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Tail group SAR of the imidazole derived analogs
2022-08-23
Tail group SAR of the imidazole derived analogs is shown in . The previous SAR study from the discovery of AMG 837 revealed that a simple un-substituted meta-biphenyl tail group was less favorable in terms of potency. Efforts to introduce polarity to the tail group were not successful. When a methyl
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Type II diabetes is characterized by an inability to
2022-08-23
Type II diabetes is characterized by an inability to maintain glucose homeostasis due to insulin desensitization and/or insufficient insulin secretion. GPR40, also known as free fatty Calcein acetoxymethyl ester mg receptor 1 (FFAR1), is a member of the G-protein-coupled lipid-activated family of r
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br Fenton reaction based nanomaterials for
2022-08-23
Fenton reaction-based nanomaterials for ferroptosis In Fenton reaction, H2O2 is converted by Fe2+ or Fe3+ to highly oxidative ROS (Eqs. (1) and (2)), which is commonly used to catalyze the degradation of refractory organics [34]. Since the tumor microenvironment is characterized by low acidity an
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Introduction The Antiretroviral Therapy ART in the last deca
2022-08-22
Introduction The Antiretroviral Therapy (ART), in the last decade, has been providing a better treatment for the Human Immunodeficiency Virus 1 (HIV) infection, by reducing its viral load to undetectable levels and recovering the immune system. In fact, according to the last data from UNAIDS the mo
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An important example of a frame is
2022-08-22
An important example of a frame is the lattice of open subsets of any topological space X. The correspondence is clearly functorial (by taking inverse images), and consequently one has a contravariant functor with the category of topological spaces and continuous maps as domain category. The fun
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Multiple studies from our laboratory and others which have u
2022-08-22
Multiple studies from our laboratory and others, which have used stoichiometric kinetic analyses of ANP/NPRA, have provided strong evidence that bound ligand-receptor complexes are internalized and processed intracellularly, and that degraded products are released into the culture medium of various
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Earlier we have shown relationship between cytotoxicity
2022-08-22
Earlier, we have shown relationship between cytotoxicity and receptor degeneration in U 46619 having specific neurotransmitter receptors (Siddiqui et al., 2008). In the present study, exposure to 4-HNE reduced expression of DA-D2 receptors in PC12 cells which was found to be concentration dependent
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Although it is currently unknown why the longer splice
2022-08-22
Although it is currently unknown why the longer splice variant found in the human has not been found in any other species, similar results have been reported for other receptors, including the DL-Dithiothreitol sale receptor splice variant ERbeta2 identified in human and primate, but not other speci
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The global spread and ever increasing
2022-08-22
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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To verify the feasibility of the proposed method
2022-08-22
To verify the feasibility of the proposed method, EIS is firstly adopted to study the modification processes of the electrode. As shown in Fig. 1A, the nyquist plot of bare gold electrode exhibits a straight line, which indicates a fast charge transfer process (curve a). After modified with probe a,
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To examine the possible role of mGluRs in the LH
2022-08-22
To examine the possible role of mGluRs in the LH/PFA in the hypercapnic ventilatory response, a nonspecific antagonist of mGluRs, MCPG, was microinjected into the LH/PFA. MCPG elicited a significantly increased hypercapnic ventilatory response in awake rats, but not during sleep, in the light and da
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In addition to GABA mediated mIPSCs glutamate
2022-08-22
In addition to GABA-mediated mIPSCs, glutamate-mediated miniature excitatory postsynaptic potentials (mEPSCs) regulate the excitability of the nervous system. GluRs can be divided into ionic and metabotropic GluRs. Ionotropic GluRs can be pharmacologically differentiated by specific binding of the a
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Phylogenetic trees of receptors for peptides similar to
2022-08-22
Phylogenetic trees of receptors for peptides similar to glucagon from diverse vertebrate species typically are similar to the tree presented in Fig. 3 (Sivarajah et al., 2001, Chow et al., 2004, Irwin and Wong, 2005, Cardoso et al., 2005, Cardoso et al., 2006, Ng et al., 2010, Park et al., 2013, Hwa
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br Acknowledgements This work was supported by
2022-08-22
Acknowledgements This work was supported by a fellowship to C.H. under the ‘100 Foreign Expert’ scheme of the Shanxi province government(R100456). Conflict of interest: Dr. Holscher is a named inventor on a patent submitted by Lancaster University on the use of dual GLP-1/GIP analogues in neurode
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According to the aforementioned preclinical
2022-08-22
According to the aforementioned preclinical and clinical data, GHS-R1a blockade appears to be a potential pharmacological approach to treat AUD. Given that GHS-R1a has high constitutive (ligand-independent) activity, inverse agonism of the receptor may exert more potent and desirable effects than pu
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