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ASA 404 As shown in Table the results
2021-10-14
As shown in Table 3, the results of individual prediction modeling with chemicals at 0.4 mM, 0.6 mM, and 0.8 mM would lead to lesser sensitivity of 60.0%, 65.0%, and 65.0%, respectively, in microsome-unused group, and 85.0%, 85.0%, and 90.0%, in microsome-used group. If we consider only the results
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br Materials and methods br Results and
2021-10-13
Materials and methods Results and discussion Conclusions Notes Declaration of interest statement Acknowledgment This work was supported by the National Natural Science Foundation of China (No. 21775132, 21505112), Scientific Research Foundation of Hunan Provincial Education Departm
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The inhibitory activities of new compounds against
2021-10-13
The inhibitory activities of new compounds against P. aeruginosa were determined in both DTSB media supplemented with heme or free iron and LB media (Table 1). The MIC50 values of the compounds ranged from 42 to 260 μg/mL in DTSB medium and from 26 to 230 μg/mL in LB medium. Among these new inhibito
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Toc and Toc are GTPases that regulate
2021-10-13
Toc34 and Toc159 are GTPases that regulate initial steps of preprotein import [3,4,26]. It was shown that GTP hydrolysis of at least one receptor is necessary to initiate the translocation process [23,27]. As reported for other small G-proteins, Toc34 and Toc159 bind their cargo in a nucleotide-depe
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Compstatin The expression of COX has been correlated with th
2021-10-13
The expression of COX-2 has been correlated with the density of amyloid plaque [65]. A study reported that IMX was effective in suppressing the expression of iNOS and IL-6, but not COX-2, in LPS-stimulated BV2 microglial cells [52]. In this study, IMX did not alter upregulation of COX-2 induced by H
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br Lactate metabolism L Lactate
2021-10-13
Lactate metabolism L-Lactate is an intermediate metabolite in glucose metabolism. Glucose can be broken down to pyruvate, and pyruvate can be either further oxidized to acetyl-CoA and enter the TCA cycle, or reduced to L-lactate by lactate dehydrogenase (LDH). In turn, LDH can oxidize L-lactate t
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A general synthetic pathway to these
2021-10-13
A general synthetic pathway to these tricyclic structures is described in (detailed procedures can be accessed in the patent application WO 2011/014520 A2). Benzylation of the appropriate ketoester using KHMDS, followed by treatment with DMF-dimethyl acetal yielded the racemic (dimethylamino)-methyl
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In recent large clinical studies AIM HIGH and HPS
2021-10-13
In recent large clinical studies, AIM-HIGH and HPS2-THRIVE, the additional treatment of nicotinic x04 to statin-based LDL-C lowering therapy did not decrease the major vascular events on the patients who had atherosclerotic vascular diseases [43,44]. In the AIM-HIGH study, the secondary analysis sho
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br MUTYH associated polyposis br MUTYH and its metal
2021-10-13
MUTYH-associated polyposis MUTYH and its metal cofactors MUTYH harbors two vital cofactors, both of which are located remotely from the active site (Fig. 6). One of these cofactors, a [4Fe-4S]2+(Fe-S) cluster, is chelated by four Cys residues in the N-terminal domain, and positions an Fe-S clu
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Also considered very rare is progressive encephalomyelitis
2021-10-13
Also considered very rare is progressive encephalomyelitis with rigidity and myoclonus (PERM); sometimes called Stiff Person Syndrome Plus (SPS Plus) and with antibodies to glutamic Diphenyleneiodonium chloride decarboxylase (GAD). However, PERM is now increasingly found with glycine receptor antib
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Glutamate aspartate transporters or excitatory amino acid tr
2021-10-13
Glutamate-aspartate transporters or excitatory amino 17 aag transporters (EAATs) are essential for the maintenance of glutamate homeostasis. EAATs are widely distributed in central neurons and glial cells (Danbolt, 2001, Martinez-Lozada et al., 2011). They are driven by Na + and K+ gradients (Jiang
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A number of GCK activators for treating
2021-10-13
A number of GCK activators for treating T2D have been developed and tested but not progressed successfully from clinical trials into therapy [45]. Our observations suggest that increased risk of hypoglycemia might be possible, particularly if drugs penetrate into brain. A further possibility is that
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For the two KO models
2021-10-13
For the two KO models (CX30 and CX43), fluorescence recovery is almost always best fitted with a 2-component exponential (Fig. 6A and D). Statistical analysis of the parameters (Table 1) shows that in both cases the two time scales and the fraction of recovery associated with the fast intracellular
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We next determined the selectivity profile of
2021-10-12
We next determined the selectivity profile of the most potent GPR40 agonists (4k–n) against other free fatty (R)-baclofen receptors (FFA3/GPR41, FFA2/GPR43 and FFA4/GPR120). FFA2 and FFA3 agonists have a preference in binding short-chain fatty acids while FFA1 and FFA4 have a higher affinity to med
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Andexanet alfa works as a decoy for
2021-10-12
Andexanet alfa works as a decoy for the FXa inhibitor to bind to irreversibly. The recently completed ANDEXA-4 trial, which was a prospective, open-label, single group study, found that patients achieved good or excellent hemostasis in 82% of subjects [, , ]. There was an overall 10% thromboembolic
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