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The lower number of samples tested for
2022-07-02
The lower number of samples tested for the comparison between cobas 4800 HIV-1 and RealTime HIV-1, especially at or below 50 copies/mL (Table 6), could limit our ability to discern a difference in the ability of the various assays to identify patients with virological failure. However, the 95% CI ar
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While phosphorylation site motifs are typically
2022-07-01
While L-Adrenaline site motifs are typically described in terms of residues that promote phosphorylation, negatively selected residues can also be an important component of substrate recognition. Such ‘forbidden’ resides can act as a filter to prevent phosphorylation of a site by the ‘wrong’ kinase,
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Having identified initial leads and further
2022-07-01
Having identified initial leads and (), further lead optimization was initiated on B- and C-rings to afford compounds with improved potency. Initial set of substituted imidazole-biphenyl-carboxylic bace inhibitors derivatives – and () were evaluated for GSNOR potency. Among this, fluoro, methyl,
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Any brain damage including that caused
2022-07-01
Any Rottlerin damage, including that caused by β-amyloid, triggers activation of microglia, the resident immune cells of the CNS. These cells cluster around amyloid plaques, in which they extend cytoplasmic processes (Combs, 2009). The significance of this response is controversial, but one possibil
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The diseases of ocular surface and the cornea
2022-07-01
The diseases of ocular surface and the cornea are very common in ophthalmological practice and as a result there is a continuous, need for novel therapeutic options. Here, we demonstrated a corneal distribution of GPR35, a potential molecular target for new drugs (; ). The search for the expression
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The occurrence of MDR in cancer patients
2022-07-01
The occurrence of MDR in cancer patients undergoing chemotherapy can be mimicked in the laboratory by culturing cancer Olaparib in the presence of chemotherapeutic drugs, thereby enforcing the evolution of acquired drug resistance. This has been described in multiple model systems including the rhab
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adrenergic antagonist br Endogenous lipids as SLC transporte
2022-07-01
Endogenous lipids as SLC6 transporter modulators Lipids constitute part of the environment in which membrane-embedded transporters operate [62]. Endogenous lipids can act as inhibitory ligands [63] or functionally important components of the membrane that impart changes in transporter structure
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br Acknowledgments We would like to acknowledge Jenna Hall M
2022-07-01
Acknowledgments We would like to acknowledge Jenna Hall, Marita Rivir, Kathleen Smith, Joyce Sorrell, and Emily Yates for assistance with in vivo pharmacology studies. We would like to acknowledge Joe Chabenne and Steph Mowery for assistance with in vitro cell-based assays, and Patrick J. Knerr f
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Different from stable transfection transient expression was
2022-06-30
Different from stable transfection, transient expression was also found to yield γ-secretase with robust proteolytic activity []. Co-transfection of all four, but not any three, components of human γ-secretase yielded high expression levels. This observation strongly suggests the co-folding nature o
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br Prospects The prospects for
2022-06-30
Prospects The prospects for GABAergic serotonin receptor can be projected from the rate at which new compounds have been introduced (Fig. 1) and the amounts used. More than three billion pounds of NCA-IA insecticides were used in the past seven decades. There was no target site cross-resistance
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The importance of T currents in the
2022-06-30
The importance of T-currents in the control of thalamic GABA synaptic function is also demonstrated by the presence of T-channel-dependent long-term synaptic plasticity, either potentiation (LTP) or depression (LTD). Indeed, in the associative posterior thalamic medial nucleus, an LTP of the GABAerg
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As a part of our continuing efforts towards discovery
2022-06-30
As a part of our continuing efforts towards discovery of new class of compounds against different therapeutic areas and based on the literature reports, we designed a dual pharmacophore which possess a long aliphatic chain of free fatty acids and a phenyl propanoid part of known GPR40 agonists. Here
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Considering the fact that NADPH oxidase is the main
2022-06-30
Considering the fact that NADPH oxidase is the main source for paraquat and maneb-induced oxidative stress, we hypothesized that NADPH oxidase activation might contribute to dopaminergic neurodegeneration induced by paraquat and maneb through ferroptosis. To test our hypothesis, we investigated the
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In conclusion a series of new carboxamido aryl isoxazoles wa
2022-06-30
In conclusion, a series of new 3-carboxamido-5-aryl-isoxazoles was designed, synthesized and screened for their inhibitory potency against FAAH. Their cytotoxicity was determined and their lipophilicity was calculated. Compounds bearing a 3-substituted biphenyl moiety with high Log values displayed
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The molecular formula of was determined to be C H
2022-06-30
The molecular formula of 2 was determined to be C20H26O5 on the basis of HRESI (−) MS data at m/z 345.1705 [M–H]− (calcd 345.1702 for C20H25O5). Detailed analysis of the 1H and 13C NMR data of 2 revealed similar fragments compared with desoxyarticulin (Faini et al., 1987) except for an additional hy
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