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A recent analysis of urine samples collected from men
2019-09-30
A recent analysis of 2721 urine samples collected from 245 men and 408 women across the US general population between 2005 and 2010 showed that MP, PP and BuP were measurable in 99.9%, 98.3% and 73.6% of samples from women and 99.3%, 90.2% and 35.9% of samples from men, respectively (Smith et al., 2
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The development and activation of T
2019-09-30
The development and activation of T enkephalin clinical play an important role in the progression of atherosclerosis. As for activation and differentiation of T cells, TCR signalling pathway is pivotal. ZAP70 plays a crucial role in formulation of TCR–microclusters, initiation of TCR signalling pat
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Saxagliptin br Cytochrome P monooxygenases Cytochrome P mono
2019-09-30
Cytochrome P450 monooxygenases Cytochrome P450 monooxygenases (P450s) belong to one of Nature’s most versatile group of enzymes for C–H functionalization and are able to perform challenging regioselective and stereoselective activations of remote, unactivated C(sp3)–H bonds, for which there are o
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br Introduction Abdominal aortic aneurysm AAA is a daily
2019-09-30
Introduction Abdominal aortic aneurysm (AAA) is a daily concern in vascular surgery, as successful treatment is exclusively achieved by open or endovascular repair. Its prevalence is 2–11% among male smokers, and rupture the major complication, is associated with unacceptably high morbidity and m
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br Analytical improvements Since our review of Oxysterol Met
2019-09-30
Analytical improvements Since our review of “Oxysterol Metabolomes” in 2011 [7], there have been a number of improvements in analytical methods for the analysis of oxysterols and related compounds. McDonald and colleagues in Dallas have refined their LC-MS methods which are now applicable for ana
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E ligases provide substrate recognition specificity Ubiquiti
2019-09-30
E3 ligases provide substrate recognition specificity Ubiquitination Kartogenin and substrate specificity in mammals is achieved by the existence of over six-hundred E3-ubiquitin ligases that catalyze the final step of ubiquitination, compared with only one E1 and very few E2 enzymes known till dat
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br Deubiquitination deubiquitinases and cancer Protein deubi
2019-09-30
Deubiquitination, deubiquitinases and cancer Protein deubiquitination is reverse process of ubiquitination and performed by deubiquitinases or deubiquitinating enzymes (DUBs), which help in removal of ubiquitin from target proteins and involve in ubiquitin maturation, recycling and editing (Pfoh
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br Results br Discussion Many assays
2019-09-30
Results Discussion Many assays in the literature for DBH require the use of catalase to protect the active site from hydrogen peroxide, which is a by-product in the initial step of the reaction. For the non-immobilized enzyme there was a visible increase in the rate with increasing amounts of
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More recently Boskovic et al have
2019-09-30
More recently, Boskovic et al. (2003) have visually corroborated that purified DNA-PKcs can bind short DNA fragments by using single particle EM. DNA biotinylated at the 5′ end was labelled by coupling to commercial streptavidin–gold particles (Fig. 4D). When analysed in the microscope, DNA-PKcs mol
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br Inhibition of DHODH The final products a
2019-09-30
Inhibition of DHODH The final products 7a–n were assessed for their DHODH inhibitory activity on rat liver mitochondrial/microsomal membranes. A procedure adapted from the literature was employed (see Experimental), in which oxidation of DHO to ORO is monitored by following the concomitant reduct
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TH287 mass The aniline R group was extensively explored and
2019-09-30
The aniline R2 group was extensively explored and a large variety of substitution was tolerated at several positions on the aryl ring (). Notably, substitution at the 3-position often gave increased potency. Increasing lipophilic bulk at this position gave increasing potency within an ether series (
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In conclusion our work led to the
2019-09-30
In conclusion, our work led to the characterization of some signalling events of the CysLT1 receptor variants, at several levels, and showed that a punctual serine mutation could alter the response of receptors to cysLTs. Although atopy is a complex phenotype implicating different cell types, mediat
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Cy5 Firefly mass Perturbation in the cytokine network is cor
2019-09-30
Perturbation in the cytokine network is correlated with disruption of growth hormone and glucocorticoid (GC) homeostasis (Thissen and Verniers, 1997; Sahid El-Radhi et al., 2000; Waxman and Holloway, 2009; Zhao et al., 2014), with important physiological consequences because cytokines affect the reg
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thip Here we describe a novel series of arylazoderivatives d
2019-09-30
Here, we describe a novel series of arylazoderivatives developed from CAN508, one of the first known selective CDK9 inhibitors. We focused on modification of both ends of parental molecule, CAN508, in order to improve cytotoxicity and CDK activity. We therefore analyzed how changes in molecules will
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Compound A and Compound B Fig were found in
2019-09-30
Compound A and Compound B (Fig. 4) were found in our in vitro screening assays and have similar CRF1 receptor in vitro profiles (Table 1). When binding was investigated using [125I]-CRF in ex vivo assay, Compound A inhibited binding of [125I]-CRF both in the frontal cortex and the pituitary; however
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