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In summary we have discovered the
2022-06-29
In summary, we have discovered the first examples of movement of Asp189 upon binding to fXa inhibitors. A series of novel and potent fXa inhibitors with a phenyltriazolinone P moiety were identified. Although the general binding mode compared to our previously-reported fXa inhibitors was maintained,
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It has been known for some time that an
2022-06-28
It has been known for some time that an oral salt load given to mammals induces a much greater natriuresis than the intravenous administration of an equivalent amount of saline (Carey et al., 1976, Singer et al., 1998). In addition, oral administration of salt to rats has been reported to augmented
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At days and hours after MI the protein expressions of
2022-06-28
At 21 days and 24 hours after MI, the protein expressions of active JNK1 (P protein RF 9 receptor of p38 was down-regulated only at 21 days after MI (P to TRAF2, JNK1, and p38 at 24 hours (P Discussion This study demonstrates the role of GSTP1 in HF by inhibiting the TRAF2-induced MAPK activatio
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GSTP c C T SNP was genotyped
2022-06-28
GSTP1 c.341C > T SNP was genotyped in 90 patients tumor and 180 normal healthy individuals. The profile of GSTP1 c.341C > T WAY-262611 australia and genotypes is shown in Table 2. The profile of the genotypes was in agreement with Hardy-Weinberg equilibrium (χ2 = 2.11). Minor allele frequency (341T)
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By combining the results of
2022-06-28
By combining the results of the melting curve analysis of exon 5 and exon 6, the allelic setup of our 250 subjects was determined; the four allelic variants are shown in Table 1. However, GSTP1-1 *A/*C and GSTP1-1 *B/*D could not be distinguished from one another because both genotypes are character
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After establishing improved GSNOR potency some of the potent
2022-06-28
After establishing improved GSNOR potency, some of the potent inhibitors were further evaluated for microsomal stability and CYP inhibition studies (). Majority of the tested analogs revealed high metabolic stability in human and rat liver microsomes, and moderate to low stability in mouse liver mic
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Approximately mammalian genes encoding family A or rhodopsin
2022-06-28
Approximately 250 mammalian genes encoding family A (or rhodopsin-like) GPCRs have been cloned (Lee et al., 2001a). As yet, the total number of cloned GPCRs reported in the literature including the secretin and metabotropic glutamate-like families of GPCRs falls short of the projected 616 GPCR-encod
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In recent large clinical studies AIM
2022-06-28
In recent large clinical studies, AIM-HIGH and HPS2-THRIVE, the additional treatment of nicotinic osi sc 175 to statin-based LDL-C lowering therapy did not decrease the major vascular events on the patients who had atherosclerotic vascular diseases [43,44]. In the AIM-HIGH study, the secondary anal
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In addition to the role of TGR the FXR
2022-06-28
In addition to the role of TGR5, the FXR-FGF15/19 axis has been implicated in other aspects of glucose metabolism and metabolic disorders. In humans, both obesity and type 2 diabetes mellitus (T2DM) are associated with lower plasma FGF19 levels [67,68]. A derivative of the naturally occurring FXR ag
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We recently reported the first cyclopropene
2022-06-28
We recently reported the first cyclopropene-analog of the amino p-Cresyl sulfate neurotransmitter glutamate (Fig. 2A) [27]. This first-generation cyclopropene-glutamate expanded the only other documented report of a cyclopropene-neurotransmitter (cyclopropene-GABA analog by Reissig and coworkers) [
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The regulation of casein expression during lactation
2022-06-27
The regulation of casein expression during lactation is a complex process involving a coordinated response at several levels. A variety of hormones are known to play roles in lactogenesis, such as prolactin (PRL), insulin, and hydrocortisone, and there is now increasing evidence that growth factors,
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br Materials and methods Manganese chloride MnCl H O
2022-06-27
Materials and methods Manganese chloride (MnCl2·4H2O), glutamate, glutamine, Lucifer Yellow, polyclonal anti-GFAP and MTT assay kits were purchased from Sigma Chemical Co. (St. Louis, MO). Dulbecco's Modified Eagle's Medium-F12 (DMEM-F12) with Earle's salts, foetal bovine serum, penicillin, and s
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br Conflicts of interest br Acknowledgements This
2022-06-27
Conflicts of interest Acknowledgements This research was supported by grants from National Research Foundation, Korea (NRF-2017RIDIA3B04033313) and Yeungnam University (216-A-061-042). Introduction Kluyveromyces lactis is a yeast that produces one of the ß-galactosidases (ß-gals) most wide
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gsk-3 Although GABA C receptors were originally described in
2022-06-27
Although, GABA-C receptors were originally described in the spinal cord [16], clues to their physiological function arise mainly from studies in the visual system [5], [26]. In mammals, GABA-C receptors are found abundantly in cone photoreceptors and bipolar cell axon terminals, where they participa
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Starting from the hypothesis that the linker portion of
2022-06-27
Starting from the hypothesis that the linker portion of the inhibitor molecules does not necessarily require the presence of an alcohol/ether or a carbonyl group, the same research group performed another scaffold hopping analysis, obtaining 1500 new compounds as potentially active HO-1 inhibitors [
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