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Toxoplasma gondii is an exceptionally
2022-03-21
Toxoplasma gondii is an exceptionally tractable apicomplexan parasite that expresses a limited yet representative subset of apicomplexan cyclase orthologs, making it an ideal model for investigating cyclic nucleotide signaling in Apicomplexa. Of the five putative nucleotide cyclases, only TgACα1 and
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br Acknowledgments This research was partially
2022-03-21
Acknowledgments This research was partially supported by the National Key Research and Development Program of China (2018YFD1000800); the National Natural Science Foundation of China (No. 31872943; No. 31501779 and No. 31372059>); 12th Five-Year State Science and Technology Support Program (2014B
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In recent years several DPP
2022-03-21
In recent years, several DPP-IV inhibitors have already been approved, such as sitagliptin, vildagliptin, saxagliptin, tenegliptin, alogliptin and linagliptin, etc. Among them, linagliptin (1, Fig. 1) is a non-peptide mimetic Thymidine mg with a unique xanthine scaffold developed through high-throu
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Having shown that some of
2022-03-21
Having shown that some of substitutions (Cl, CF) at the 2-position of the thiophene improved rat microsomal stability, and polar groups at the 4-position of the aryl ring had a beneficial effect on stability in both human and rat microsomes, we combined these features in a new set of analogs. Methyl
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Several studies have indicated MUC to
2022-03-21
Several studies have indicated MUC1 to be an effective marker for identifying various malignant tumors, such as gastric, breast, pancreatic, ovarian, gallbladder, uterus, lung, and prostate cancers, as well as for prognostic outcomes [16], [17], [18], [19], [20], [21], [22], [23]. Studies by Kaira e
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Fpr which belongs the family of the
2022-03-21
Fpr1, which belongs the family of the formyl peptide receptors with FPRL1 and FPRL2, is the principal receptor for formylated peptides which prototype is the tri-peptide fMLF. Fpr1 is highly expressed on neutrophils and macrophages [6,30], promotes their migration into the mucosa and lumen in respon
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br Conclusions Symptoms from bilateral thalamic edema caused
2022-03-18
Conclusions Symptoms from bilateral thalamic edema caused by increased venous hypertension can be reversed with appropriate management of the inciting vascular lesion. This case demonstrates a rare patient with decreased CBF in the thalamus in SPECT and completely recovered after factor Xa inhib
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The synthesis of target compound
2022-03-18
The synthesis of target compound (RS)-C02 is illustrated as Scheme 2. Compound (RS)-3 was synthesized as reported procedures [40] and then reacted with ethyl piperidine-4-carboxylate to yield (RS)-C01, which subsequently was converted to target molecule (RS)-C02 by performing a nucleophilic substitu
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The NF B family of transcription factors is
2022-03-18
The NF-κB family of transcription factors is involved in acquisition of resistance to anticancer drugs as well as to apoptosis. NF-κB-mediated mdr1 gene upregulation is part of the anti-apoptotic protection mechanism of proximal tubule (PT) ITSA1 against cadmium-induced oxidative stress and apoptosi
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GSTP catalyzed reduction of Prdx enhances
2022-03-18
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 Pancuronium dibromide receptor to measure the influence of GSTP1 allelic variation on peroxidase activity. Specificity for detectio
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The beta catenin TCF complex is an important target
2022-03-18
The beta-catenin/TCF complex is an important target in the Wnt/beta-catenin pathway. This complex has proven challenging to target. However, natural inhibitors of this complex have been identified. One group of inhibitors is called the inhibitors of Wnt response (IWR-1/2). IWR-1/2 targets Axin and s
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A few research articles described that PLGA could alone impr
2022-03-18
A few research articles described that PLGA could alone improve physiological activities in certain illnesses by exerting therapeutic effects. These reported therapeutic activities of PLGA can be appended to the hydrolysis products of PLGA lactate, glycolate, and H+. We will recapitulate their respe
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rad51 inhibitor Here we show that lactate
2022-03-18
Here we show that lactate activates the Gi-coupled receptor GPR81, which is exclusively expressed on adipocytes, and that lactate released from adipocytes in response to glucose and insulin mediates insulin-induced antilipolysis by activation of GPR81. Results Discussion Nutrients and their m
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Several studies have proposed that high levels of KYNA in
2022-03-18
Several studies have proposed that high levels of KYNA in the mineralocorticoid receptor antagonists contribute to cognitive dysfunctions presented by patients who suffer from schizophrenia [30], [31], [32], [33]. Considering that: (i) KYNA is a known GPR35 agonist [2], (ii) cognitive impairments in
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No compounds in this series showed any
2022-03-18
No compounds in this series showed any appreciable activity at GlyT2 and can thus be considered GlyT1-selective. For the GlyT2 IC was >20μM. To determine CNS penetration of -(2-(azepan-1-yl)-2-phenylethyl)-benzenesulfonamides, select compounds were evaluated in a cassette CNS exposure screen in ma
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