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Hepatic inflammation and fibrosis are hallmarks of the NASH
2024-01-25

Hepatic 73122 mg and fibrosis are hallmarks of the NASH phenotype and are thought to occur in a subset of patients with NAFLD. While it is hypothesized that therapeutic lowering of hepatic lipids will be sufficient to improve hepatic fibrosis and inflammation secondarily, this remains controversial
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Recent studies demonstrated that AHR has
2024-01-25

Recent studies demonstrated that AHR has an important role in the interplay between cancer metabolism and tumor-specific immunity. Tryptophan catabolism is increasingly recognized as a metabolic pathway that promotes tumorigenesis through its role in immune suppression [75]. The rate-limiting enzyme
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Perhaps the discovery of this linkage
2024-01-25

Perhaps the discovery of this linkage has served to catapult much of the work on ABCA1, leaving its family member in need of a relationship with a defined human pathology. In this regard, there is by now a quite mature literature that suggests that ABCA2 may have been overlooked in terms of its impo
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The pathogenesis of d penicillamine induced MG is not
2024-01-25

The pathogenesis of d-penicillamine-induced MG is not clear. The repertoire of anti-AChR Picrotoxin mg in d-penicillamine-induced MG has been shown to be similar to that in idiopathic MG in terms of AChR antigenic regions, suggesting a common immune mechanism (Tzartos et al., 1988). About 20% of d
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DMAT br Thymic expression of AChR Both linear unfolded epito
2024-01-25

Thymic expression of AChR Both linear unfolded epitopes of AChR subunits and the intact AChR are avidly expressed in thymus, particularly by thymic epithelial cells and myoid cells [17], [18], [19]. AChR-antibody positive MG patients often show thymic hyperplasia, characterized by lymphoid follic
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Using constant potential amperometry and electrochemical
2024-01-25

Using constant potential amperometry and electrochemical enzyme-based biosensors selective for choline—and, therefore, an accurate readout of EMD638683 release (Baker et al., 2015; Bruno et al., 2006a; Parikh et al., 2004, 2007)—tonic and phasic release of acetylcholine were measured simultaneously
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Finally Urban Ciecko et al asked
2024-01-25

Finally, Urban-Ciecko et al. (2018) asked whether this enhancement is specific to the pyramidal to SST neuron synapses or more generally observed in other synapses of the cortical microcircuit. Synapses between pyramidal cells showed no sign of potentiation after either bath application of the choli
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The relatively high concentration of HT
2024-01-24

The relatively high concentration of 5-HT used in this study (100 µM) is consistent with the concentrations used in other published ex vivo studies (Ropert and Guy, 1991, Passani et al., 1994, Shen and Andrade, 1998). In our paradigm 5-HT was focally applied at the surface of the slice via a fast pe
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HT receptors are distributed throughout the brain
2024-01-24

5-HT3 receptors are distributed throughout the brain, within the brainstem (e.g., nucleus tractus solitarius, area postrema and spinal trigeminal nucleus) and C527 (e.g., hippocampus, amygdala, nucleus accumbens, putamen and caudate) (Abi-Dargham et al., 1993, Barnes et al., 1989, Bufton et al., 19
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Derivatives of M that possess
2024-01-24

Derivatives of (+)-M100907 that possess either an alkyne or an azide have been synthesized. The most active enantiomer was obtained by resolution of a relatively early intermediate in the synthesis. The ability of these Ursodiol synthesis to maintain 5-HTR antagonist properties as (+)-M100907 was d
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The knowledge on the structure of CYP including its active
2024-01-24

The knowledge on the structure of CYP17, including its active site, provides a rationale for understanding many mutations that are found in enzyme dysfunction in clinical disease as well as the enzyme's dual hydroxylase and lyase catalytic capabilities. This knowledge will assist rational drug desig
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Aurora A or B selective and pan aurora inhibitors have
2024-01-24

Aurora -A or -B selective and pan-aurora inhibitors have demonstrated different preclinical and clinical therapeutic efficacies [2,[19], [20], [21], [22], [23]]. For example, clinical trials for a pan-Aurora inhibitor VX-680 (developed by Vertex) were halted at phase II for toxicity reasons (one cas
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We used the lead compound C to
2024-01-24

We used the lead compound C4 to demonstrate that small molecule ACL inhibitors can recapitulate ACL knockdown (KD) in modulation of cancer stemness. We have shown previously that ACL KD reduced the CSC population in multiple cancer cell lines. The E-snail cells are an established CSC model system. E
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In clinical studies BA has been reported to
2024-01-24

In clinical studies, BA has been reported to promote dose-dependent LDL-C lowering effects of up to 30% as monotherapy, and up to an additional 24% when added in combination with stable statin therapy, or approximately 50% when combined with ezetimibe 109, 110, 111, 112. These effects were accompani
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In addition to drawing attention to
2024-01-24

In addition to drawing attention to Ser454 of ACL as a phosphosite that is regulated by both BDK and PPM1K, our phospho-proteomics screen identified several additional sites in other proteins. For example, Ser25, Ser29, and Ser79 of the lipogenic enzyme acetyl-coA carboxylase 1 (ACC1) were found to
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