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It is believed that emphysema in smokers
2021-03-23
It is believed that emphysema in smokers is mediated by proteases released from inflammatory 2-D08 that cause destruction of the extracellular matrix in alveolar septa [1]. Metalloprotease-12 is mainly released by macrophages and is considered the enzyme responsible for emphysematous lesions in exp
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The Kaempferia parviflora extract met the criteria for a
2021-03-23
The Kaempferia parviflora extract met the criteria for a non-competitive interaction with CYP1A1 based on the decrease of Vmax and unchanged Km. The high Ki value and low IC50, as well as the high Km value was indicative of the weakness of the interaction between the Kaempferia parviflora extract an
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br Acknowledgments br Multicellular organisms respond rapidl
2021-03-23
Acknowledgments Multicellular organisms respond rapidly, and adapt to cellular stress to maximize cell survival. The cellular stress response, also called (ISR), is universally conserved and independent of the stressor. ISR induces rapid, transient reprogramming of cellular protein translation
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The authors identified inhibitors of
2021-03-23
The authors identified inhibitors of SUMOylation using two assays to monitor the conjugation of SUMO1 to RanGAP1 by E1 and E2 enzymes: a fluorescence resonance energy transfer (FRET) primary screen that evaluated over 250,000 compounds and a chemiluminescence secondary screen. A counter screen was u
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br DGKs bind and regulate other signalling proteins Based on
2021-03-23
DGKs bind and regulate other signalling proteins Based on the evidence noted above, DGKs achieve specificity of function through a combination of post-translational modifications, the availability of cofactors, and through the availability and access to substrate DAG. DGKs appear to achieve an ad
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Of the acidic hydroxyazoles involved hydroxypyrazole had the
2021-03-23
Of the acidic hydroxyazoles involved, hydroxypyrazole had the weakest acidic profile (pKa in the range of 6–7), although highly deprotonated at physiological pH. During hit optimization, the two pyrazole ring positions available for substitution provide an opportunity for a better exploration of the
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Substituents at the C position An oxygen containing substitu
2021-03-23
Substituents at the C11 position — An oxygen-containing substituent at the C11 position also affects the catalytic activity of Δ1-KSTDs. The Δ1-KSTDs from the Gram-positive bacteria R. equi [29], N. simplex ATCC 6946 and IFO 12069 [48,49,52], and R. rhodochrous IFO 3338 [27] were able to 1(2)-dehydr
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An increasing body of evidence demonstrates that MXC can cau
2021-03-23
An increasing body of evidence demonstrates that MXC can cause neurobehavioral and neuropathological alterations [7]. In the brain, there are several steroidogenic enzymes, which are responsible for neurosteroid production. Neurosteroids are subsets of steroids that rapidly change neuronal excitabil
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br Results br Discussion Thus
2021-03-23
Results Discussion Thus, the biochemical and structural studies of six Maf proteins from different organisms have revealed two subfamilies of new enzymes with the metal-dependent nucleoside triphosphate pyrophosphatase activity against both canonical and noncanonical pyrimidine nucleotides (Yh
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We next considered the mechanism of
2021-03-23
We next considered the mechanism of the hepatospecific decrease in CYP3A exerted by EGCG. We examined the possibility that orally administered EGCG was absorbed from the intestine and directly decreased the CYP3A expression level in the liver. Although the DC_AC50 receptor rate of orally administer
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It is important to note
2021-03-22
It is important to note that CRF1 may be activated during acute stress and early phases of anxiety disorders (Coric et al., 2010, Ising et al., 2007), as well the administration of Astressin 2B into the lateral septum did not have an effect on anxiety-like behavior in low-stress conditions but had a
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Several highly selective COX inhibitors coxibs have
2021-03-22
Several highly selective COX-2 inhibitors (coxibs) have been reported and marketed [6], including celecoxib [7] and etoricoxib [8] (Fig. 1). Even though these drugs produce less ulceration than conventional NSAIDs, coxibs still produce significant gastric and cardiovascular side effects due to the d
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Recently several Pt IV complexes as prodrugs have been desig
2021-03-22
Recently, several Pt(IV) complexes as prodrugs have been designed and studied to enhance anti-tumor efficacy of traditional Pt(II) drugs, improving their cellular uptake and blood-circulation time [26], [27], [28], [29]. Compared with their Pt(II) counterparts, six-coordinated Pt(IV) complexes with
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The evaluation of internal exposure in workers
2021-03-22
The evaluation of internal exposure in workers with omethoate is challenging. Unfortunately, OPs are metabolized and excreted quickly in the urine usually within 24–48 h of exposure, and the variation in metabolic rates exists. Many factors influence daily urinary output, such as salt intake, urea a
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br Materials and methods br Results We
2021-03-22
Materials and methods Results We examined the effects of curcumin in Fluo-4 loaded SH-EP1 Sulindac stably transfected with human α7-nACh receptor. Application of curcumin alone in the concentrations up to 100 μM for 30 sec. did not induce any detectable change in intracellular Ca2+ levels in
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