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Molecular properties as well as metabolic
2021-10-12

Molecular properties as well as metabolic stability in rat and human liver microsomes for the most active nitro (), nitrile (), methylsulfone (), and sulfonamides () analogues were measured (). All these derivatives possessed excellent membrane permeability as measured in the Pampa assay and further
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An increased sympathetic tone and the hormone
2021-10-12

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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br Acknowledgements This work was supported
2021-10-12

Acknowledgements This work was supported by the grants from National key Basic Research Program of China (2012CB124702), 948 Program (2015-Z33), National Natural Science Foundation of China (31172093, 31301947), the National Science Foundation for Fostering Talents in Basic Research (J1103510), S
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neostigmine bromide br Drug design Over the
2021-10-11

Drug design Over the past decades, the development of synthetic, direct fXa inhibitors has undergone four phase. Although these fXa inhibitors possess various scaffolds, most of them bind to the active site in a characteristic l-shaped conformation. In other word, they have a three-component syst
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In neurons and neuroendocrine cells the
2021-10-11

In neurons and neuroendocrine cells, the productive fusion pathway is thought to initiate with the Munc18-1/Syx1 complex (Ma et al., 2013, Hughson, 2013, Lai et al., 2017). The Munc13-1 MUN domain is able to catalyze opening of Syx1 (the transition from the Munc18-1/Syx1 complex to the SNARE complex
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We have expanded these studies by doing EEG recording in
2021-10-11

We have expanded these studies by doing EEG recording in the ET-1 model. Using this technique, we demonstrated that activation of either the ETA ESI-09 or the ETB receptor induces electrical seizures. ET-1 induced electrical seizures occurred in the presence of either the ETA receptor antagonist or
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In our study we found that HER mutant lung
2021-10-11

In our study, we found that HER2-mutant lung cancers occurred commonly in female patients with an advanced stage at time of diagnosis and in a relatively younger age group. Previously, Mazières et al. [8] obtained comparable epidemiological findings, including a median age of 60 years, a high propor
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Measured physicochemical water parameters including conducti
2021-10-11

Measured physicochemical water parameters including conductivity, suspended solids and nutrient load along the studied sites (Table 1) were high compared to levels usually found in undisturbed rivers within Europe (Chapman and Kimstach, 1996). In particular conductivity, suspended solids and phospha
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366 2 Our study expands our current knowledge of Ras like
2021-10-11

Our study expands our current knowledge of Ras-like small GTPase molecules involved in TLR-mediated responses in macrophages. We found that steady-state levels of Rap2a mRNA and protein undergo alterations after stimuli with TLR agonists. Although statistically significant, the effect of LPS-induced
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br Discussion Regulation of redox
2021-10-11

Discussion Regulation of redox homeostasis is critical in the maintenance of normal cell functions, and both glutathione S-transferase and peroxiredoxin enzymes are important contributors to this process. There are numerous reports of aberrant expression patterns of GSTP linked with cancer and wi
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Conflict of Interest The authors have no
2021-10-11

Conflict of Interest: The authors have no conflicts of interest to declare. Acknowledgments Understanding Pulmonary Remodeling The effects of serotonin (5-hydroxytryptamine, 5-HT) class 2 receptors (5-HT2) on airway function and remodeling in respiratory disorders are unclear. Using murine pr
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br STAR Methods br Introduction Glycosylation is
2021-10-11

STAR★Methods Introduction Glycosylation is one of the most prevalent post-translational modifications of proteins. It not only plays major roles in folding, transport and localization of proteins [1], but also regulates various biological processes such as cell growth, viral replication and im
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We noticed that the spontaneous openings of the D R
2021-10-11

We noticed that the spontaneous openings of the D97R α1 GlyR appeared to be quite similar to those elicited by a maximally-effective glycine concentration on wildtype GlyR; both generated similar open and shut dwell-time histograms, both exhibited openings grouped into clusters with Popen values gre
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br Methods br Results br
2021-10-11

Methods Results Discussion Previous work by the Hirano group investigated the effect of GIP in murine atherosclerotic models and found infusion of GIP (1–42) by osmotic mini-pumps to decrease lesion size after 4 weeks in non-diabetic as well as in diabetic ApoE−/− mice [8], [9]. Mechanistic
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br Materials and methods br
2021-10-11

Materials and methods Results Discussion Several peripheral hormones that are involved in the central regulation of energy homeostasis, such as leptin, insulin, and amylin [34], [35], [36], [37], [38], cross the BBB by saturable and unsaturable mechanisms. Whether these transport processes
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