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Although many factors influence the effects
2024-01-29
Although many factors influence the effects of medications, during recent years it has become evident that genetic factors could explain the differences between individuals in drug response. These differences are due to variants in genes encoding drug targets [8]. The challenge for pharmacogenetics
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Akt is another upstream kinase known to phosphorylate AMPK
2024-01-29
Akt is another upstream kinase known to phosphorylate AMPK Ser489 in response to high insulin levels [7], [21]. HepG2 AGI-5198 show an increase in phosphorylation of AMPK at Ser485 when incubated with either insulin or troglitazone individually (Fig. 5A and C). Despite this concurrent increase, onl
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Nx rats feces collected in nd week th
2024-01-27
5/6Nx rats’ feces collected in 2 nd week, 4 th week, 6 th week, 8 th week and 10 th week were tested by 16S rDNA sequencing. The 16S rDNA sequencing data was analyzed in the level of PHYLUM, CLASS, ORDER, FAMILY and GENUS. There are more than 1000 types of gut microbiota in the level of Genus [50],
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br Materials and methods br Results br Discussion br
2024-01-27
Materials and methods Results Discussion Competing financial interests Acknowledgements The work was partially supported by grants from the National Natural Science Foundation of China (Grant no. 31530053 and 31401424) and National Science and Technology Support Plan (Grant no. 2013BA
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br Funding This work was supported
2024-01-27
Funding This work was supported by Arena Pharmaceuticals, Inc, San Diego, CA, USA. Introduction 5-hydroxytryptamine 1B (5-HT1B) receptors are widely distributed in the central nervous system (CNS); they have various modulatory functions in drug reinforcement, appetitive behaviors, stress, moo
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In vitro studies with soman inhibited non aged AChE
2024-01-27
In vitro studies with soman-inhibited, non-aged AChE revealed a species dependent reactivating potency of HI-6 and MMB-4. With guinea pig AChE second order reactivation rate constants of 0.051 and 0.038mM−1min−1 were determined for HI-6 and MMB-4, respectively (Luo et al., 2007). Corresponding value
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From our in vivo studies and
2024-01-27
From our in vivo studies and previously reported findings [25], we have found that orteronel possesses excellent oral BA. Indeed, single oral dosing of orteronel at doses of 0.3–10.0mg/kg decreased serum DHEA levels in a dose-dependent manner. Of interest, DHEA levels did not return to levels compar
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Pyrimidine is the important pharmacology
2024-01-27
Pyrimidine is the important pharmacology core in many Aurora inhibitors, such as VX-680, ENMD-2076, CYC-116 and ENMD-2076 [12]. To identify additional effective Aurora inhibitors, we designed a series of 2,4-diaminopyrimidine compounds, our modeling studies suggested that the Amoxapine sale core as
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br Aurora A Aurora B and Aurora C small molecule
2024-01-27
Aurora-A, Aurora-B and Aurora-C small molecule inhibitors Nicholas et al. described phenotypic cellular screening of new highly potent and selective class of Aurora kinase inhibitors. Fragment based approach was utilized; core structure of 57 (Fig. 5) was optimized and selective inhibitor 58 (Fig
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The enzyme Arginase ARG plays a role
2024-01-26
The enzyme Arginase 1 (ARG1) plays a role in the hepatic urea cycle by hydrolyzing L-arginine to L-ornithine and urea [13]. In the context of macrophages and MDSCs, ARG1 expression redirects L-arginine metabolism to abolish cytotoxic nitric oxide production [14], suppress T-cell function [15], [16],
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br Drugs with documented pro apoptotic effects on platelets
2024-01-26
Drugs with documented pro-apoptotic effects on platelets More than 200 drugs are reported to cause thrombocytopenia [5,42]. The concept of platelet apoptosis is relatively new and was only recently evaluated in the context of drug-induced thrombocytopenia [43]. Table 2 lists the drugs presently k
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Apelin induced G i activation has been
2024-01-26
Apelin induced Gαi activation has been demonstrated as a benefiting effect on cardiac contractility [12], [38], [39], and a vasodilator activity that protects against angiotensin-II-induced cardiovascular fibrosis and atheroma [40], [41]. In contrast, stretch causes hypertrophy through diminishing G
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Hsp also called FK binding protein FKBP is one of
2024-01-26
Hsp56 (also called FK506-binding protein 52, FKBP52) is one of the steroid receptor-associated immunophilins with tetratricopeptide repeat domains, which serve as binding sites for Hsp90 (Peattie et al., 1992). Hsp56 is elevated in breast cancer compared with normal breast tissue (Ward et al., 1999)
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The major phase trial NCT enrolled
2024-01-26
The major phase 2 trial (NCT01343966) enrolled 431 participants with mild to moderate AD who received either low-dose SC crenezumab 300 mg or placebo biweekly (n = 184) or high-dose intravenous crenezumab 15 mg/kg or placebo every 4 weeks (n = 247) for 68 weeks 38, 40. No significant treatment benef
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iwr br Experimental section br Abbreviations PSA puromycin s
2024-01-26
Experimental section Abbreviations PSA, puromycin–sensitive aminopeptidase; APN, aminopeptidase N; AML, acute myeloid Leukemia; ALL, acute lymphoblastic leukemia; AADR, amino iwr deprivation response; PAN, puromycin aminonucleoside; DCC, dicyclohexyl carbodiimide; NHS, N–hydroxy succinimide;
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