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Recent studies in our laboratory demonstrated that several h
2021-12-24

Recent studies in our laboratory demonstrated that several histamine H1 receptor antagonists induce apo A-I gene expression while histamine itself represses it [20]. In humans, there are three histamine receptor genes (H1, H2, and H3) that code for G-protein-coupled receptors (GPCR's) which bind his
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Most studies of HIF have focused on its
2021-12-24

Most studies of HIF-1α have focused on its transcriptional activity-dependent functions. However, our results indicate that the oxidative stress-related effects of mtHIF-1α occur independently of its translocation to the nucleus and do not require its transcriptional activity. In fact, several stud
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br cAMP cGMP effector systems in human
2021-12-24

cAMP/cGMP effector systems in human platelets (PKA, PKG, PDEs) In eukaryotic cells, the effects of intracellular cAMP are mediated by two types of cAMP-dependent protein kinases (PKA type I and II) and cAMP-regulated guanine nucleotide exchange factors (EPAC/cAMP-GEF) which activate the RAS GTPas
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Firstly the impact on activity and
2021-12-24

Firstly, the impact on activity and selectivity was made by replacing the 2, 3-di-F substitution of ring A with 2,3-OCHO- () and 2-NO () substitutions, and replacing the 3, 5-di-F substitution of ring B with 3,5-di-OMe () and 3,5-di-Me () substitutions. Compound kept moderate activity (EC = 220 nM)
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In this study we find that DH CBD induces analgesic
2021-12-24

In this study, we find that DH-CBD induces analgesic effects on inflammatory but not acute pain and the bepridil level of spinal α1 GlyRs increased after CFA paw injection. These results suggest that GlyR α1 is only involved in chronic pain. A possible explanation is that once the expression of α1
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ap-1 transcription factor The neurobiological mechanisms und
2021-12-24

The neurobiological mechanisms underlying DHK-induced NOR learning and memory impairments remain unclear. Accumulated evidence shows that astrocyte-neuron lactate shuttle is of crucial important in synaptic plasticity and memory formation, and regulation of neuronal gene expression related to synapt
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In this study we present the synthesis and structure
2021-12-24

In this study, we present the synthesis and structure–activity studies of a structurally distinct series possessing high potency and selectivity in HEK cell lines together with a potentially promising overall biopharmacological profile. Focusing on creating sufficient structural dissimilarity with g
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br Mechanisms of gap junction internalization
2021-12-24

Mechanisms of gap junction internalization: disaggregation, endocytosis and annular gap junctions It has been clearly shown that gap junction internalization can occur by a distinctive mechanism where one cell internalizes an entire gap junction via formation of double membrane structure termed a
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The sexual dimorphism in dlGALR a and
2021-12-24

The sexual dimorphism in dlGALR1a and dlGALR1b receptors found in the gonads of adult fish led us to hypothesize that the gene expression difference between female and males might be attributed to the differences in steroid production between female and male gonads. Interestingly we have found that
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Introduction galactosidase d galactoside galactohydrolase or
2021-12-23

Introduction β-galactosidase (β-d-galactoside galactohydrolase or lactase; EC 3.2.1.23) is an important type of glycoside hydrolase that can catalyze the conversion of lactose to 1-NM-PP1 and galactose. Furthermore, it can also catalyze transglycosylation reactions, which are usually used for the s
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However T DM and associated hyperglycemia
2021-12-23

However, T1DM and associated hyperglycemia can adversely affect the structure and function of the heart in several mechanisms including inhibiting the anabolic effect of insulin due to its deficiency, generation of higher levels of ROS and induction of lipid peroxidation, and subsequent activation o
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br Cellular transportation of nanoparticles and nanocomplexe
2021-12-23

Cellular transportation of nanoparticles and nanocomplexes Endocytosis and exocytosis are critically important phenomena in cellular metabolism, which involve the complex vesicular system. They deal with major cellular transportation activities including membrane homeostasis by transporting prote
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br Mechanisms of HDAC inhibition dependent cardioprotection
2021-12-23

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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According to literature RASs V M
2021-12-23

According to literature, RASs V36M, T54S, Q80K and R155K are considered primary resistance mutations to different PIs. RASs V36M and R155K can reduce susceptibility to recently approved PIs simeprevir, paritaprevir and grazoprevir [18], [31], [32]. T54S is associated to resistance for first-wave tel
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br Other Functions of HCA Receptors
2021-12-23

Other Functions of HCA Receptors HCA receptors, in particular HCA1, are expressed in various primary tumor description 77, 78, 79. This is of interest, as most solid tumors show increased glucose uptake and lactate formation even under normoxic conditions, with lactate concentrations in the tumor
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