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Numerous stimuli lead to inactivation of GSK including
2022-06-27

Numerous stimuli lead to inactivation of GSK-3, including Growth Factors such as EGF (Epidermal Growth Factor), PDGF (Platelet-Derived Growth Factor), BDNF (Brain-derived neurotrophic factor), IGF (Insulin-like growth factor) and insulin (Beaulieu et al., 2009, Chen and Russo-Neustadt, 2005, Cohen a
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SB 204990 br Action of GPR in metabolically active tissues I
2022-06-27

Action of GPR55 in metabolically active tissues In addition to being highly expressed by discrete brain regions, as described in Section 2, GPR55 is also expressed in a wide range of peripheral tissues, including spleen, adrenals and bone (Sawzdargo et al., 1999, Ryberg et al., 2007, Whyte et al.
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br Introduction High dose niacin
2022-06-27

Introduction High dose niacin, or nicotinic acid, has been used as an athero-protective drug for more than 50 years (Carlson, 2005, Offermanns, 2006). When taken in pharmacological doses (>1g/day), the nicotinic SB 216763 form of niacin modulates plasma lipid profiles including decreasing circul
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In summary we have developed an efficient synthetic route to
2022-06-24

In summary, we have developed an efficient synthetic route to the required urea-isostere containing hydroxamic acid-based inhibitor . The target molecule, , was found to retain the inhibitory potency of the corresponding carbo-analog against glyoxalase-I while possessing resistance to cleavage by γ
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The need for an inflammatory risk
2022-06-24

The need for an ‘inflammatory risk profile’ was recently discussed by several investigators. The present study is all the more significant in that it shows that a phenomenon that is influenced by various atherosclerotic risk factors and acute phase proteins is, indeed, associated with a less favorab
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EAAT glutamate uptake is driven
2022-06-24

EAAT glutamate uptake is driven by the co-transport of three sodium ions and one proton, as well as the counter-transport of one potassium ion (Fig. 1B). This complex stoichiometry frees up enough energy to permit online job of glutamate into the cell against a steep concentration gradient. Addition
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Therefore we investigated the acute
2022-06-24

Therefore, we investigated the acute and delayed response of 92 human mono- and dizygous twins to an acute shift from low fat to high fat diet with respect to serum levels of VEGF and the expression of SLC2A1 in subcutaneous adipose tissue (AT). By comparing the degree of concordance of basal and di
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This study was approved by our institutional ethics
2022-06-24

This study was approved by our institutional ethics committee, and informed consent was obtained from each participant or legal guardian. We performed whole-genome SNP genotyping in the one unaffected and two affected siblings by using the Illumina Human 610 Genotyping BeadChip panel, which interrog
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To date three GAL subtype
2022-06-24

To date, three GAL subtype receptors have been cloned and characterized, GALR1, GALR2 and GALR3. However, it is unknown which one(s) of the three subtype receptors in JC-1 is most effective to regulate insulin resistance in diabetic rats as yet. Recent studies fromanimalmodels of diabetes and obesi
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Andexanet alfa works as a decoy for
2022-06-24

Andexanet alfa works as a decoy for the FXa inhibitor to bind to irreversibly. The recently completed ANDEXA-4 trial, which was a prospective, open-label, single group study, found that patients achieved good or excellent hemostasis in 82% of subjects [, , ]. There was an overall 10% thromboembolic
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Andexanet alfa works as a decoy for
2022-06-24

Andexanet alfa works as a decoy for the FXa inhibitor to bind to irreversibly. The recently completed ANDEXA-4 trial, which was a prospective, open-label, single group study, found that patients achieved good or excellent hemostasis in 82% of subjects [, , ]. There was an overall 10% thromboembolic
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The present study was designed to clarify the distribution a
2022-06-24

The present study was designed to clarify the distribution and the function of the endothelin receptors in the guinea-pig urinary bladder. We found that endothelin-1 produced a clear tonic contraction via both A 205804 mg subtypes, the endothelin ETA and ETB receptor, and that sarafotoxin S6c also
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Although epigenetic mechanisms are implicated in the pathoge
2022-06-23

Although epigenetic mechanisms are implicated in the pathogenesis of hematopoietic malignancies, little is known about the role of lysine-specific histone demethylases and whether manipulation of these enzymes can be translated into targeted therapies. KDM6A is the most frequently mutated histone de
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br Materials and methods br Results We examined
2022-06-23

Materials and methods Results We examined the cardiac mitochondrial density of HKI and markers of oxidative and metabolic stress in trout exposed to an aerated control exposure, an aerated (normoxic) thermal insult, or a hyperoxic thermal insult. Should mtHK provide a cardioprotective effect i
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P Benzoxaborole substituted macrocyclic compounds based
2022-06-23

P4-Benzoxaborole-substituted macrocyclic compounds based on ITMN-191 scaffold were prepared using a general scheme as shown in . ITMN-191 was prepared by following a patent procedure. The P4 BOC group was removed by treatment with TFA in dichloromethane to give amine . The coupling of the amine to 6
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