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Molecular properties as well as
2022-01-15

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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br Flavonoid function Antioxidants are
2022-01-15

Flavonoid function Antioxidants are compounds - when present at a lower concentration compared oxidizable substrate - that delay or prevent oxidation of the substrate [14], [106]. Antioxidants act as nucleophiles to reduce an oxidative molecule to prevent its interaction with another molecule [14
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To evaluate SLC A abundance after transfection we performed
2022-01-15

To evaluate SLC45A1 abundance after transfection, we performed western blots. Transfected COS-7 Potassium Canrenoate were lysed and separated for membrane fraction. Equal amounts of proteins from membrane fractions were resolved by SDS-PAGE, transferred to a nitrocellulose filter, and immunoblotted
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br Conclusion In conclusion SHP
2022-01-15

Conclusion In conclusion, SHP289-04 was demonstrated as a potent glucokinase activator. It could normalize the blood glucose level and lipid level in spontaneous type 2 diabetes model KKAy mice. At the same time, it ameliorated the function of islets and liver in KKAy mice. It had been proved to
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Yeast two hybrid screening studies
2022-01-15

Yeast two-hybrid screening studies have provided the foundation for countless investigations of protein-protein interactions [[141], [142], [143]]. To identify additional hepatic proteins similar to GKRP that are implicated in GCK regulation, a group of researchers conducted a two-hybrid study using
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br Experimental Procedures br Acknowledgments This work was
2022-01-15

Experimental Procedures Acknowledgments This work was supported by NIH/National Human Genome Research Institute (NHGRI) R00 HG006922 and NIH/NHGRI R01 HG008974 (to J.G.), the Huntsman Cancer Institute, and the Women’s Cancers Disease-Oriented Team at the Huntsman Cancer Institute. Research rep
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br Acknowledgements br Introduction High intensity noise exp
2022-01-15

Acknowledgements Introduction High-intensity noise exposure has long been known to induce damage in the peripheral and central auditory system, often resulting in auditory pathologies such as hearing loss, tinnitus and hyperacusis (Syka, 2002; Roberts et al., 2010). Within the inner ear, struc
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It was previously proposed that glucagon acts in
2022-01-15

It was previously proposed that glucagon acts in the liver, in which a signal is produced and relayed to the GSK2269557 via vagal nerves [8], [36], [37]. The concept that the liver is the primary target site was supported by the studies reporting that the glucagon receptor is localized in the liver
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br Some general considerations on anterior pituitary cell ty
2022-01-15

Some general considerations on anterior pituitary cell type, models, sex and drugs Historically, real-time analysis of native endocrine anterior pituitary cell excitability has been somewhat limited and thus much of the pioneering work on anterior pituitary cell excitability and stimulus-secretio
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br Conclusions GPCRs are versatile signaling molecules
2022-01-14

Conclusions GPCRs are versatile signaling molecules regulating almost all physiological processes, including energy homeostasis and glucose homeostasis.105, 106 They also prove to be important therapeutic targets. Drugs targeting GPCRs account for 30% of current pharmaceutical sales. GPR40 is a m
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The measured ROcc values and mg
2022-01-14

The measured ROcc50 values (4.8 and 42 mg/kg, respectively) were lower than those estimated from the mouse free Methylcobalamin concentrations (0.4 and 9.3 mg/kg for the sigma-1 and histamine H3 receptor, respectively) or rat CSF levels (0.65 and 4.5 mg/kg, respectively). This discrepancy is almost
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Given the overexpression of HO in some tumors such as
2022-01-14

Given the overexpression of HO-1 in some tumors, such as CML, and its potential involvement in chemoresistance to classical chemotherapeutic agents, compounds 4 and 8f were tested in CML cell lines resistant to IM, a classical TK inhibitor used in CML. Compounds 4 and 8f, in combination with IM, sho
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br Introduction Topological hedgehogs keep generating intere
2022-01-14

Introduction Topological hedgehogs keep generating interest in point-set topology as they are a rich source of counterexamples and applications (for a comprehensive survey on topological hedgehogs we refer to [1]; see also [9]). They may be described as a set of spines identified at a single poin
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In order to study the role of haspin s
2022-01-14

In order to study the role of haspin’s kinase activity in mitosis (and other cellular processes) and its potential role in cancer, we sought to identify and optimize inhibitors. Utilizing a recently developed time-resolved fluorescence resonance energy transfer (TR-FRET) high throughput screening (H
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The relaxant response to carperitide was
2022-01-14

The relaxant response to carperitide was influenced neither by the removal of the endothelium nor by treatment with the nitric oxide synthase inhibitor or nitric oxide scavenger. This result was to be expected as previous studies showing that the vasodilator action of atrial natriuretic peptide is e
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