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As a part of our
2022-01-15

As a part of our continuing efforts towards discovery of new class of compounds against different therapeutic areas and based on the literature reports, we designed a dual pharmacophore which possess a long aliphatic chain of free fatty acids and a phenyl propanoid part of known GPR40 agonists. Here
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AKR D is very highly expressed in
2022-01-15

AKR1D1 is very highly expressed in human liver and based upon the observations outlined above, with respect to other steroid hormone pre-receptor metabolising enzymes, it is entirely plausible that AKR1D1 could represent a critical regulatory step in the control of metabolic phenotype within the liv
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Whether or not SMO and SMO dependent
2022-01-15

Whether or not SMO and SMO-dependent HH signaling play a role in hematopoiesis is a subject of strong controversy. Obviously, the effects of SMO deletion are highly contextual and dependent on the timing of deletion. transplanted murine Smo−/− fetal liver Meleagrin into sublethally irradiated mice
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PK profiles of were evaluated and
2022-01-14

PK profiles of were evaluated and found to be improved compared to compound presumably due to interruption of β-oxidation. Low clearance and high plasma exposure were considered to be suitable profiles as an oral agent (). We first examined in vitro insulinotropic effects of compound from MIN6 cel
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In conclusion a novel series of GPR
2022-01-14

In conclusion, a novel series of GPR40 agonists containing nitrogen heterocyclic rings derived from TAK-875 were designed and synthesized. The structural activity relationship studies indicated that the substituents on the nitrogen Penciclovir had a remarkable effect on the GPR40 agonistic activity
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br Conclusions Symptoms from bilateral thalamic edema caused
2022-01-14

Conclusions Symptoms from bilateral thalamic edema caused by increased venous hypertension can be reversed with appropriate management of the inciting vascular lesion. This case demonstrates a rare patient with decreased CBF in the thalamus in SPECT and completely recovered after factor Xa inhibi
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Coenzyme Q10 The following are the supplementary data relate
2022-01-14

The following are the supplementary data related to this article. Transparency document Introduction Hypoxia is a pathological process that causes abnormal changes in metabolism, function and morphological structure of tissue because of insufficient oxygen supply. It's reported that hypoxia w
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Acknowledgments br INTRODUCTION AND OBJECTIVES br
2022-01-14

Acknowledgments INTRODUCTION AND OBJECTIVES METHODS RESULTS CONCLUSIONS Introduction Class 3 alcohol dehydrogenase (EC 1.1.1.1), also known as ADH5 chi polypeptide in humans, was first identified by Koivusalo et al. [1] as a NAD+-dependent hydroxymethylglutathione (HMGSH) oxidase. By
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GLP is known to be expressed
2022-01-14

GLP-1 is known to be expressed in a subset of taste bud cells and has been shown to co-localize with GPR120 in the circumvallate papillae [22]. Local GLP-1 regulates taste preference for sucrose [54]. Analogous to intestinal mediation of GLP-1 by GPR120, Martin et al.[22] report induction of GLP-1 s
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FPG had no consistent activity in reducing G T transversions
2022-01-14

FPG-2 had no consistent activity in reducing G→T transversions. Gao and Murphy [2] earlier reported that FPG-2 had a limited amount of activity in vitro on depurinated, UV-treated, and methylene-blue-treated DNA (but not on 8-oxo-G-containing oligonucleotides). FPG-2 contains the N-terminal domain a
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To further investigate the molecular
2022-01-14

To further investigate the molecular mechanisms that underlie glycine's β-cell protective effects through its antioxidative activity in diabetes, we used a H2O2/high glucose-induced apoptosis cell model. Similar effects on ROS generation of high glucose and H2O2 support the in vivo results, suggesti
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5-alpha reductase inhibitors EAAT glutamate uptake is driven
2022-01-14

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 5-alpha reductase inhibitors of glutamate into the cell against a steep concentration
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br Vesicular glutamate transporters VGLUTs br
2022-01-14

Vesicular glutamate transporters (VGLUTs) Conclusions Due to the molecular cloning of EAAT and VGLUT subtypes, a better understanding of the functional properties of these carriers has been elucidated over the last few years. In the case of the EAATs, specific blockers, such as trans-2,4-PDC,
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The simple carrier model for GLUT
2022-01-14

The simple carrier model for GLUT1 transport activity proposes that the transporter alternates between an outward facing glucose binding site and an inward, cytoplasmic, facing glucose binding site. Cytochalasin B is an endofacial inhibitor and appears to preferentially bind to the open, inward faci
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Herein exploiting several spectroscopic techniques i e CD UV
2022-01-13

Herein, exploiting several spectroscopic techniques, i.e. CD, UV and NMR, along with gel electrophoresis, size exclusion chromatography and in silico prediction analysis, the conformational behaviour of R1.2 and R1.3 was studied in Na+- and K+-rich solutions, which mimic the extra- and intracellula
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