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A general synthesis of the tetrazole
2021-12-06

A general synthesis of the tetrazole is shown in . First, a magnesium-halogen exchange reaction quenched with DMF afforded benzo[]thiophene-5-carbaldehyde , which was further decorated with a bromine at the 3-position (). A Suzuki reaction with -tolylboronic RN 1734 synthesis followed by reduction
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Here we examined whether complete ablation of GIP
2021-12-06

Here, we examined whether complete ablation of GIP production could reduce weight gain in the absence of the adipocyte hormone leptin, a condition that results in extreme hyperphagia, obesity, hyperinsulinemia, and insulin resistance, in both mice [24] and humans [25]. We found that Lepob/ob mice be
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br Acknowledgments We apologize for the omission of
2021-12-04

Acknowledgments We apologize for the omission of primary citations owing to space limitations. This work was supported by grants from National Natural Science Foundation of China (81772801 and 81472455 to C.D.), the Key Program of Zhejiang Provincial Natural Science Foundation (LZ17H160002 to C.D
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br Acknowledgements We thank Dr Bhushan Nagar and Dr Albert
2021-12-04

Acknowledgements We thank Dr. Bhushan Nagar and Dr. Albert Berghuis for access to the X-ray diffraction machine at McGill University. We also thank Dr. Manon Couture and Dr. Steve Charette at Université Laval for access to scientific equipment. Funding for this research was provided by Discovery
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Methylcobalamin The coenzyme S adenosylmethionine SAM bindin
2021-12-04

The coenzyme S-adenosylmethionine (SAM)-binding pocket of Set7 is connected to the histone-tail binding groove by a conserved lysine-channel, similarly observed in vSET (Figures 2D and S3). The Set7 SAM-binding pocket is negatively charged as observed in other known HMTase structures. However, the b
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Ristocetin A sulfate br Conclusion GST expression was
2021-12-04

Conclusion GST expression was detected in the Hemicornea construct and the commonly used animal cornea models at both the protein and functional levels. The results are summarized in Table 1. However, the construct exhibited lower levels of activity of GST, a marker of phase II enzymatic activity
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We first set out to identify the minimum pharmacophore Early
2021-12-04

We first set out to identify the minimum pharmacophore. Early structure activity relationships (SAR) indicated that the chloro substituents were not required and that the benzisoxazole moiety could be replaced by a number of other groups. A broad survey of “left-hand” hydrophobic moieties was conduc
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In order to elucidate the mechanisms behind the observed
2021-12-04

In order to elucidate the mechanisms behind the observed changes in metabolic activity in the cardiomyoblasts we investigated changes in gene and protein expression subsequent to treatment with PSN632408 with or without concurrent exposure to palmitate. Activating GPR119 in basal and high palmitate
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br Membrane transporters as a novel therapeutic target in
2021-12-03

Membrane transporters as a novel therapeutic target in pediatric TBI The concept of targeting membrane transporters began with identifying a neuroprotective drug and a corresponding transporter inhibitor. Somewhat serendipitously, we discovered that N-acetylcysteine (NAC), a cysteine donor for GS
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In addition to the increase of extracellular glutamate ICH
2021-12-03

In addition to the increase of extracellular glutamate, ICH can also increase the levels of reactive oxygen species (ROS) and oxidative stress. Although the products of red blood cell lysis and plasma components, as well as the excitotoxic effect of glutamate have been to increase oxidative damage (
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br Acknowledgements This work was supported by the
2021-12-03

Acknowledgements This work was supported by the Science and Technology Department of Hubei Province (No.2016CFB368) and the National Natural Science Foundation of China (No. 81201053). Introduction L-Glutamate (glutamate) is the most important excitatory neurotransmitter of the central nervou
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br Conclusion Infections caused by the P aeruginosa could no
2021-12-03

Conclusion Infections caused by the P. aeruginosa could not be cured by current antibiotics, making multiple drug resistance of P. aeruginosa an increasing threat for human lives. Looking for a new therapeutic mechanism for infections caused by the P. aeruginosa has become a central issue. There
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The first suggestion that the
2021-12-03

The first suggestion that the Hh pathway might be involved in the pathogenesis of chronic liver disease was reported at the beginning of this millennium by Shackel et al. who noted that Patch and Gli were upregulated in their microarray analysis of liver tissues from patients with primary biliary ch
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The RAS RAF MEK ERK pathway is a central
2021-12-03

The RAS/RAF/MEK/ERK pathway is a central controller of cell proliferation and survival and, consequently, alterations to some of its components lead to hyperactivation of the pathway, an event related to numerous types of cancer [172]. High rates of alterations to this pathway are found in leukemia,
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It is interesting to note that the long
2021-12-02

It is interesting to note that the long and short forms of GPR120 exist at different basal levels of phosphorylation, with the short form demonstrating a greater degree of constitutive activity [12]. Importantly, Burns and Moniri [12] showed that, upon activation, the long and short isoforms of GPR1
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