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br GLP R expression in the
2022-04-01

GLP-1R expression in the vascular endothelium Immunohistochemistry studies utilizing GLP-1R antibodies that have now been demonstrated to be non-specific [46], initially identified GLP-1R protein expression in both mouse mesenteric artery SMCs and heart coronary SMCs [7]. However, evidence for VS
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The novel Ghsr IRES Cre knock
2022-04-01

The novel Ghsr-IRES-Cre knock-in mouse line allowed us to deconstruct the involvement of MBH GHSR-expressing neurons in mediating food intake responses using chemogenetic modulation of their neuronal activity. In our studies, hM4Di DREADD virus injections to inhibit GHSR neurons targeted several nuc
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br Fipronil resistance associated with A
2022-04-01

Fipronil resistance associated with A2′S and A2′G mutations Fipronil is a second-generation NCA (Fig. 1), and A2′S and A2′G mutations provide a low level of cross-resistance to fipronil (Cole et al., 1995, Gao et al., 2007). As shown in Table 1, the A2′S GSK343 mg confers high resistance to dield
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br The Farnesoid X receptor FXR identification
2022-04-01

The Farnesoid X receptor (FXR): identification and ligands The Farnesoid X receptor (FXR) belongs to a family of proteins called Nuclear Receptors (NRs). NRs are a class of ligand-activated transcription factors, which transactivate networks of target genes, thereby mediating a wide range of phys
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The pharmacokinetic properties of were amenable to oral dosi
2022-04-01

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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Till date the first line treatment of T DM is
2022-04-01

Till date, the first line treatment of T2DM is oral metformin followed by oral sulfonylureas, dipeptidyl peptidase-IV-inhibitors, and TZDs. As the disease progresses, injectable glucagon-like peptide-I analogues or ultimately insulin become necessary to maintain glycaemic control. Despite the establ
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Wnt-C59 The suboptimal trypsin selectivity profile of
2022-04-01

The suboptimal trypsin selectivity profile of DPC423 prompted us to investigate additional P moieties for potency and selectivity. Glycinamide P () showed low nanomolar binding affinity against fXa which suggested that this P moiety sits deeper into the S pocket of fXa. To further elaborate on this
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Several observations about structure activity
2022-04-01

Several observations about structure–activity relationships can be made from this series, including that: (1) all lead compounds are NSAIDs of the 2-arylpropionic Cy5.5 carboxylic acid (non-sulfonated) sale class, (2) analogues with -oriented aryl substituents showed the best inhibition of FAAH, an
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It is well established that transcription
2022-04-01

It is well established that transcription factors are the major key players in regulating the transcriptional state of the targeted gene. 15 TFs were found in the present study, which were predicted to have the binding affinity with the EZH2 promoter region. Out of these, GCF, AP-2 and Sp1 were most
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Compounds and were evaluated for their pharmacokinetic
2022-04-01

Compounds and were evaluated for their pharmacokinetic properties in rats and the results are summarized in . Following intravenous (IV) administration, both compounds displayed low clearance (CL), short half-lives (t) and low volumes of distribution (V). When dosed orally as a solution, exposure
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In the present study we investigated
2022-03-31

In the present study, we investigated the mechanisms underlying the ability of 5-FU to modify histone acetylation. Our results suggested that 5-FU induces global histone de-acetylation in CRC by promoting the degradation of p300 and CBP, two important homologous HATs catalyzing acetylation at multip
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Although histamine can induce both proliferation and
2022-03-31

Although histamine can induce both proliferation and differentiation in vitro (Molina-Hernandez and Velasco, 2008), the promotion of neurogenesis conferred by H3R antagonism here does not seem to be caused by either the proliferation or the reduction of apoptosis of NSCs (Figure S3). Furthermore, H3
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In this study there is a
2022-03-31

In this study, there is a limitation in the study of sex differences. Only female rats were used in our study. This is because the rats cannot urinate autonomously after SCI. Manual ARCA synthesis emptying was needed until reflex bladder emptying was established (Lu et al., 2008, Ma et al., 2015).
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The transcription factor Nrf is a master
2022-03-31

The transcription factor Nrf2 is a master regulator of cytoprotective responses to endogenous and exogenous stresses caused by reactive oxygen species (ROS) and electrophiles [6]. Nrf2 promoter polymorphisms are significantly associated with the development of gastric mucosal inflammation, either in
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Galanthamine HBr br Conclusion The following is the suppleme
2022-03-31

Conclusion The following is the supplementary data related to this article. Conflict of interest Author contributions Heart transplantation is the most important treatment for end-stage heart failure. Ischemia/reperfusion injury is a common condition during transplantation surgery and is
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