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Thiomyristoyl Although pharmacological studies from the end
2021-11-22

Although pharmacological studies from the end of the 20th century suggested that β1-AR induces a cAMP-dependent apoptosis [30], more recently it has been demonstrated that cAMP, acting through PKA, may be a crucial anti-apoptotic factor in cardiac myocytes [31]. cAMP can also stimulate PI3K, and the
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In diseased blood vessels increased production of reactive o
2021-11-20

In diseased blood vessels, increased production of reactive oxygen species (ROS), such as peroxynitrite, superoxide, and hydrogen peroxide, have been found [[53], [54], [55]]. Peroxynitrite was suggested to alter the redox state of sGC [53] while hydrogen peroxide interfered with the action of NO bu
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The differential tissue and ligand dependent signaling descr
2021-11-20

The differential tissue- and ligand-dependent signaling described here has important implications for the therapeutic potential of synthetic GPR109A agonists for the treatment of atherosclerosis. The failure of MK-0354, a biased, partial GPR109A agonist, to activate signaling pathways upstream of va
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br Ligand binding free energies In order
2021-11-20

Ligand-binding free energies In order to compute the absolute free Poly (A) Tailing associated with binding a ligand to a flexible iGluR LBD, a theory that accounts for all the principal thermodynamic contributions from ligand docking and LBD closure had to be developed. This was accomplished us
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Regarding IAV types of hemagglutinin and types of
2021-11-19

Regarding IAV, 18 types of hemagglutinin and 11 types of neuraminidase were described and none of the commercialized antiviral drugs are susceptible to protect against all strains that will emerge from the animal reservoir (Webby and Webster, 2003). The strong dependencies of influenza viruses on we
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Tail group SAR of the imidazole derived analogs is
2021-11-19

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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br Introduction In addition to glucose
2021-11-19

Introduction In addition to glucose, which is the foremost stimulator of insulin secretion in beta-cells, other nutrients such as free fatty acids (also called non-esterified fatty acids, NEFA) contribute to glucose-stimulated insulin secretion (GSIS). Glucose triggers the processes leading to in
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The ability of the vasculature to determine the nature and
2021-11-19

The ability of the vasculature to determine the nature and magnitude of a stimulus is essential for the appropriate and proportionate response. The vascular response to injury include rapid changes to blood flow to reduce the loss of blood, followed by increased contact with the sub-endothelial laye
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br Acknowledgement This research was
2021-11-19

Acknowledgement This research was supported by Basic Science Research Program through the National Research Foundation of Korea funded by the Ministry of Education, Science and Technology (NRF-2016R1A2B4012818). Oral dihydroquercetin is the most popular administration route due to good patien
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A biochemical characterisation of this
2021-11-19

A biochemical characterisation of this functionally crucial LSD1-p53 interaction is the focus of this study. Using several complementary assays [29], [30], [31], [32], we find that a well-defined segment of p53-CTD is capable of binding to LSD1 active site, thereby inhibiting the enzymatic activity
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The histamine H receptor H R
2021-11-19

The histamine H3 receptor (H3R; 326–445 amino-acids) is located on histaminergic neuron somata, dendrites and axon varicosities, as well as on the axon varicosities and somata of other neurons, providing negative feedback to inhibit histamine synthesis and the release of histamine or other transmitt
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Although no data exist on Ptc
2021-11-19

Although no data exist on Ptc52 gene nuclear receptors in other plant species, the expression pattern presented in this study shows perceptibly low levels of transcript accumulation in tomato seeds and roots, low levels in the stem, flower and green fruit, and high levels in the leaves. This coinci
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It has been reported that CD
2021-11-19

It has been reported that CD133+ glioma stem Gambogic Acid are resistant to temozolomide (TMZ) therapy [155]. Dose dependent TMZ treatment of CD133+ cells enhanced activities of the Notch and SHh pathways [156]. Moreover, 500 μmol/L TMZ induced a significant upregulation of Gli1, HES1 and HES5 trans
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These inhibitors possess a cap
2021-11-19

These inhibitors possess a cap group build from cyclization of several amino-acid or non-amino-acid residues, four or more, with one residue bearing an alkyl arm terminated by ZBGs of various types: thiols, ketones or epoxides. In the case of romidepsin 30 (Fig. 7), the thiol group is initially in a
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Overall more males were HCV mono and co infected though
2021-11-19

Overall, more males were HCV mono- and co-infected, though there was no significant age difference among groups and between men and women (all p>0.05). Almost all patients included in this study were over 40 years, in line with the period in which no HCV screening was performed in Brazilian blood b
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