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Linagliptin is a recently approved dipeptidyl peptidase DPP
2025-01-13

Linagliptin is a recently approved dipeptidyl peptidase-4 (DPP-4) inhibitor and widely considered as first-line treatment for patients with type 2 diabetes. DPP-4 is responsible for the inactivation of incretin hormones, such as glucagon-like peptide 1 (GLP-1). GLP-1 is released by the intestine aft
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Secondly as pointed out by
2025-01-13

Secondly, as pointed out by Sulentic and Kaminski in their recent paper [90], most of the AhR literature to date has focused on mouse AhR. Although both mouse and human AhR are interchangeable in many in vitro systems, the in vivo ligand binding affinity is drastically different between the two AhRs
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As an alternative to chronic receptor blockade we have
2025-01-13

As an alternative to chronic receptor blockade, we have been targeting adenosine kinase (ADK) – an astrocyte-based enzyme that catalyses the phosphorylation of adenosine, as a means to modify dihydrofolate reductase inhibitor adenosinergic signalling (Boison, 2006, Etherington et al., 2009). Up-reg
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Furthermore our lab previously reported that cadmium treatme
2025-01-13

Furthermore, our lab previously reported that cadmium treatment increased AChE-S and decreased AChE-R variants gene expression, which mediates the cell death observed on basal forebrain cholinergic neurons (Del Pino et al., 2016b). AChE-R decreased expression, which presents a neuroprotective role i
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Molecular docking is widely used to predict the interaction
2025-01-13

Molecular docking is widely used to predict the interaction between an enzyme and its inhibitors. This is a computational simulation approach that can be used as a tool to investigate the structure-activity relationship of ACE inhibitory peptides (Goodsell, 2009). It has been recently shown that ACE
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Introduction Chronic inflammation is increasingly
2025-01-13

Introduction Chronic inflammation is increasingly known as one of the most critical etiological factors in gastrointestinal (GI) cancers (Lee et al., 2016; Wang and Cho, 2015). Overexpression of 5-lipoxygenase (5-LOX), 5-LOX-activating protein (FLAP), as well as other leukotriene (LT) biosynthetic
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The ATX LPA signaling axis has been implicated in
2025-01-13

The ATX–LPA signaling “axis” [5] has been implicated in a perplexing variety of physiological and pathophysiological processes, including vascular and neural development [5], [26], [27], [28], [29], tumor progression and metastasis [30], [31], lymphocyte trafficking [22], bone development [32], neur
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Fencilli et al reported derivatives of PHA which demonstrate
2025-01-13

Fencilli et al. reported derivatives of PHA-680626 (15) which demonstrated strong anti-proliferative activity against large group of leukaemia cell lines including IM-resistant BAF3 cells expressing mutants like T315I, M351T and E255K. Decrease in Histone H3 phosphorylation led to induction of endo-
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The distribution and subcellular localization differs betwee
2025-01-10

The distribution and subcellular localization differs between the subtypes of mGlu receptors. Most mGlu receptors are broadly expressed in the brain, except for mGlu6, which is restricted to the retina. Some mGlu receptors are additionally found in glial cells, such as mGlu3 and mGlu5 (Aronica et al
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br The pathogenesis of AD and the targets of apelin
2025-01-10

The pathogenesis of AD and the targets of apelin Alzheimer's drugs Conclusions Introduction APJ, first identified from a human genomic library in 1993, belongs to a member of seven trans-membrane G protein-coupled receptor family. Its amino ATP detection kit sequence has 31% homology wi
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The results of our in vivo experiments provide
2025-01-10

The results of our in vivo experiments provide promising evidence that the apelin/APLNR axis is implicated in CCA growth and that targeting this axis with a receptor specific antagonist may help develop effective, tumor directed therapies. Not only do we show decreased proliferation and angiogenesis
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Numerous investigators have shown that RACK has several
2025-01-10

Numerous investigators have shown that RACK1 has several important, possibly related, roles in mRNA splicing and in translation. RACK1 interacts directly with specific components of the 40S ribosomal subunit (specifically, the 18S rRNA and ribosomal proteins rpS16e, rpS17e, and rpS3e [new names: uS9
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A rate limiting step in the
2025-01-10

A rate-limiting step in the generation of kynurenine and xanthurenic Lin28 1632 mg is the oxidation of N-formyl-kynurenine to l-kynurenine via indolamine 2,3-dioxygenase (IDO) or tryptophan dioxygenase (TDO). IDO and/or TDO knockdown decreases and ectopic over-expression increases production of end
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br Materials and methods br Results The average body
2025-01-10

Materials and methods Results The average body weights for each group of mice over the course of the study are shown in Fig. 2A. The average body weights of the mice in the saline control group and PACAP group increased slightly during the study. In contrast, starting at day 17, the body weigh
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br Conclusions and clinical relevance Astrogliosis
2025-01-10

Conclusions and clinical relevance Astrogliosis and an increase in ADK is a pathologcial hallmark of epilepsy. The consequence of increased ADK in the epileptic 5 methoxyuridine buy is a decrease in the ambient adenosine tone and A1R activity. As a result, systemic administration of A1R agonists
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