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Although exhibited high inhibitory activity was found to be
2022-01-14

Although exhibited high inhibitory activity, was found to be metabolically unstable due to the hydrolysis of the phosphate group (data not shown), which prompted us to modify the phosphate moiety of . Comparison of the activities between three compounds bearing no or different spacer groups (, , a
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The Ala to Leu substitution would reduce the size of
2022-01-14

The Ala116 to Leu110 substitution would reduce the size of the active-site cavity disfavoring the production of longer allylic compounds as a result of steric hindrance, according to the observations of Poulter and co-workers [29], [30]. However, this explanation appears to be unlikely since several
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The VirScan assay has several
2022-01-14

The VirScan assay has several advantages over alternative multiplex serological assays for peptide discovery. These advantages include quantitative assessment of antibody binding to peptides that span all open reading frames in the HIV genome, including both structural and regulatory proteins; repre
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Two typical properties of Gi o
2022-01-14

Two typical properties of Gi/o protein-coupled receptors, namely an increase in 35S-GTPγS binding (Strange, 2010) and an inhibition of exocytotic noradrenaline release (Schlicker and Göthert, 1998), were not shared by H4 receptor activation on cortical membranes (guinea-pig and mouse) and cortical s
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Metallothioneins MTs that are intracellular proteins respons
2022-01-14

Metallothioneins (MTs) that are intracellular proteins responsible for the maintenance of metal homeostasis are involved in arsenic toxicity (Kita et al., 2006). Four major MT isoforms have been reported so far, MT1, MT2A, MT3 and MT4. The synthesis of MT1 and MT2A isoforms in mammal cells can be in
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On the basis of the structure of the Rab ACAP
2022-01-14

On the basis of the structure of the Rab35/ACAP2 complex, the authors identified Thr76 in switch II of Rab35 as one key specificity determinant (Lin et al., 2019). The crystal structure shows that the hydroxyl group of Thr76 forms a Amyloid Beta-Peptide (1-40) with Asp756 in ACAP2, while the methyl
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br Acknowledgments This research was
2022-01-14

Acknowledgments This research was partially supported by the National Key Research and Development Program of China (2018YFD1000800); the National Natural Science Foundation of China (No. 31872943; No. 31501779 and No. 31372059>); 12th Five-Year State Science and Technology Support Program (2014B
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PBI is an agonist of GPR and acts as
2022-01-14

PBI-4050 is an agonist of GPR40 and acts as an antagonist or inverse agonist of GPR84. It cannot be excluded that other targets besides GPR40 and GPR84 could be implicated in the mechanism of action of PBI-4050 and could be explored in future studies. However, the present study, and in particular th
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On the other hand it is quite
2022-01-14

On the other hand, it is quite possible that strychnine-sensitive glycine sites are responsible for mediating the anticonvulsant effects of GlyT1 inhibitors. Strychnine, which acts as an antagonist at these sites, is a well-known as a convulsant drug, and elevation of endogenous glycine levels at th
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GlxI is a member of the superfamily of proteins
2022-01-14

GlxI is a member of the βαβββ superfamily of proteins, consisting of fosfomycin resistance protein (FosA), methylmalonyl-CoA epimerase (MMCE), extradiol dioxygenase (DIOX), mitomycin C resistance protein (MRP) and bleomycin resistance protein (BRP) [29], [30], [31]. These proteins are believed to ha
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Besides the described effects on gross locomotor
2022-01-14

Besides the described effects on gross locomotor function, impairment of visuo-motor coordination and fine-motor skills like resting tremors, bradykinesia and rigidity were also investigated, reflecting on the symptomatology of Parkinson's disease in humans (Inzelberg et al., 2008). Preclinically, t
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At present many methods have been applied for multiple detec
2022-01-13

At present, many methods have been applied for multiple detection. For example, octopamine [[9], [10], [11]] is frequently used to detect multiple targets because of its exquisite sensitivity and specificity, but it is difficult to design experiments to test short-length oligonucleotides. Electroch
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We identified three genes KEAP
2022-01-13

We identified three genes—KEAP1, NAA38, and ABCC1/MRP1—as negative regulators of glutathione abundance in human cells. Like KEAP1, NAA38 appears to regulate NRF2 stability, as NAA38 deletion increased NRF2 protein levels and the expression of NRF2 target genes. NAA38 is a component of the NatC N-ter
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br Experimental br Acknowledgments We
2022-01-13

Experimental Acknowledgments We thank Mintek and Rhodes University for generous financial support and permission to publish these findings. T.O.O. gratefully acknowledges Obafemi Awolowo University, Ile-Ife, Nigeria for study leave. Introduction There are ∼35.3 million people living with H
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Saikosaponin A australia Recent studies have also identified
2022-01-13

Recent studies have also identified additional proteins that could act as scaffolds and promote the interaction of core Hippo pathway components. APC, which is best known as a key component of the β-catenin destruction complex, was observed in mammalian Saikosaponin A australia to have an additiona
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