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In this paper we report the
2019-10-22
In this paper, we report the synthesis and microbiological evaluation of a series of novel chromogenic sugar-based enzyme substrates based upon catechol, 2,3-dihydroxynaphthalene and 6,7-dibromo-2,3-dihydroxynaphthalene 9 cores (Fig. 1).14, 15 2,3-Dihydroxynaphthalene is inexpensive and available i
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Preliminary studies suggest that dimerization of the
2019-10-22
Preliminary studies suggest that dimerization of the AT1 receptor occurred during the biosynthesis in the endoplasmic reticulum before surface expression [27,40], which may explain the presenece of these ep4 receptor before the addition of any ligand. Our results showed that the presence of Ang II
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verapamil hydrochloride In general cellular senescence is co
2019-10-22
In general, cellular senescence is considered a programmed response to stress that can be activated by oxidative stress, irradiation or action of substances or drugs. These stressors cause DNA damage and, through the action of specific proteins (p53 and p21), lead to cell senescence (di Fagagna, 200
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Introduction The number of patients with type diabetes is in
2019-10-22
Introduction The number of patients with type 2 diabetes is increasing globally, and has become a serious public health problem. Type 2 diabetic patients exhibit a higher risk of bone fracture [1]. In addition, clinical studies have indicated that increased fracture risk is associated with long-ter
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From the general synthetic route we first
2019-10-21
From the general synthetic route, we first synthesized a directed set of analogues of general formula , keeping the synthesis simple by using a symmetrical pyrazole (R=R=Me). The SAR of a set of 30 compounds in the GTPγS binding assay turned out to be quite tight: only 4 (13%) compounds showed moder
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Imatinib Bcl functions as a transcription repressor via
2019-10-21
Bcl6 functions as a transcription repressor via its N-terminal BTB domain and middle “second repression,” or “RD2” domain (Chang et al., 1996, Seyfert et al., 1996). A loss of function of the BCL6 BTB domain markedly impairs survival and proliferation of mature GC Imatinib in a B cell intrinsic man
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br Experimental section br Author contributions
2019-10-21
Experimental section Author contributions Acknowledgements Introduction Many Allopurinol sale in cells are sequential enzymatic reactions where the product of one enzyme serves as the substrate of a second enzyme (1, 2). Experimental evidence suggests that some of these consecutive enzy
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ApicomplexansApicomplexans are unicellular and spore
2019-10-21
ApicomplexansApicomplexans are unicellular and spore-forming obligate intracellular parasites that occupy diverse host niches (Mogi and Kita 2010). They have remodeled mitochondrial carbon and energy metabolism through reductive evolution. The development of novel drugs is now a very serious challen
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br Results and discussion br Conclusion Novel and selective
2019-10-21
Results and discussion Conclusion Novel and selective aziridine-based inhibitors for the Leishmania mexicana protease LmCBP2.8 were discovered. Compounds 7d (Ki = 0.8 μM), 9d (Ki = 1.36 μM), 12d (Ki = 0.77 μM), 14d (Ki = 0.9 μM) and 18 (Ki = 0.441 μM) showed the highest potency and selectivity
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OU749 Based on our studies presented
2019-10-21
Based on our studies presented above, atipamezole can be used as a new in vitro and in vivo tool OU749 as a pan-CYP inhibitor for CYP mediated metabolism study. It carries many unique characteristics compared to ABT which is currently being widely used for this purpose. These new characteristics in
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br Materials and methods br
2019-10-21
Materials and methods Results Discussion TP has aroused extensive explorations because of its potent anti-inflammatory, immune-suppressive and antitumor activities. Notwithstanding these, TP has yet to enter Phase II clinical trials owing to its severe toxicity (Zhou et al., 2012). TP could
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As the COMT enzyme is primarily related to
2019-10-21
As the COMT enzyme is primarily related to prefrontal dopamine degradation (e.g., Yavich et al., 2007), the present study supports the notion that prefrontal dopamine modulates retention of fear extinction rather than within-session extinction (Abraham et al., 2014). Consistent with other studies we
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In the present study we investigated the effect of morphine
2019-10-21
In the present study we investigated the effect of morphine withdrawal on G-protein coupling to opioid and ET receptors in neonatal rats. Morphine-induced G-protein activation was significantly higher in neonatal rats undergoing morphine withdrawal; suggesting enhanced coupling of the receptors to G
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alpha adrenergic blockers br Introduction Cell transplantati
2019-10-21
Introduction Cell transplantation therapies using embryonic stem cell (ESC) and induced pluripotent stem cell (iPSC)-derived retinal tissue (ESC/iPSC retina) or alpha adrenergic blockers have emerged as therapeutic options for retinal degeneration following recent breakthroughs. A number of grou
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Estrogen related receptors ERRs are orphan nuclear receptors
2019-10-21
Estrogen-related receptors (ERRs) are orphan nuclear receptors and have three members including ERRα, ERRβ, and ERRγ (Yasumoto et al., 2007). Though they are termed as ERRs due to the sequence homology with estrogen receptors, they don’t need to bind estrogens to exert action. Generally, ERRs bind t
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