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Due to the high structural similarity between GlxI
2021-09-29
Due to the high structural similarity between GlxI and FosA, it is possible that GlxI directed evolution experiments could produce FosA enzymatic activity in a GlxI enzyme. Although the current investigation was unable to detect FosA activity by mutation of a key metal liganding residue in the activ
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The neuronal glycine receptor HSOR allopregnanolone pathway
2021-09-29
The neuronal glycine receptor/3α-HSOR/allopregnanolone pathway may also be extended to the central nervous effects of gelsemine and koumine in brain. 3α-HSOR is expressed in certain brain regions in rats and humans, such as the limbic system including hypothalamus, hippocampus and amygdala, in addit
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Ketamine has recently been found to exert rapid and
2021-09-29
Ketamine has recently been found to exert rapid and sustained antidepressant effect. Single dose ketamine can have an efficacy of up to 1 week [20]. Furthermore, ketamine is an effective drug against refractory depression [21,22]. The antidepressant mechanism of ketamine is still unclear. Whether CO
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Heart failure affects approximately million people over
2021-09-29
Heart failure affects approximately 6.5 million people over 20 years of age in the United States, with its prevalence estimated to increase about 45% by 2030 to almost 8 million . It is a chronic disease with complex etiology and heterogeneity in its pathological manifestations. Major risk factors f
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The regulation of casein expression during lactation is
2021-09-29
The regulation of casein expression during lactation is a complex process involving a coordinated response at several levels. A variety of hormones are known to play roles in lactogenesis, such as prolactin (PRL), insulin, and hydrocortisone, and there is now increasing evidence that growth factors,
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Introduction Parkinson s Disease PD is a
2021-09-29
Introduction Parkinson's Disease (PD) is a neurodegenerative disease affecting approximately 5–6 million individuals worldwide [1]. This number is expected to escalate to ∼10 million by the year 2030 as the world's population rapidly ages [2]. In the United States, more than 1 million individuals h
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In this study we saw
2021-09-28
In this study, we saw change in GHS-R1a mRNA expression in fasting condition. It is noteworthy that changes in ghrelin and GHS-R1a mRNA expression synchronized in organs were examined. In the HTH-01-015 sale and pituitary, gene expression increased 4days after fasting, and the increased level declin
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The Cx family of integral
2021-09-28
The Cx family of integral membrane proteins [13] are key components of the Gap Junction channels that provide GJIC, which is indispensable in the preservation of tissue integrity and homeostasis in multicellular organisms. Gap Junction channels form a conduit for exchange of ions (Ca2+), second mess
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br Gamma secretase trafficking GS activity
2021-09-28
Gamma-secretase trafficking GS activity for APP can be influenced by sub-cellular trafficking, as APP cleavage differs depending on its localization. APP is synthesized in the ER and transported to the trans-Golgi network (Annaert et al., 1999, Pasternak et al., 2003, Ray et al., 1999a, Rechards
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The pharmacokinetic properties of were amenable to oral dosi
2021-09-28
The pharmacokinetic properties of 12 were amenable to oral dosing allowing in vivo comparison to 6. Compared to a maximum efficacious dose of 6 (60mg/kg), 12 demonstrated improved glycemic control during OGTT in high-fat fed/STZ treated (HF/STZ) and BDF/diet-induced obesity (DIO) mouse models of typ
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Arena Pharmaceutical introduced a biaryl sulfone derivative
2021-09-28
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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The synthesis of target compound RS
2021-09-28
The synthesis of target compound (RS)-C02 is illustrated as Scheme 2. Compound (RS)-3 was synthesized as reported procedures [40] and then reacted with ethyl piperidine-4-carboxylate to yield (RS)-C01, which subsequently was converted to target molecule (RS)-C02 by performing a nucleophilic substitu
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There are five main research findings
2021-09-28
There are five main research findings regarding possible mechanisms of low-level HBsAg expression: Most of these findings are related to the use of antiviral therapy, which results in pre-S/S gene mutations, the development of occult hepatitis, the use of immunosuppressants or S gene methylation, b
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Over the last few years experimental evidence for
2021-09-28
Over the last few years, experimental evidence for the involvement of Epac1 in cancer progression is beginning to emerge (Almahariq et al., 2015, Banerjee and Cheng, 2015, Parnell et al., 2015, Parnell et al., 2015, Schmidt et al., 2013). For example in melanoma cells, silencing of Epac1 attenuates
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A number of in vivo studies
2021-09-28
A number of in vivo studies have investigated the antitumor activity of distinct GSK-3 inhibitors in a variety of cancer cell line-derived tumor xenograft models [14], [21], [22], [24], [33], [39], [40]. These studies utilized toolkit GSK-3 inhibitors as monotherapies. Although inhibition of tumor g
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