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The synthesis of compounds a and b are outlined in
2020-09-21
The synthesis of compounds 7a and 7b are outlined in Scheme 2. Compound 5 was obtained by di-tert-butyl pyrocarbonate protection of bcr-abl inhibitor 4a. Then, compounds 6a and 6b were obtained by amination of the fluoride with a morpholino and dimethylamine, respectively. Target compounds 7a and 7b
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br Methods br Results br
2020-09-21
Methods Results Discussion To our knowledge, this is the first report to investigate the association between DBH genotype and pDβH activity in Han Chinese subjects. We also examined the relationship among DBH gene polymorphisms, pDβH activity and cognitive function in patients with schizoph
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DHODH activity has been traditionally measured with the stan
2020-09-21
DHODH activity has been traditionally measured with the standard colorimetric assay that monitors 2,6-dichloroindophenol (DCIP) reduction as absorbance decrease at 600 nm . This assay has permitted the identification of several families of DHODH inhibitors in a successful high-throughput screening (
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One possible explanation for differences in the binding
2020-09-21
One possible explanation for differences in the binding ability of monomeric versus dimeric forms of DDR2 ECD to collagen could be that the monomeric form only binds to the primary GVMGFO site, whereas dimeric (and oligomeric) DDR2 ECD binds to additional sites on the collagen triple-helical molecul
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Consistent with previous simulations on the DFG
2020-09-21
Consistent with previous simulations on the DFG-Asp-out/-in interconversion of Abl kinase, we only observe the DFG flip with protonated Asp747 (Shan et al., 2009). We showed previously that the pKa for the DFG-Asp in Abl is elevated at 6.5. Further “constant pH” simulations whereby protonation event
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Eukaryotic cell cycle machinery is thought
2020-09-21
Eukaryotic cell cycle machinery is thought to appropriately modulate cell proliferation and cell expansion in various developmental stages and environmental conditions. The core feature of cell-cycle control is the fluctuation of CDK activity, which is regulated by three interactive and conserved me
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Baicalin Our structures also provide new insights into CRTH
2020-09-19
Our structures also provide new insights into CRTH2 drug development. The ligand binding pocket revealed by our structures comprises many aromatic residues and a few polar residues at the distal end. Correspondingly, most CRTH2 antagonists share a similar structural feature characterized by an aceta
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Recently it was reported that Crm is
2020-09-19
Recently, it was reported that Crm1 is linked to spindle pole body (SPB) by Spc72 in cellular metabolism yeast [9]. Spc72 and Spc110 are two specific receptors of γ-tubulin complex (Tub4), which target Tub4 to SPB and mediate the nucleation of microtubules from SPB [20]. It was found that disruptin
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Previously we had proposed three possible models with
2020-09-19
Previously we had proposed three possible models, with one being that hCrm1 fundamentally interacted more favorably or strongly with Rev-RRE complex, compared to mCrm1. We decided to test that model, which was the simplest and most straightforward, by both biochemical and genetic means. By using bac
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The crystal structure of LiCoO is presented in
2020-09-19
The crystal structure of LiCoO2 is presented in Fig. 1. We can notice that the Li and Co atoms occupy the centers of two different edge-sharing [CoO6]-octahedra, which results in formation of separate Li and Co layers. Hence, the layered structure of LiMO2 is able to intercalate lithium into transit
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The regression also revealed a significant association betwe
2020-09-19
The regression also revealed a significant association between admission selectivity (SELECT) and exam pass rate (PASS%) (p 10-Hydroxycamptothecin serve as an indicator of a student’s ability to learn and their aptitude for academic success. These same qualities likely enable more selective schools
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Further studies are needed as continuation of
2020-09-19
Further studies are needed as continuation of this work to explore the effects of type and position of substituents of pyridazinone ring on anti-inflammatory activity profile. Taking into consideration that the phenyl moiety at position 2 wasn\'t a favorable substituent, even certain studies may be
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In this study we also conducted an
2020-09-19
In this study, we also conducted an analysis comparing the expression profiling of Hh genes among the sarcomas investigated. In these tumors, the IHH gene showed a higher expression level than PTCH1 gene in RMS and SS samples (pMG 149 receptor in human RMS cell lines as well as mouse NIH-3T3 fibrob
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In conclusion we designed novel E
2020-09-19
In conclusion, we designed novel E1 inhibitors based on the three-dimensional structure of E1 in complex with ubiquitin. Following an enzymatic assay evaluating synthetic compounds , , and , we identified compound as a novel E1 inhibitor. Comparing the inhibitory activity of compound with and ,
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The aim of the following work was to untap the
2020-09-19
The aim of the following work was to untap the potential of DIS as a low-cost substrate for fungal production of lignocellulolytic enzymes via SSF. Fungal strains with the ability to transform the unpretreated DIS to a mixture of industrially relevant lignocellulases were identified. Furthermore, th
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