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br Introduction Initial studies of cancer metabolism in
2022-03-25

Introduction Initial studies of cancer metabolism in the early 1920s showed that the cancer phenotype for glucose metabolism is unique, with increased abilities to take up glucose and produce lactate, even under aerobic conditions [1]. This pathway, called aerobic glycolysis or the Warburg effect
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Our aim was to gain insight into mechanisms that
2022-03-25

Our aim was to gain insight into mechanisms that underlie the contribution of thrombospondin-1 (TSP1) to progression of CKD. TSP1 is the most-studied member of the thrombospondin family of matricellular proteins. Previous studies have demonstrated that pharmacological suppression or genetic depletio
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For some agonists these stable GPR responses were resistant
2022-03-25

For some agonists, these stable GPR119 responses were resistant to washing. Thus, sustained activation could continue, for at least a number of hours, even after removal of free agonist. These data are consistent with reports for other GPCR systems that do not desensitize (Calebiro et al., 2009, Fer
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br RNA preparation cDNA synthesis and RT PCR Trizol
2022-03-25

RNA preparation, cDNA synthesis and RT-PCR Trizol reagent (Invitrogen, Carlsbad, CA, USA) was used to extract total RNA from tissues according to the manufacturer’s protocol and isolated RNA quantity was determined by UV spectrophotometry (Nanodrop, Thermo Scientific, USA) and RNA integrity was v
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The glucokinase protein sequence is
2022-03-25

The glucokinase protein sequence is most closely related to the C-terminal domain of 100kD hexokinases, thus for glucokinase to evolve from a larger hexokinase ancestor it must have lost its N-terminal kinase domain. The genetic mechanism by which this occurred is currently unknown. Here we propose
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Regulation of pancreatic and cell mass has been extensively
2022-03-25

Regulation of pancreatic α and β cell mass has been extensively studied and hotly debated, due to potential therapeutic implications. Early claims of Angptl8 as “betatrophin” and Angptl4 as a regulator of glucagon secretion and α cell proliferation (Yi et al., 2013, Ben-Zvi et al., 2015) have not st
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To identify inhibitors of the
2022-03-25

To identify inhibitors of the Hh/GLI signaling pathway from natural resources, we have recently reported the successful construction of a cell-based screening assay system for the Hh/GLI signaling pathway (Fig. 1). This is an assay using a GLI-dependent luciferase reporter in human keratinocyte cell
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Extending time action is another strategy
2022-03-25

Extending time action is another strategy to increase in vivo efficacy. Twice daily administration of the unacylated analogs herein caused greater body weight loss in DIO mice than the equivalent dose administered as a single daily injection, suggesting that protracted time action should yield more
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LDN 57444 br Acknowledgments br Introduction When human red
2022-03-25

Acknowledgments Introduction When human red blood cell (hRBC) membranes are depolarized, either as intact LDN 57444 suspended in depolarizing (low Cl−) Ringers or under voltage clamp conditions using excised inside-out patches, they respond by opening a nonselective voltage-dependent cation (
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Another strategy adopted to enhance the
2022-03-24

Another strategy adopted to enhance the action of endocannabinoids is indirectly through blocking their metabolism. Indeed, amplifying the action of anandamide and 2-AG by inhibiting their enzymatic degradation has emerged to develop the endocannabinoid system for medicinal purposes. It is interesti
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In non Hodgkin lymphoma the catalytic SET
2022-03-24

In non-Hodgkin lymphoma the catalytic SET domain of the histone methyltransferase EZH2 is subject to recurrent heterozygous missense mutations . These alterations have been observed in ∼20% of patients with diffuse large B cell lymphoma (DLBCL) and ∼10% of patients with follicular lymphoma (FL). The
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The coenzyme S adenosylmethionine SAM binding
2022-03-24

The coenzyme S-adenosylmethionine (SAM)-binding pocket of Set7 is connected to the histone-tail binding groove by a conserved lysine-channel, similarly observed in vSET (Figures 2D and S3). The Set7 SAM-binding pocket is negatively charged as observed in other known HMTase structures. However, the b
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Sometime ago we have described diamino
2022-03-24

Sometime ago we have described diamino-1,3,5-triazines as histamine H4R ligands,12, 13 and aryl derivatives of the 1,3,5-triazine, which attenuated inflammatory and nociceptive response in vivo in the rodent models of inflammation induced by BTB06584 synthesis and zymosan. In this work we describe
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Almost all of the series and compounds exhibited higher
2022-03-24

Almost all of the series and compounds exhibited higher activities compared with the compounds in the other series. In these series, the tetrazole group was directly linked to a nitrogen atom of the amide group at the C-28 position, and the C-3 hydroxy group was either unmodified, oxidized, esterifi
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br Discussion By using ultra deep
2022-03-24

Discussion By using ultra-deep sequencing, we conducted a thorough assessment of HCV-NS3 protease variants in chronic PI-naïve patients infected with HCV-1a and HCV-1b under telaprevir-based triple therapy at baseline and after 4weeks of treatment. Several synonymous and non-synonymous substituti
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