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br Authors contribution br Disclosure
2020-12-30
Authors contribution Disclosure statement Acknowledgements This study has received funding from the Italian Ministry of University and Research (PRIN 2015, grant number 2015373Z39_008) and from the Innovative Medicines Initiative 2 Joint Undertaking under grant agreement No 115797 (INNODIA)
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br Conclusions Present work comprehensively characterizes th
2020-12-30
Conclusions Present work comprehensively characterizes the inhibitory activity of Yersinia enterocolitica against cysteine proteases. All tested strains, regardless of their bioserotype, genotype and the presence of virulence markers, synthesized the high-molecular-weight inhibitors of papain and
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Further studies are needed as continuation of this work to
2020-12-30
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 r
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WRTs AI AI and AI showed the
2020-12-30
WRTs AI-82/1, AI-9-1 and AI-60 showed the same ST as was published by Dingle et al. in RTS 103, 013 and 097 (Dingle et al., 2011). WRTs 015 and 002 were assigned as WRTs 015-like and 002-like due to slight changes in their CE-ribotyping profiles; however, the ST of WRT 002-like (ST8) was identical t
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Rat pheochromocytoma PC cells have been widely used as a
2020-12-30
Rat pheochromocytoma PC12 cells have been widely used as a cell system to study intracellular signaling leading to neurite outgrowth. The advantages of using PC12 cells in the CHK studies are the fact that they naturally express the rat form of CHK and the observation that down-regulation of CHK fun
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In this study we investigated whether the Ednra signaling
2020-12-30
In this study, we investigated whether the Ednra signaling is involved in Hoxa9/Meis1-mediated leukemogenesis. We found an upregulation of Ednra in leukemic murine bone marrow (BM) NMS-E973 overexpressing Hoxa9 and Meis1 compared to cells overexpressing Hoxa9 alone. We showed that overexpression of
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Also important in binding of E to the ER
2020-12-30
Also important in binding of E2 to the ER is the hydroxyl on the D ring, which has a stabilizing contact with His-524 in ERα (Fig. 7) and with His-475 in ERβ (Fig. S1) [8,9,36,37]. The spatial relationship of the functional groups on the A and D rings on E2 has been used to develop chemicals contai
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At first cartilage damage in osteoarthritis reflects the los
2020-12-30
At first, cartilage damage in osteoarthritis reflects the loss of proteoglycan and collagen network that increases the swelling of tissues. The incremented expression of DDR2 receptor has also co-related with the depletion of cartilage in surgically induced OA model [8]. Osteoarthritis, a degenerati
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br Results and discussion br Conclusion
2020-12-30
Results and discussion Conclusion In the current study, a series of novel ‘open-chain’ classes of E. coli PDHc E1 inhibitors, N-acylhydrazone pyrimidine derivatives A, B, and C were designed and synthesized. As novel ThDP analogs, all A displayed moderate to powerful inhibitory activity with I
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The cyclin dependent kinase deactivation is
2020-12-29
The cyclin-dependent kinase deactivation is carried out by a particular group of proteins cyclin-dependent kinase inhibitors (CDKIs). These group of proteins blocks kinase activity by interfering with the interaction of cyclin-CDK complex [43]. The inhibition of CDK naturally occurs during a G1 phas
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Beside the previously reported Topo
2020-12-29
Beside the previously reported Topo I inhibition, time and concentration dependent CRM1 inhibitory properties of klavuzon derivatives have been shown as a second mechanism of action in this work. Especially, compounds 3 and 20 are the most effective derivatives and they completely inhibit CRM1 activ
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Flexible alignment of isopropylphenylaminobenzimidazole with
2020-12-29
Flexible alignment of 7-isopropylphenylaminobenzimidazole 16 with the lead cdc42 inhibitor 1 was performed using MOE. It was found that the aryl group of compound 16, exemplified as a yellow circle in Figure 2, overlapped well with the corresponding alkyl chain of compound 1 as well as the other ke
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For any vector let and For let The information
2020-12-29
For any vector , let , and . For , let The information matrix for the partial likelihood at Eq. (2.2) can be expressed as It is well known that opioid receptor under certain regularity conditions such as (A)–(D) in Andersen and Gill (1982), where and denote the maximum likelihood estimator fr
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br Conclusions br Acknowledgements br Protein tyrosine kinas
2020-12-29
Conclusions Acknowledgements Protein tyrosine kinases (PTKs) of Src family are important components in cellular signal transduction pathways that couple diverse extracellular signals to appropriate cellular responses . Their activities are tightly regulated in the cells and aberrant activati
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br Results and discussions In general experimental analysis
2020-12-29
Results and discussions In general, experimental analysis is time consuming and expensive. Thus, In the present study, Taguchi design of experiments (DOE) was adopted to reduce the number of trials. To analyze the data, a High Level Analysis (HLA) is performed by averaging measured data for each
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