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The phenolic hydroxyl group of ezetimibe tolerated various s
2019-12-02

The phenolic hydroxyl group of ezetimibe tolerated various structural modifications (disaccharide, carboxyalkyl and glucuronide) that retained inhibitory activity.13, 14, 15 We conjugated glycylglycine to phenolic hydroxyl group and synthesized ten 1H-pyrrole-2,5-dione derivatives 14a-j successfully
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HG-10-102-01 Oral antipsychotics are substrates of CYP enzym
2019-11-30

Oral antipsychotics are substrates of CYP450 enzymes, which are crucial to their metabolism and elimination (Fig. 1). The efficacy and toxicity of antipsychotic agents is affected by factors that induce or inhibit CYP450 expression and function, such as drug–drug interactions. Additionally, the mult
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Moreover a ligand for fusin has recently been found the
2019-11-30

Moreover, a ligand for fusin has recently been found: the lymphocyte chemoattractant stromal-derived factor-1 (SDF-1) binds to CHO Indacaterol Maleate transfected with fusin and promotes secondary messenger production (Bleul et al., 1996; Oberlin et al., 1996). A new name, CXCR-4, has been proposed
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In our preliminary evaluation of
2019-11-30

In our preliminary evaluation of this series, we were surprised to discover that Ciclopirox ethanolamine mg was found to bind CSF-1R in a classical DFG-in binding mode (a). Dramatic conformational differences in the juxtamembrane domain and activation loops are apparent when this DFG-in structure
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br Material and methods br Results br Discussion In
2019-11-30

Material and methods Results Discussion In vitro evidence indicates that LAS191859 is a potent CRTh2 antagonist as demonstrated in GTPγS binding studies with potency in the low nanomolar range and in addition it demonstrates a long receptor residence time. This potency is also maintained in
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Different types of environmentally induced antinociception h
2019-11-30

Different types of environmentally induced antinociception have been reported in a wide range of species (e.g., Behbehani, 1995, Bolles and Fanselow, 1980, Harris, 1996, Millan, 2002, Rodgers, 1995). According to Bolles and Fanselow (1980), fear and pain are independent and competing motivational sy
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Cubic equations of state CEoS are particularly popular due t
2019-11-30

Cubic equations of state (CEoS) are particularly popular due to their simplicity and relatively good accuracy in predicting vapour-liquid equilibrium and liquid-liquid equilibrium for small, non-polar, non-associating molecules, such as light hydrocarbons. CEoS can match the phase boundaries (L/LL a
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Our study revealed elevated basal Akt phosphorylation in die
2019-11-30

Our study revealed elevated basal Akt phosphorylation in diet-induced obesity, the effect of which was reversed by ETAKO. Activation of Akt promotes cardiac hypertrophy via a number of cellular mechanisms including activation of its downstream targets such as mTOR and GSK3β [45, 46]. Short-term acti
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The most significant finding was the inhibition
2019-11-30

The most significant finding was the inhibition of EROD and BFCOD activity by CLO. Inhibition of EROD and BFCOD were reversible, as pre-incubation did not enhance CLO inhibitory potency, and no reductions in IC50 values were observed. We further characterized the kinetic pattern of inhibition using
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In normal cells the apoptotic stimuli lower the expression
2019-11-30

In normal cells, the apoptotic stimuli lower the expression level of antiapoptotic proteins by increasing turnover rate and preventing the constant degradation of proapoptotic proteins. Thus, the dysregulation of anti-/pro-apoptotic proteins will confer the survival of cancer bafilomycin a1 via enh
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CAA is a carcinogenic metabolite of vinyl chloride forming
2019-11-30

CAA is a carcinogenic metabolite of vinyl chloride, forming several different DNA adducts including the cyclic cx 4945 adducts 3,N4-ethenocytosine (εC), 1,N6-ethenoadenine (εA), N2,3-ethenoguanine (εG), and 1,N2-ethenoguanine (1,N2-εG), with the A and C cyclic adducts the most predominant, and all
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beta lactamase inhibitor The anticholinesterase activities o
2019-11-29

The anticholinesterase activities of all subfractions derived from EtOAc extract were detected and summarized in . Fraction 5 and its resulting subfractions (5B, 5C, 5D, 5C3, 5C4, 5D3, and 5D4) were found to show attractive activities. Subsequently, ten compounds (–) were obtained from these active
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Soybean Glycine max is an important
2019-11-29

Soybean (Glycine max) is an important oilseed and can be a useful source of epoxy fatty acids (EFAs). This UFA contains an oxygen bridge across adjacent carbon atoms at single or multiple positions in the acyl chain, making them highly reactive and prone to cross-linking, and thus valuable industria
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br Materials and Methods br
2019-11-29

Materials and Methods Acknowledgements Introduction Collagen fibrillogenesis, the assembly of collagen fibers, is a critical process in the development, maturation, and repair of mammalian tissue. Alterations in the structure and amount of deposited collagen fibers can greatly alter the int
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br Materials and methods br Author contributions br Acknowle
2019-11-29

Materials and methods Author contributions Acknowledgements Supported by grants from the Zhejiang Provincial Natural Science Foundation (LY16H030016, LY17H030012), and the Zhejiang Science and Technology Public Welfare Project (2015C33279), Anesthesiology Center in North of Zhejiang Provinc
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