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Epinephrine responses to hypoglycemia are probably triggered
2022-07-25

Epinephrine responses to hypoglycemia are probably triggered centrally, perhaps with input from peripheral hypoglycemia sensing [3], [4]. We observed increased epinephrine responses in GCK-MODY and I366F diabetic mice. Consistent with a role for osi sc 175 GCK in detecting a low blood glucose, we a
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Extensive pharmacological and structural analysis
2022-07-25

Extensive pharmacological and structural analysis shows GCGR antibody REMD-477 competitively blocks GLC binding to the GCGR with 30-pM binding affinity, and can fully inhibit the receptor activity at low nanomolar concentrations in ARRY334543 14, 17, 20. Functionally identical to REMD-477, REMD2.59
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Attempting to further elucidate the role
2022-07-25

Attempting to further elucidate the role of amphetamine sulfate receptor and activation of the Gcgr without the influence of GLP-1, we used DT-Gcg mice with acute knockdown of all proglucagon products. This mouse model has previously been shown previously to have a normal total islet area as well a
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So far several methods have been
2022-07-25

So far, several methods have been used to monitor the level of GJC and its regulation in astrocytes studied in acute N-acetyl D-galactosamine slices (see Giaume et al., 2012). This mainly includes approaches based either on electrophysiological properties of gap junction channels or on “dye coupling
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Initially we carried out gap FRAP experiments using the two
2022-07-25

Initially, we carried out gap-FRAP experiments using the two-photon configuration of the confocal microscope. A SR101-positive astrocyte was targeted and a 5 × 5 μm square area was exposed to a laser illumination (5 flashes of 5 s each during 25 s). This procedure resulted in a bleaching of this ast
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The orientation of the immobilized enzyme may
2022-07-25

The orientation of the immobilized enzyme may affect its activity and stability and therefore the final biocatalyst performance. Since proteins present areas more prone to unfolding in their surface or near to it [36], the immobilization through these areas may improve the final biocatalyst stabilit
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We have isolated various bioactive peptides acting by bindin
2022-07-22

We have isolated various bioactive Floxuridine acting by binding to the receptors of endogenous bioactive peptides such as opioid, bradykinin, neurotensin, and complements C3a and C5a etc. [24]. Rubimetide is the first example of an agonist peptide of the FPR2 of exogenous origin. Anxiolytic-like a
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All of the abovementioned effects of PUFAs signal their invo
2022-07-22

All of the abovementioned effects of PUFAs signal their involvement in a cellular phenotype switching phenomenon, which is increasingly recognized as a potential target for future pharmacotherapies of atherosclerosis, especially for individuals who do not respond to the classical lipid-lowering stra
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In the previous paper we
2022-07-22

In the previous paper, we described the design and synthesis of tricyclic thiazoles as FBPase inhibitors, and a series of SAR studies led to the identification of phosphate 3 and difluoromethylenephosphonate 4 exhibiting potent FBPase inhibitory activities (IC50=13, 47nM, respectively) (Fig. 2). In
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Next we were interested in replacing the ketobenzimidazole
2022-07-22

Next, we were interested in replacing the ketobenzimidazole fragment of our inhibitors with a noncarbonyl bearing heterocycle. We reasoned that if we could replace the carbonyl while maintaining comparable FAAH inhibition, it would provide evidence for a noncovalent mechanism of action. Thus, we eva
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Introduction Human immunodeficiency virus HIV persue to be
2022-07-22

Introduction Human immunodeficiency Fluticasone propionate (HIV) persue to be a major global public health problem (Joint United Nations Programme on HIV/AIDS, 2018). Globally, 36.9 million (range, 31.1 million–43.9 million) people were living with HIV in 2017 (UNAIDS, 2018a). The burden of the epi
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The possibility of having false
2022-07-22

The possibility of having false positives, even if minimized, is always present and requires that a reactive result should be followed by a confirmation test. Traditionally, Western blot (WB) has been used, but various types of immunoblotting that use recombinant Hydroxysafflor yellow A or syntheti
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Oxaliplatin br Conclusion Whilst acknowledging that forensic
2022-07-22

Conclusion Whilst acknowledging that forensic science critically needs strategic investment across every domain [27], forensic science needs to bring both ‘hedgehog’ and ‘fox’ approaches together to address the roots of the major challenges the discipline faces. Addressing these challenges in a w
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Our results show furthermore that higher concentrations of
2022-07-22

Our results show furthermore, that higher concentrations of butyric BTS additionally affect GSTP1 mRNA stability leading to a strongly reduced half-life. Concentration-dependent effects of butyric acid on RNA stability and cell signaling pathways involved in the regulation of GSTP1 expression remai
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br Conclusion In this report we describe
2022-07-22

Conclusion In this report, we describe the synthesis and evaluation of oxadiazole-based GSK3 inhibitors. Occupation of the ATP-binding pocket in its entirety led to the identification of several potent and selective compounds. These compounds are characterized by IC50 values in the low nanomolar
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