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bms-708163 PKC does not however directly
2022-03-30

PKC does not, however, directly stimulate secretion by initiating calcium influx into the cell [51]. Work from multiple groups measuring calcium currents has shown that PMA alone or coupled with glucose does not modulate intracellular calcium influx [34], [51], [52], [53]. Instead of contributing to
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AD is a major neurological disorder
2022-03-30

AD is a major neurological disorder, usually effecting the elderly population, which is difficult to diagnose until symptoms begin to accumulate. As of 2013, approximately five million Americans were living with AD. The number with this disease is projected to be 16 million by 2050 (Hebert et al., 2
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Although the presence of histamine
2022-03-30

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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In tumor cells HK II induction is
2022-03-30

In tumor cells HK-II induction is mediated by Akt/mTOR pathway [6], [11]. HK-II dynamically shuttles between the mitochondria and cytoplasm under different metabolic conditions. In cardiomyocytes, Akt enhances HK-II binding to mitochondria, setting the heart at a state resistant to ischemic injury [
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br Multiple sclerosis MS is an immune mediated
2022-03-30

Multiple sclerosis MS is an immune-mediated disease of the human CNS with a pathological signature featuring immunocyte infiltration, altered cytokine production, oligodendroglial degeneration, astrogliosis, microglial activation, multifocal demyelination and axonal degeneration (Schipper, 2004b)
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Introduction Heme is an important small molecule and an esse
2022-03-30

Introduction Heme is an important small molecule and an essential cofactor for a variety of enzymes (George, 1948; Morrison and Stotz, 1954; Maehly, 1952; Igo et al., 1961). During cellular respiration, heme populates cytochromes and serves as an electron acceptor in the electron transport chain (M
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br Introduction Soluble guanylyl cyclase GC maintains vascul
2022-03-30

Introduction Soluble guanylyl cyclase (GC-1) maintains vascular function through the NO/GC-1/cGMP pathway [1,2] by catalyzing the conversion of GTP into cGMP (Fig. 1). The GC-1 heme prosthetic group binds NO with picomolar affinity, resulting in a 100- to 200-fold increase in catalytic activity.
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br Conclusions br Acknowledgement br Introduction The
2022-03-29

Conclusions Acknowledgement Introduction The macrophage is an important cell species that plays key roles in innate immune responses and inflammatory reactions through phagocytosis of foreign bodies and secretion of inflammatory mediators such as interleukin (IL)-1, tumor necrosis factor (T
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Aurora Kinase Inhibitor III Finally our work showed that HAA
2022-03-29

Finally, our work showed that HAART resulted in significant inter-individual variability among DEGs, which reflected the Aurora Kinase Inhibitor III in HIV-affected human gene expressions (Fig. 1, Fig. 2, Fig. 3, Fig. 4). These observations also highlighted the importance of determining common as we
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Compounds and were tested for pharmacodynamic
2022-03-29

Compounds , and were tested for pharmacodynamic effects in a mouse oral glucose tolerance test (oGTT) in wild-type and GPR120 deficient mice, and each compound demonstrated GPR120 mechanism-based effects. Data for compound is shown in , indicating mechanism-based reduction in glucose excursion a
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dillution It appears that not all GPR agonists require a hig
2022-03-29

It appears that not all GPR119 agonists require a high dose to elicit acceptable dillution control. According to preclinical data presented at the GTCbio Diabetes Summit, a 3mg/kg dose of AR-7947 was enough to induce similar blood glucose-lowering effects compared to those achieved by 30mg/kg sitag
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This data is in accordance with our
2022-03-29

This data is in accordance with our recent results on the influence of cholesterol-depleting agent methyl-β-cyclodextrin on platelets (Borisova et al., 2011a). Dissipation of the proton electrochemical gradient of secretory granules by methyl-β-cyclodextrin did not evoke the release of endogenous gl
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Previous attempts to minimize the
2022-03-29

Previous attempts to minimize the contribution of the compensatory changes due to chronic loss of Gcgr, have used temporally-controlled reduction of glucagon levels by alpha-cell ablation, glucagon immunoneutralization, and the use of small molecule or antibody glucagon receptor antagonists [10], [3
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In single channel studies Zn primarily inhibits
2022-03-29

In single channel studies, Zn2+ primarily inhibits GABA-A receptors through the reduction of channel opening probability (Smart, 1992, Smart et al., 1994). In slice recordings, Zn2+ significantly reduces phasic mIPSC event amplitude and kinetics, as well as desensitization kinetics (Barberis et al.
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G007-LK In conclusion a novel series of GPR
2022-03-29

In conclusion, a novel series of GPR40 agonists containing nitrogen heterocyclic rings derived from TAK-875 were designed and synthesized. The structural activity relationship studies indicated that the substituents on the nitrogen G007-LK had a remarkable effect on the GPR40 agonistic activity. Com
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