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To further explain the energy differences between Group
2022-06-28

. To further explain the energy differences between Group-A and Group-B, the average distances between ligands and the zinc cation were obtained from the last 1ns trajectory. It turns out that the members of group A were within the coordination distance of the zinc ion, whereas those of group B stay
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Although side effects as paresthesia due to the application
2022-06-28

Although side effects as paresthesia due to the application of β-alanine are known, a study in 2006 pointed out that there are no clinical (biochemical or hematological) changes after a long-term supplementation with β-alanine. In 2015, the International Society of Sports Nutrition rejected any argu
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br Conflict of interest statement br Acknowledgments This wo
2022-06-28

Conflict of interest statement Acknowledgments This work was funded in part by a grant from the National Institutes of Health, NIDDK award #DK61425 (to PWS). Introduction The efflux of toxic compounds from the cell by multidrug exporters is an important mechanism for cellular homeostasis a
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br Voltage dependent anion channel VDAC
2022-06-27

Voltage-dependent anion channel VDAC is a ubiquitous protein showing well conserved structural and functional properties in spite of major variations in its sequence (for review see [50]). Most of what we know about VDAC electrophysiological properties (for reviews, see [51], [52]) was initially
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br Cellular transportation of nanoparticles
2022-06-27

Cellular transportation of nanoparticles and nanocomplexes Endocytosis and exocytosis are critically important phenomena in cellular metabolism, which involve the complex vesicular system. They deal with major cellular transportation activities including membrane homeostasis by transporting prote
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YM 58483 receptor br Acknowledgement The authors would like
2022-06-27

Acknowledgement The authors would like to thank the University of Johannesburg and the National Research Foundation for the financial support. Mr. D Harris and Dr. R Meyer from Shimadzu South Africa are thanked for their technical support. Prof Ian Dubery is thanked for access to the LC-MS instru
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Compared to the other histamine receptor subtypes the H rece
2022-06-27

Compared to the other ABT-869 receptor subtypes, the H3 receptor exhibits rather complex pharmacology, being subject to extensive splicing, leading to two major (H3-445 and H3-365) and possibly more functional human receptor isoforms; for a comprehensive review please see Leurs et al. (2005) and Bon
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GSTP catalyzed reduction of Prdx enhances its peroxidase act
2022-06-27

GSTP1-1 catalyzed reduction of Prdx6 enhances its peroxidase activity. Using standard NADPH/GR/GSH-coupled assays we used cell lysates from the transiently transfected fty720 to measure the influence of GSTP1 allelic variation on peroxidase activity. Specificity for detection of Prdx6 activity was
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br Conclusion br Author statement br Acknowledgments br Intr
2022-06-24

Conclusion Author statement Acknowledgments Introduction The hypothalamic-pituitary-gonadal (HPG) axis is an important neurohormone network for vertebrates that regulates their gonadal development and maturation, guarantees their pubertal development and maintains their normal reproducti
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Due to the therapeutic potential of GlyT inhibitors
2022-06-24

Due to the therapeutic potential of GlyT1 inhibitors, numerous drug screening campaigns have been started - and are still going on - which aimed at the identification of compounds with biological activity at or affinity for this drug target. For characterization of biological activity at GlyT1, tran
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In conclusion we demonstrated that the atypical high
2022-06-24

In conclusion, we demonstrated that the atypical high-basal activity of the mGlu3 Anhydrotetracycline hydrochloride receptor results mostly from its activation by low ambient glutamate concentrations. This is due to a unique interaction network located in the extracellular domain of the mGlu3 recep
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GK also called hexokinase IV or D is a glycolytic
2022-06-24

GK, also called hexokinase IV or D, is a glycolytic enzyme that converts beta lactamase to glucose-6-phosphate. GK has unique characteristics compared with those of the ubiquitously expressed hexokinase isoforms I–III, and is predominantly expressed in the pancreas and liver. In pancreatic β-cells,
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A number of GCK activators for treating T D
2022-06-24

A number of GCK activators for treating T2D have been developed and tested but not progressed successfully from clinical trials into therapy [45]. Our observations suggest that increased risk of hypoglycemia might be possible, particularly if drugs penetrate into brain. A further possibility is that
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Acknowledgments br Introduction The gut derived hormone oxyn
2022-06-24

Acknowledgments Introduction The gut-derived hormone oxyntomodulin (OXM) is a naturally occurring dual agonist of both the glucagon receptor (GCGr) and glucagons-like peptide 1 receptor (GLP-1r). Structurally OXM is the 29 (+)-MK 801 of glucagon with a C-terminal octapeptide tail. Administratio
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To directly address whether pharmacological attenuation of p
2022-06-24

To directly address whether pharmacological attenuation of physiological GIP provides therapeutic benefits in obese mice, we pursued a selective long-acting antagonist to complement the work we report on GIPR agonism. We report a GIP analog of sufficient aqueous solubility that employs a shortened N
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