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br Mechanisms of action Ghrelin
2022-02-12
Mechanisms of action Ghrelin is a 28-amino Albendazole peptide hormone primarily produced in the oxyntic mucosa of stomach, but also in other gastrointestinal tissues [7] (Fig. 1). It acts as the endogenous ligand for the ghrelin receptor [GHS-R1a] and causes the release of growth hormone from t
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Recent studies have elucidated a profound role for FFA in
2022-02-12
Recent studies have elucidated a profound role for FFA4 in modulation of metabolism and energy utilization as well as endocrine and immune function, and as a consequence, have thrust FFA4 to the forefront of drug discovery efforts. For example, activation of FFA4 by fatty Nicotinamide or synthetic
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br Conclusions GPCRs are versatile signaling molecules regul
2022-02-12
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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Tail group SAR of the imidazole derived analogs is
2022-02-12
Tail group SAR of the imidazole derived analogs is shown in . The previous SAR study from the discovery of AMG 837 revealed that a simple un-substituted meta-biphenyl tail group was less favorable in terms of potency. Efforts to introduce polarity to the tail group were not successful. When a methyl
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br Experimental procedures br Results br Discussion The data
2022-02-11
Experimental procedures Results Discussion The data herein confirm the well documented neuroinflammatory effect of TLR3 activation following systemic administration of the viral mimetic poly I:C and the associated acute sickness response which includes fever, reduced body weight and allodyn
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br Application of TIRFM to visualizing
2022-02-11
Application of TIRFM to visualizing exocytosis TIRFM was first used to visualize exocytosis from large secretory granules from chromaffin Sorbitol (Steyer et al., 1997). Before that, visualization of secretory organelle was strictly limited to a few exceptions, such as mast cell of mutant mice,
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loteprednol etabonate synthesis Compounds and were evaluated
2022-02-11
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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br Discussion Considering cardiovascular risk factors
2022-02-11
Discussion Considering cardiovascular risk factors, there was a significant difference in prevalence of dyslipidemia in both groups, 57.5% in HIV-infected stroke patients compared to 8.9% in the HIV-uninfected patients. These results are similar to that of Chow et al. who found a dyslipidemia pre
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To validate the effects of the G
2022-02-11
To validate the effects of the G9a HMT inhibitors on HMEC-1 Alfacalcidol and transcriptional responses we generated knockdown cells for G9a using an shRNA approach. Upon transduction of HMEC-1 and doxycycline activation of the shRNA, both G9a HMT mRNA and protein expression were effectively decreas
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br Introduction Lysine acetylation is
2022-02-11
Introduction Lysine acetylation is an important post-translational modification that is found on numerous cellular proteins, including both histone and non-histone proteins [1], [2]. Dynamic acetylation and deacetylation is regulated by enzymes called histone acetyltransferases (HATs) as writers
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VDAC interacts with hexokinase and is implicated in NLRP
2022-02-11
VDAC interacts with hexokinase and is implicated in NLRP3 activation in response to noxious stimuli including monosodium urate, silica, and alum (Zhou et al., 2011). Hexokinase dissociation may allow VDAC to carry out this role. It will be informative to block or silence VDAC to explore its function
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br Introduction Circulating tumor cells CTCs
2022-02-11
Introduction Circulating tumor scopolamine hydrobromide (CTCs) are cancer cells that have invaded blood vessels or lymphatics and are carried around the body by the blood. CTCs constitute potential seeds for metastasis because they can reach and implant into distant organs. The clinical importan
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br Mechanisms of HDAC inhibition dependent cardioprotection
2022-02-11
Mechanisms of HDAC inhibition-dependent cardioprotection Multiple preclinical studies have demonstrated potent cardioprotective benefits of HDAC inhibition in murine models of myocardial stress, including I/R [19,25,29,30]. TSA reduces myocardial infarct size by up to 50% [19,25]. In addition, tr
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Urinary As species monomethylated MMAV percentage might
2022-02-11
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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Receptor guanylyl cyclases play essential roles
2022-02-11
Receptor guanylyl cyclases play essential roles in cardiovascular and gastrointestinal (patho-)physiology, reproduction biology, cell proliferation, bone growth and sensory signal transduction and, therefore, are important pharmacological targets. Accordingly, the receptor guanylyl cyclase agonists
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