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The GSTP promoter region in PCA cells without
2022-06-23

The GSTP1 promoter region in PCA cells without or with reduced GSTP1 mRNA expression had a different histone modification pattern than BPH-1 cells with GSTP1 mRNA expression: the repressive histone modifications H3K9me3/H3K27me2 were distinctly increased and H3K27me3/H3K9me2 were slightly decreased
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The observed glucose intolerance and elevated fasting
2022-06-23

The observed glucose intolerance and elevated fasting blood glucose in this study is in consonance with earlier study (Ferris and Kahn, 2012). These have been the common features of GC exposure and are not unexpected. Previous researches that reported IR during GC exposure have shown controversy con
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While PLGA implants could be beneficial for regenerative
2022-06-23

While PLGA implants could be beneficial for regenerative angiogenesis in the context of wound healing, they 3,3',5'-Triiodo-L-thyronine synthesis could also lead to adverse effects. Indeed, extracellular acidification inhibits osteoblast proliferation, differentiation, and extracellular matrix mine
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Several studies have found that GPR
2022-06-23

Several studies have found that GPR55 possesses a distinct pharmacology from that of CB1 and CB2, and that only certain cannabinoids act at this receptor. In transfected s6 kinase expressing hGPR55, out of more than 20 synthetic and endogenous cannabinoids evaluated, only 2 compounds, SR141716A (Ri
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GLP is known to be expressed in a
2022-06-23

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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br FXR Agonists Azepinol b
2022-06-23

FXR Agonists Azepinol[4,5-b]indole 1 (hEC50=600nM, efficacy (eff)=100%) was identified as a FXR agonist lead from a high-throughput screening effort. Structure–activity relationship (SAR) studies around the azepine ring demonstrated that dialkyl substitution at C-1 led to a 30-fold improvement in
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The spatial effects of Ebi involve the creation
2022-06-23

The spatial effects of Ebi2 involve the creation of a moderate bias in CD4+ T cell distribution toward the LN periphery. Is this modest effect meaningful in an evolutionary sense? In this regard, we think the following considerations are relevant. First, asymmetric CD4+ T cell positioning is highly
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An alternative approach to improving pharmacokinetic profile
2022-06-23

An alternative approach to improving pharmacokinetic profile while retaining high GlyT1 potency was also pursued. Libraries were prepared in which potency enhancing piperidine C4 substituents were combined with clearance lowering truncated alkyl sulfonamides. The result was the discovery of (). Unl
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br Membrane transporters as a
2022-06-23

Membrane transporters as a novel therapeutic target in pediatric TBI The concept of targeting membrane transporters began with identifying a neuroprotective drug and a corresponding transporter inhibitor. Somewhat serendipitously, we discovered that N-acetylcysteine (NAC), a cysteine donor for GS
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br Conflicts of interest br Funding This work
2022-06-23

Conflicts of interest Funding This work was supported by the National Natural Science Foundation of China (No.81670558; 81800542), and the Science & Technology Development Fund of Tianjin Education Commission for Higher Education (No.2017KJ221). Acknowledgements Introduction Free fatty
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br The concept of the axo myelin synapse
2022-06-23

The concept of the axo-myelin ‘synapse’ Axons can release glutamate in a Ca+-dependent and independent manner (reviewed in [13,69]). Glutamate released from axons activates GluRs located in myelin, a feature that gave rise to the idea of the axo-myelin ‘synapse’ by analogy with classical synaptic
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Introduction As per WHO report in more than million peoples
2022-06-23

Introduction As per WHO report, in 2014 more than 422 million peoples were living with diabetes and according to International Diabetes Federation, by 2045 this figure would reach 693 million [1,2]. Diabetes, a fast growing major health problem, is common chronic, metabolic disease characterized by
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Considerable evidence links sustained GCG administration
2022-06-23

Considerable evidence links sustained GCG administration to the reduction of food intake, enhancement of energy expenditure and weight loss in rodent and human studies [16], [17], [18]. Moreover, patients presenting with GCG-producing tumors frequently manifest severe weight loss, through mechanisms
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br Mechanisms of gap junction internalization disaggregation
2022-06-22

Mechanisms of gap junction internalization: disaggregation, endocytosis and annular gap junctions It has been clearly shown that gap junction internalization can occur by a distinctive mechanism where one cell internalizes an entire gap junction via formation of double membrane structure termed a
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br Acknowledgements br Introduction Muscle FBPase is very
2022-06-22

Acknowledgements Introduction Muscle FBPase is very sensitive to AMP inhibition and in the presence of physiological concentrations of this effector in muscle fibres FBPase should be almost completely inactive [1], [2]. Recently, we have presented evidence that, in vitro, muscle aldolase binds
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