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br Gastrointestinal peptides and intestinal health Gastroint
2022-01-20
Gastrointestinal peptides and intestinal health Gastrointestinal peptides are intimately involved in the regulation of feeding behaviors, energy metabolism and bodyweight 36, 37, 38, 39, 40, 41. GPR120 has been demonstrated to induce secretion of two such peptides: GLP-1 and cholecystokinin (CCK)
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With this goal in mind we proceeded
2022-01-20
With this goal in mind, we proceeded to explore the C5-heteroaryl class of pyrazole-acids. Initial efforts, focused on a thiophene replacement, demonstrated little improvement. The 2-thiophene derivative (0.25μM and 0.24μM), a surrogate to the phenyl moiety, demonstrated only a modest boost in acti
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The global spread and ever
2022-01-20
The global spread and ever-increasing incidence of metabolic syndrome over the past few decades has not only categorized it as an ‘epidemic’ but has also dramatically increased the risk of cardiovascular diseases and diabetes. The increase in prevalence of diabetes in the United States alone has bee
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Crystal structure of CD LEL have
2022-01-20
Crystal structure of CD81-LEL have revealed the head sub-domain to be implicated in binding to HCV (Kitadokoro et al., 2001). In a study using African green monkey CD81, T163A, F186 L, E188K and D196E mutations disrupted HCV E2 binding (Higginbottom et al., 2000). In our docking studies, T163 and D1
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br Discussion Agonist and antagonist action at the GluN GluN
2022-01-20
Discussion Agonist and antagonist action at the GluN1/GluN3 CAY10603 is known to be complex [4], [10]. Recombinant GluN1/GluN3 receptors produce only small excitatory currents in response to glycine, likely because of a combination of activation via GluN3 and desensitization via GluN1 [2], [3],
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An increased sympathetic tone and the hormone glucagon are t
2022-01-20
An increased sympathetic tone and the hormone glucagon are the main glucose mobilizing factors [28], [29]. Single-cell transcriptome analysis of human islet cells suggests the expression of Ffar1 not only in β-cells but also in α-cells [30]. Moreover, analysis of rat α-cells indicates that FFAR1 exp
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Determination of enzyme activity differs from other analytic
2022-01-20
Determination of enzyme activity differs from other analytical procedures. In this 4-P-PDOT case , instead of enzyme concentration, a substrate depletion or product accumulation should be monitored. Such approach allows calculating activity basis of calibration curves performed for enzymatic reactio
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Factor Xa FXa has emerged as a particularly
2022-01-20
Factor Xa (FXa) has emerged as a particularly promising target for the development of effective anticoagulant drugs because FXa acts at the convergence point of the extrinsic and intrinsic coagulation pathways. It efficiently catalyzes the conversion of prothrombin to thrombin with one molecule of F
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YK-4-279 We also evaluated the effect
2022-01-20
We also evaluated the effect of varying ionic strength. These experiments included previously characterized H3 (residues 1–21) and SNAIL (residues 1–9) peptides [8], [34] to allow a comparative analysis with different ligands (Fig. 1A). As shown in Fig. 2 and listed in Table 2, it is evident that a
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br Introduction Glycolysis plays a
2022-01-20
Introduction Glycolysis plays a key role in c di gmp energy metabolism [[1], [2], [3]]. It is initiated mainly by hexokinase I (HKI), the major hexokinase isoform of the brain ([3,4] and references therein). Up to 90% of brain HKI is bound to the mitochondrial outer membrane (MOM) through the vol
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br Heme oxygenase inhibitors Historically the first class of
2022-01-20
Heme oxygenase-1 inhibitors Historically, the first class of competitive HO-1 inhibitors was represented by MPs, heme analogs in which the central iron GSK 2830371 of heme is exchanged by another element, such as zinc, cobalt, tin, or chromium. These molecules compete with heme for binding to th
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Oxamic acid The overall characteristic of RNA profile of Ley
2022-01-20
The overall characteristic of RNA profile of Leydig cell is still a mystery. Variation in total RNA will cause subsequent difference in protein expression and phenotypic modulation [16]. In this study, we used a murine nicotine exposure model coupled with next generation RNA sequencing (NGS) and fou
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L-Adrenaline Apo E is defined as a polym http
2022-01-19
Apo E is defined as a polymorphic protein arising from three alleles. The human Apo E gene was widely studied and described to be located on chromosome 19, closely linked to the Apo C-I/C-II gene complex [9]. The three major alleles, termed Epsilon-2, Epsilon-3 and Epsilon-4 have been reported [10].
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dpni Compared to methadone or morphine buprenorphine is
2022-01-19
Compared to methadone or morphine, buprenorphine is a partial mu-opioid agonist, which shows high affinity for, and slow dissociation from, mu-opioid receptors. This maintenance of homeostasis may help to counter the development of an overt withdrawal syndrome, and may explain the lower risk of deve
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In three groups independently proposed two different
2022-01-19
In 2001, three groups independently proposed two different mechanisms for the catalytic reaction of GlxI [5], [6], [7]. Richter and Krauss (RK) used HF/4–31G calculations of the active site, coupled with a frozen effective fragment potential description [8], [9] of eleven residues in the binding sit
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