optimization of fused-ring phenyl propanoic acids as novel GPR40 agonists, leading to the discovery of compound 40a which exhibits excellent pharmacokinetic properties, improved hepatobiliary transporter inhibition, and significant glucose-lowering efficacy during
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br Methods and materials br Results br Discussion In
2021-09-22

Methods and materials Results Discussion In this study we demonstrate that CF epithelial metaformin synthesis exhibit features of apoptosis in their basal, unstimulated state including increased caspase (-3 and -8) activation compared to non-CF epithelial cells. Analysis of factors respons
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a replacement Depletion of PI P e
2021-09-22

Depletion of PI(4,5)P2, e.g. by knockout of PIPKIγ, also profoundly inhibits SV endocytosis (Di Paolo et al., 2004). Conversely, loss of the PI(4,5)P2-metabolizing PI-phosphatase synaptojanin or its recruitor endophilin stalls SV recycling at the level of clathrin-coated vesicles (Bai et al., 2010,
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br Problem of cellular retention not only affects the
2021-09-22

Problem of cellular retention not only affects the cellular activity of the nanoparticles and nanocomplexes but can also have ramifications in their in vivo applications. While inorganic nanoparticles are being developed extensively for detection as well as treatment of different human diseases, i
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br Histamine H R The cloning of the H
2021-09-22

Histamine H4R The cloning of the H3R (Lovenberg et al., 1999) provided a template for the search of other hop over to this website receptors, and resulted in the most recent discovery of histamine H4R. This concluded with six independent groups that have reported the cloning of the H4R (Leurs et
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10-Hydroxycamptothecin synthesis In various models histamine
2021-09-22

In various models, histamine has been shown to induce chemotaxis. This was first appreciated over 40 years’ ago in studies with eosinophils (Clark et al., 1977). At that time, only histamine H1 and histamine H2 receptors were recognized and studies with ligands to these receptors indicated that neit
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According to the experimental data HKI preferentially
2021-09-22

According to the experimental data, HKI preferentially binds to the mitochondrial inter-membrane contact sites formed by ANT and VDAC [[5], [6], [7],27], mainly via the VDAC1 isoform [7,8]. These electrogenic contact sites allow application of a part of IMP to MOM by transferring phosphoryl groups f
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