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Obesity is one of the worldwide concerns
2022-02-11

Obesity is one of the worldwide concerns, with high prevalence and adverse effects on human health and life expectancy. According to the World Health Organization (WHO), obesity is defined as abnormal or excessive fat accumulation in the body with body mass index (BMI) of 30 or more. Obesity increas
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It should be noted that
2022-02-11

It should be noted that one of the two phenyl groups of 15 is found in the main western pocket and the second phenyl group occupies the western secondary pocket (Ser53, Leu54, and Leu213). The nitrogen of the amide bond is involved in a hydrogen bonding interaction with Asp140. The alcoholic functio
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br Introduction Nicotinic acid has been used
2022-02-11

Introduction Nicotinic 4 hydroxytamoxifen has been used clinically for more than 50 years [1] since it has anti-atherogenic effects, including the ability to reduce triglyceride (TG) and low-density lipoprotein cholesterol (LDL-C), and elevate high-density lipoprotein cholesterol (HDL-C) [2]. Ni
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Acknowledgments We would like to thank
2022-02-11

Acknowledgments We would like to thank Dr. Greg Morriello, Mr. Lehua Chang, Mr. Chris Moyes and Mr. Nam Fung Kar for intermediate 3 syntheses. Cheng Zhu would like to thank Dr. Milana Maletic, Mr. Kake Zhao and Mrs. Wanying Sun for helpful discussions. Introduction Glucagon-like peptide-1 (GLP-
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Previously we have shown that
2022-02-11

Previously, we have shown that rapid action of E2in vitro is mediated through two E2 membrane receptors, GPR30 (GPER1) and the STX-sensitive membrane receptors (Noel et al., 2008; Kenealy et al., 2011a, Kenealy et al., 2011b). This is significantly different from receptors implicated in the positive
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Introduction The hypoglossal nucleus is
2022-02-11

Introduction The hypoglossal nucleus is the nucleus of the twelfth cranial nerve and is located on both sides of the mid line in the dorsal medulla oblongata and is situated between the proximal end of the medullary central canal and the beginning of the fourth ventricle (Tomasch and Etemadi, 1962)
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Here we report the first attempts to assess roles
2022-02-11

Here we report the first attempts to assess roles of NTs and ABC transporters in transfer of ribavirin across the placental barrier using human placental villous fragments and microvillous plasma membrane (MVM) vesicles, in situ dually perfused rat term placenta, and cell-based models. Materials
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In the spinal cord EAAT constitutes of all high
2022-02-11

In the spinal cord, EAAT1 constitutes 40% of all high-affinity EAATs, and it is abundantly present in lumbar dorsal horn (Queen et al., 2007). In physiological conditions, EAATs remove glutamate from the synaptic cleft by co-transporting glutamate and sodium into adjacent glial cells. The inefficien
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Because sleep and metabolism are intimately linked the
2022-02-11

Because sleep and metabolism are intimately linked, the authors next move to study whether Eaat2 also controls metabolic rate. First, we must ask how sleep and metabolism are connected at a functional level. The NG,NG-dimethyl-L-Arginine hydrochloride allocation hypothesis of sleep posits that organ
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In respect of clinical development Takeda
2022-02-11

In respect of clinical development Takeda has pioneered the field with the GPR40 agonist TAK-875 or fasiglifam (Figure 2A), which in phase-II studies decreased HbA1c as efficiently as sulfonylurea without signs of hypoglycemia [24]. This was obtained with surprisingly little effect on systemic insul
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The molecular identity of RA
2022-02-11

The molecular identity of RA’s target during LTP induction was determined by pharmacological testing. The inhibitory effects of CNQX and niflumic acid on LTP induction remained even in the presence of RA, indicating RA did not affect either the AMPA receptor nor chloride channel (Fig. 2B and D) [26]
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PKI-402 Nuclear export of GK has been reported to
2022-02-11

Nuclear export of GK has been reported to be dependent on a GK nuclear export signal (NES), mapped to residues 300–310 (Shiota et al., 1999). The assignment of a nuclear export signal common to both the liver and pancreatic GK isoform sequence suggests a possible reversible translocation of GK acros
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GCK MODY is the most common
2022-02-11

GCK-MODY is the most common form of MODY diabetes in many populations (Chevre et al., 1998; Massa et al., 2001; Barrio et al., 2002; Estalella et al., 2007; Pruhova et al., 2010; Capuano et al., 2012; Giuffrida et al., 2017). However, data about GCK-MODY among North African populations are very rare
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Growing evidence supporting the anti inflammatory and tissue
2022-02-10

Growing evidence supporting the anti-inflammatory and tissue-protective effects of FPR antagonists led to the screening of commercial libraries for novel small-molecule FPR antagonists. As result of these screening efforts and/or structure–activity relationship (SAR)-directed design and synthesis, a
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The precise mechanism by which erastin
2022-02-10

The precise mechanism by which erastin inhibits SLC7A11-mediated cystine import it still unknown. The initially proposed mechanism, by which erastin binds a related transport protein, SLC7A5, and inhibits SLC7A11 in trans [25], was revised soon after, and it was suggested that erastin inhibits SLC7A
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