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An ideal CHK inhibitor would be minimally cytotoxic while en
2021-03-02
An ideal CHK-1 inhibitor would be minimally cytotoxic, while enhancing the anti-tumor effect of a real cytotoxic agent that would be used in combination with the inhibitor. Our CHK-1 inhibitors have shown excellent selectivity over a panel of kinases including those regulating the cell cycle, but th
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Glycolysis is important to maintain
2021-03-02
Glycolysis is important to maintain the vital functions of T. gondi. Extracellular T. gondii shift its Asunaprevir metabolism towards glycolysis, based on the observation that a relocation of glycolytic enzymes from the cytosol to the pellicle occurs at the time when tachyzoites egress from host c
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Next we compared the protease specificity of viruses NS GFP
2021-03-02
Next, we compared the protease-specificity of viruses NS116-GFP/AE and NS116-GFP/AT for trypsin, neutrophilic elastase or supernatant of human neutrophils. For later purposes, we determined the viral yield in a co-cultivation system of infected Vero phosphatidylinositol 4-kinase with human neutroph
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When six chemical inhibitors were incubated
2021-03-02
When six chemical inhibitors were incubated with TRB or TRC and human liver microsomal preparation, HLM2, the results showed that ketoconazole (a CYP3A4 inhibitor) was very effective in inhibiting 4β-C hydroxylation of TRB and TR, whereas sulfaphenazole (a CYP2C9 inhibitor) and quinidine (a CYP2D6 i
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Consistent with our previous study Gao et al b
2021-03-02
Consistent with our previous study (Gao et al., 2018b; Wu et al., 2018), we found that TCB-2 disrupted both pup preference and home-cage maternal behavior. Based on the findings that 4-h pup fiin (a technique presumably increases maternal motivation) failed to attenuate the TCB-2-induced maternal d
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The HPV E proteins are
2021-03-02
The HPV E7 proteins are acidic oncoproteins of approximately 98–103 blasticidin that contain 3 domains: the conserved region (CR) 1, CR2, and the carboxyl terminal (C-terminal) domain. The CR1 domain is necessary for cellular transformation and RB degradation in mucosal high risk HPVs. The CR2 domai
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We further verified the presence of CLIC CLIC
2021-03-02
We further verified the presence of CLIC1, CLIC4 and CLIC5 in purified mitochondria following protocols described earlier (Singh et al., 2012). As shown in Fig. 4, CLIC4 and CLIC5 were present in the ultra-pure mitochondrial fraction (M3). All the three fractions obtained from 30% (v/v) Percoll grad
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The inhibition of CYP activity by NOR
2021-03-02
The inhibition of CYP11β activity by NOR was 11- and 2.5-fold higher than those reported for the antifungal agents ketoconazole (IC50: 4.4μM) and clotrimozole (IC50: 1.0μM) (Fernandes and Porte, 2013). Furthermore, NOR was able to inhibit P450 aromatase activity in carp ovaries, although at a rather
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In countries such as China where there is a
2021-03-02
In countries such as China where there is a high commercial production of rice, the use of rice husk ash (RHA) as an alternative cementing material can become a great asset for environmental rehabilitation and address the difficult disposal issues associated with this agricultural waste [23]. RHA po
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br Halogenases Enzymatic C H activation leading to halogenat
2021-03-02
Halogenases Enzymatic C–H activation leading to halogenation is another emerging area in biocatalysis [55,56]. Incorporation of halogen atoms during medicinal chemistry eff ;orts is a well-established practice, presenting an effective means to control the molecule’s bioactivity and physicochemical
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beauty spot We also note that though the deletion
2021-03-01
We also note that though the beauty spot of the N-terminus in Ube2E1∆N46 or the mutations in Ube2E16KtoR enhanced their activity compared to the wild type, it failed to match Ube2D2 (Fig. 1). We concluded this difference to be multi-factorial as none of the Ube2E1∆N46 point mutants involving “Ub bac
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Mulan is one of three E ubiquitin ligases that are
2021-03-01
Mulan is one of three E3 ubiquitin ligases that are present in the mitochondria along with MARCH5/MITOL (membrane associated RING-CH5) and RNF185 [14], [15], [16], [17]. Mulan is a 352-residue polypeptide that crosses the mitochondrial outer membrane (OMM) twice, its amino-terminus, which includes t
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br Fragment based drug discovery FBDD is
2021-03-01
Fragment-based drug discovery (FBDD) is a powerful method to discover drug leads and has been widely adopted in both academia and industry. FBDD can be used to explore chemical AZD 0530 space with libraries which are smaller in size, producing drug leads with high ligand-binding efficiency. It al
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The genomic DNA sequences of CXCL and
2021-03-01
The genomic DNA sequences of CXCL8 and CXCRs were retrieved from the fugu genome database v4.0. The intron–exon boundaries were identified with the corresponding cDNA sequences. This comparison revealed that the fugu gene is about 1.13kb long and contains four exons separated by three introns (top p
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The results of bisaryl ether linker study
2021-03-01
The results of bisaryl ether linker study are shown in . It was found that the methylene linker () moderately improved the binding to the DP receptor. The increased binding potency was also diminished in the presence of plasma, possibly due to higher plasma protein binding. Other linkers, such as th