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br Materials and methods br Results Table presents
2024-04-13
Materials and methods Results Table 1 presents the metabolic phenotype of obese minipigs. After 60 d of HFHS feeding, minipigs not only showed an increased body weight (+45%), but also a perturbed Praziquantel mg homeostasis, with higher insulin levels (about +2-fold), HOMA-IR (+5.5-fold), an
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Sertraline HCl Application of the broad acting HTR
2024-04-13
Application of the broad-acting 5-HTR antagonist methiothepin (Bard et al., 1996, Hoyer et al., 1994, Peroutka, 1990) converted the TBS-induced response of both thalamocortical and intracortical A1 synapses from LTP to LTD, an effect that was mimicked by the selective 5-HT2R antagonist ketanserin (L
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Toxicity is the main reason for the failure at all
2024-04-13
Toxicity is the main reason for the failure at all stages of the new drug development process. The major part of safety-related attrition occurs at preclinical phases while predicting preclinical safety liabilities earlier in the drug development process. This strategy enables the design and/or sele
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The srd a isoforms showed unique expression profiles in earl
2024-04-13
The srd5a isoforms showed unique expression profiles in early FHM development (Fig. 2). Similar to amphibian embryos, there was a high abundance of both srd5a1 and srd5a3 at 1dpf in FHMs, suggesting that mRNA for these enzymes may be maternally deposited and that these enzymes may play a key role in
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At present drugs that specifically inhibit YAP activity are
2024-04-13
At present, drugs that specifically inhibit YAP activity are not available. In fact, verteporfin, which was originally described as a specific inhibitor of YAP-TEAD interaction, has been recently shown to exert its activity through selective induction of proteotoxicity rather than through YAP inhibi
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Matthew et al synthesized and carried out SAR studies
2024-04-13
Matthew et al. synthesized and carried out SAR studies of imidazo-[1,2-a]-pyrazine as Aurora kinase inhibitors with enhanced kinase selectivity and found that (+)-Apogossypol 39 showed optimal potency on Aurora-A and Aurora-B with IC50 value of 4 nM and 13 nM while on phosphorylation histone H3 (pH
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br Acknowledgments and Disclosures br
2024-04-12
Acknowledgments and Disclosures Introduction Over the last decade, the most visible strategy for the treatment of Alzheimer's disease (AD) has been amyloid β peptide (Aβ) immunotherapy (reviewed in [1]). Although the first efforts with Aβ immunotherapy failed to complete clinical trials [1], A
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We have recently begun to
2024-04-12
We have recently begun to demonstrate this concept by reporting a novel class of β-hairpin peptidomimetics, built on a piperidine-pyrrolidine semi-rigid β-turn inducer [12] and bearing two recognition pentapeptide sequences, designed on oligomeric and fibril structures of Aβ1-42 (compound 1, Fig. 1)
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A has been reported to decrease insulin receptors
2024-04-12
Aβ has been reported to decrease insulin receptors and impair insulin signaling in neurons, preventing phosphorylation of Akt and glycogen synthase kinase 3β (GSK-3β), downstream of insulin signaling, and to increase phosphorylation of tau protein causing neurofibrillary tangles (Tokutake et al., 20
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Chlorpromazine HCl In this study we demonstrated that DRR pr
2024-04-12
In this study, we demonstrated that DRR1 protein level in GBM tissues was significantly higher compared to normal Chlorpromazine HCl tissues. This data suggested that DRR1 might play a role in the tumorigenesis of glioma. To investigate whether DRR1 could accurately predict the outcome in patients w
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shows the synthesis of imidazole intermediates and The key p
2024-04-12
shows the synthesis of imidazole intermediates , , and . The key precursor keto aldehyde – was prepared in situ by SeO mediated oxidation of corresponding carbonyl compounds and or hydrolysis of dibromo ketone . Subsequent treatment with -Boc piperidine-4-carbaldehyde in the presence of aqueous
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Introduction hydroxytryptamine HT is found throughout the bo
2024-04-12
Introduction 5-hydroxytryptamine (5-HT) is found throughout the body and influences smooth muscle activity in various tissues including the intestine, vasculature and urinary ciprofloxacin receptor (Kim and Camilleri, 2000, Klarskov and Horby-Petersen, 1986, Mohammad-Zadeh et al., 2008). The curren
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Adenosine can modulate neutrophil bactericidal functions A d
2024-04-12
Adenosine can modulate neutrophil bactericidal functions. A dual regulatory effect has been reported for adenosine on phagocytosis. Indeed, the activation of A1 receptors augments this process, while the stimulation of A2A receptors was found to reduce the phagocytic activity of neutrophils [89]. In
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br Introduction Adenosine deaminase ADA also known
2024-04-12
Introduction Adenosine deaminase (ADA), also known as adenosine aminohydrolase, is a key enzyme involved in the purine metabolism that converts adenosine to inosine irreversibly (Lupidi et al., 1997). It is a zinc containing metalloenzyme present in both prokaryotes and eukaryotes. In humans ADA
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Both subcutaneous s c and mucosal administration
2024-04-12
Both subcutaneous (s.c.) and mucosal administration of short synthetic peptide derivatives of AChR prevent the onset of EAMG, but do not treat ongoing EAMG [80], [81], [82], [83], [84], [85]. The selection of peptides for treatment is mainly based on the identification of immunodominant T- and B-cel
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