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Midazolam oral clearance is used for characterization of bot
2020-07-02
Midazolam oral clearance is used for characterization of both intestinal and hepatic CYP3A activity. However, the identification and subsequent use of metabolic markers of CYP3A activity can eliminate the need for unnecessary administration of probe drugs such as midazolam. Such metabolic markers wo
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Several evidences showed that seizures increase brain
2020-07-02
Several evidences showed that seizures increase brain extracellular glutamate, which binds to N-methyl-d-aspartate (NMDA) receptor, then up-regulated cyclooxygenase-2 (COX-2) expression in brain capillaries to increase BBB P-gp expression [11,13,29,30]. A recent study demonstrated a different signal
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iox As we all known hypoxia is a hallmark of tumour
2020-07-02
As we all known, hypoxia is a hallmark of tumour microenvironment, which is a key regulator of tumour growth and metastasis [4]. Hypoxia meditates a series of cellular responses including angiogenesis by activating transcriptional factor hypoxia inducible factor (HIF), which is consist of an obligat
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Chloroquine As described above we designed and synthesized a
2020-07-02
As described above, we designed and synthesized a new 1,4-di-substituted isoquinoline lead compound, and was identified as a ligand with moderate potency for the CRTH2 receptor. We initially we examined the effects of the steric factor of R group on the CRTH2 binding potency (). When the methyl grou
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Introduction The inflammation process involves sequential ac
2020-07-02
Introduction The inflammation process involves sequential activation of signaling molecules, pro-inflammatory mediators, such as prostaglandins, leukotrienes, and oxygen free radicals [1]. Two cyclooxygenases Cisplatin were responsible for activation of the production of prostaglandins (PG1s) and
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When women reach the menopause they
2020-07-01
When women reach the menopause they experience a number of physical complaints such as hot flushes, vaginal dryness and mood changes [1]. Bone loss also becomes manifest at this time [1], [2], but women will often not suffer from back pain before a vertebral fracture occurs. Women who have had one f
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The discovery of proteases that are active in organic
2020-07-01
The discovery of proteases that are active in organic solvent media has greatly extended their ability in the synthesis of useful products. Microbial proteases which are able be catalyse in non-aqueous solvents present new expectation in enzyme applications. This kind of enzymes gives a major contri
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br EBV BILF A Virus Encoded TM Receptor
2020-07-01
EBV-BILF1—A Virus-Encoded 7TM Receptor with Immune Evasive Functions The EBV-encoded BILF1 receptor (EBV-BILF1) is thought to be implicated in the immune evasion strategy of EBV.56, 61, 62 This orphan 7TM receptor is expressed at significant levels during the early lytic phase of the virus infect
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Although many GPCR heteromers have been identified using het
2020-07-01
Although many GPCR heteromers have been identified using heterologous cell lines, only very few fit all three criteria. This is mainly due to the difficulties to study these structures in native tissues because of the lack of sensitive and selective tools, not only capable of detecting in vivo evide
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Moreover recent structural studies of VEEV nsP pro in comple
2020-07-01
Moreover, recent structural studies of VEEV nsP2pro in complex with E-64d revealed an important molecular interaction at the interface of two subdomains. In this structure, Asn475 which is in polar contact with carbonyl oxygen of Asp507 of the protease subdomain makes an H-bond with Arg662 of the MT
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Cystatins are potent inhibitors of cysteine proteases from t
2020-07-01
Cystatins are potent inhibitors of cysteine proteases from the C1A family. These inhibitors primarily reduce the activities of cathepsin L-like proteases, although high concentration of barley cystatin hampers the degradation of storage proteins caused by cathepsin F-like protein (HvPap-1) (Cambra e
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In this study we characterized the
2020-06-30
In this study, we characterized the metabolic function of tra2 in the Drosophila fat body. Similar to the 9G8 phenotype, decreasing tra2 levels in the Drosophila fat body using RNAi resulted in increased starvation resistance and a large increase in triglycerides. This increased storage of triglycer
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The goal of this paper is to investigate the
2020-06-30
The goal of this nmda antagonist paper is to investigate the penalized empirical likelihood method for the Cox model, as a competitor to the penalized partial likelihood. Since empirical likelihood (EL) was proposed by Owen, 1988, Owen, 2001, empirical likelihood methods have been investigated well
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The absence of an observable time dependence of kobs
2020-06-30
The absence of an observable time dependence of kobs on inhibitor concentration for histone acetyltransferase 3 with AChE and compounds 1, 3 and 4 with BuChE parallels a similar absence of time dependence for some related fluoro ketones with AChE. Nair et al. found that trifluoromethyl acetophenones
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The question remains however as to the downstream signaling
2020-06-30
The question remains, however as to the downstream signaling by Epacs that contributes to persistent sensitization of sensory neurons. Activation of the Ras family of GTPases by Epac1 (RapGEF3) or Epac2 (RapGEF4) (Bos, 2003, de Rooij et al., 1998) is linked to a number of downstream signaling effect
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