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Acute in vivo experiments were
2021-12-08
Acute in vivo experiments were performed in normoglycemic 129SVE mice to confirm GPR119 activation and corresponding rotenone control. GIP release was utilized as a biomarker for target receptor engagement and plasma GIP levels were measured 45min after oral dosing (). Both 3 and 10mg/kg produced an
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However Gingrich and Hen reported that absence of the
2021-12-08
However, Gingrich and Hen reported that absence of the gene at all stages of ontogenesis of mice may interfere with the normal developmental program and/or the organism may undergo changes in other systems to compensate for gene absence (46). In addition, potentially altered maternal behavior of GPR
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The development of immobilization techniques for glucosidase
2021-12-08
The development of immobilization techniques for β-glucosidase offers a potential way to enable its reuse several times [13]. The aim of immobilization is to trap the enzyme within or on the surface of an insoluble material with retention of its catalytic activity [14]. The immobilization strategy a
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br Introduction Glucose is the major carbon source in most
2021-12-08
Introduction Glucose is the major carbon source in most organisms. Cancer eph receptor in particular require a steady source of energy to maintain growth and proliferation, and preferentially use glycolysis for their energy supply even under aerobic conditions. Glucose uptake in mammals is mainl
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In type diabetic subjects with mean baseline
2021-12-08
In type-2 diabetic subjects with mean baseline glycated hemoglobin A (HbA) of 8.4%, q.d. administration of MK-0893 for 12weeks as a monotherapy resulted in dose-dependent decreases in HbA and FPG. Administration of MK-0893 q.d. at doses of 20, 40, 60, and 80mg led to observed reductions in HbA of 0.
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br Discussion According to the generally accepted notion
2021-12-08
Discussion According to the generally accepted notion which originated from the study of ATP-depleted Oseltamivir the changes in Ca2+ homeostasis induced by ATP depletion and leading to the activation of the Gárdos effect are due to the inhibition of Ca2+ pumping, and the subsequent entry of Ca2
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We hypothesize that HBO increases
2021-12-08
We hypothesize that HBO2 increases GABA activity at the GABAA receptor via a nitric oxide dependent mechanism. Blotting for the phosphorylated β3 subunit of the GABAA receptor should theoretically be increased when there is more GABA activity at the receptor (McDonald et al., 1998). We expected that
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Another small compound targeting IBAT has been
2021-12-08
Another small compound targeting IBAT has been evaluated in Phase I clinical trial (EudraCT 2013-001175-21) [86]. The oral administration of A4250 to healthy subjects did not give rise to any serious adverse events, was well tolerated and had a similar safety profile as elobixibat; however, it cause
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In summary we have discovered the first examples of movement
2021-12-08
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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Another important question for future studies will
2021-12-08
Another important question for future studies will be whether FAAH inhibitors work to normalize impairments in fear extinction that are known to be produced by environmental insults such as exposure to abused drugs and stress 97, 103. Indeed, several authors have posited utility of FAAH inhibitors f
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The Jumonji JmjC domain containing KDM family members
2021-12-07
The Jumonji (JmjC) domain-containing KDM family members can be clustered into seven subfamilies (KDM2 – KDM8). The KDM2 cluster catalyzes H3K36me2/me1 demethylation; in addition, KDM2B/JHDM1B/FBXL10 has been suggested to catalyze demethylation of H3K4me3 [3]. Cell culture studies support that KDM2 p
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Cux is a cell cycle dependent
2021-12-07
Cux1 is a cki dependent transcription repressor that is aberrantly expressed in the Pkd1 null, Pkd1CD, and cpk mouse models of PKD, as well as in human ADPKD cells (Vanden Heuvel et al., 1996; Sharma et al., 2005; Paul et al., 2011; Alcalay et al., 2008). In Pkd1 null mice and in human ADPKD cells
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CONUT score is an effective detector of
2021-12-07
CONUT score is an effective detector of predicting OS and RFS in HCC patients. We found that patients with a damaged immune-nutrition status had significantly poor OS and RFS. Our initial literature review also retrieved other studies evaluating the survival of HCC patients using CONUT score [36,48,
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In the present study we observed
2021-12-07
In the present study, we observed a decrease in body weight gain in Tg rats. It is uncertain whether this effect is due to Denr, Gpr81, or Gpr109a. In this regard, Gpr81 mice have been reported to have reduced body weight gain [28]. Moreover, a small clinical study has reported that obese patients t
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A subsequent modeling study by a
2021-12-07
A subsequent modeling study by a different group was based on the bovine rhodopsin homology model using the 1L9H construct [38]. However, the site-directed mutagenesis data and docking suggested that the niacin-binding pocket is different to that described in the aforementioned report, but similar t
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