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Till date several predictive models have been
2021-01-08
Till date, several predictive models have been developed by different research groups to speed up the process of library selection and drug optimization (Walters et al., 1999, Caldwell, 2000, Plewczynski et al., 2006, Wang and Ramnarayan, 1999, Pogorelcnik et al., 2015, Greenbaum et al., 2002, Sadow
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Kuo et al Have shown that DAPK function in
2021-01-08
Kuo et al. (2006) Have shown that DAPK1 function in inhibiting microtubule (MT) assembly is through the activation of microtubule affinity-regulating kinases (MARK)/PAR-1 family kinases MARK1/2, which destabilize MT by phosphorylating tau and related MAP2/4. This relation with DAPK1 has demonstrated
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br Results br Discussion GPCRs
2021-01-08
Results Discussion GPCRs recognize a broad range of molecules with a vast chemical M 1145 through different mechanisms. Our understanding of the recognition of lipid mediators by GPCRs primarily comes from the structural studies of receptors for lysophospholipids and endocannabinoids including
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Other mutations in the SYNE region exons
2021-01-07
Other mutations in the SYNE1 3′ region (exons 81–85) have been implicated in an upper motor neuron disease, ARCA1 (Gros-Louis et al., 2007). The disease is characterized by progressive movement, coordination, and balance problems caused by disrupted Purkinje cell function and their impaired signalin
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Peptides undergoing only a single hydroxylation i e PA Hyp
2021-01-07
Peptides undergoing only a single hydroxylation, i.e. PA-Hyp-KPAPK and PAPK-Hyp-APK, were then used to investigate the kinetics of vCPH co-factor and co-substrate dependences. The values for KMapp for Fe(II) and KM for 2OG for the two peptide substrates were within error (KMapp, Fe(II): 0.9 μM ± 0.1
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To develop novel EPAC inhibitors
2021-01-07
To develop novel EPAC inhibitors, Zhou and co-workers optimized the HTS hit as the chemical lead. After modifications of the substituents on the phenyl ring or C6-position of compound , compound () was identified to be the more potent compound in this series with an IC value of 4.0µM (EPAC2). Dock
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It is well known that acrolein
2021-01-07
It is well known that acrolein, a metabolite of cyclophosphamide, is responsible for the cyclophosphamide-induced cystitis, and that acrolein is capable of activating TRPA1 channels expressed in the capsaicin-sensitive primary afferents [2], [11]. In this context, it is likely that the early phase o
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Future advances in the in vivo molecular imaging
2021-01-07
Future advances in the in vivo molecular imaging of enzyme activity will greatly benefit from the progress towards the quantitative detection of enzymes. Quantitative imaging requires knowledge of both the location and concentration of a specific enzyme, which is dependent on the simultaneous measur
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Although DP technologies are convenient for users to manufac
2021-01-07
Although 3DP technologies are convenient for users to manufacture devices automatically, the printing materials are inevitably limited by the manufacturers of 3D printers. Strategies are increasingly being developed to functionalize the raw printing materials or their printed devices with other phys
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br Chondroitin sulfate proteoglycans CSPGs are major compone
2021-01-07
Chondroitin sulfate proteoglycans (CSPGs) are major components of the extracellular matrix in cartilage. Each CSPG comprises a single core protein and attached chondroitin sulfate (CS), belonging to the glycosaminoglycan family of sugar chains. CSPGs and CS are involved in numerous biological and
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Introduction CYP is a superfamily of heme containing monooxy
2021-01-07
Introduction CYP450 is a superfamily of heme-containing monooxygenases, many of which are expressed in the liver, and they are significant phase-I XL184 australia in drug metabolism and detoxification. There are three subfamilies (CYP1, CYP2 and CYP3) that are mainly involved in the metabolism of
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While PRRSV has been recently shown to
2021-01-07
While PRRSV has been recently shown to induce SGs, the exact nature of SG formation and its underlying mechanism of regulating antiviral immune response during PRRSV infection remain unclear (Zhou et al., 2017). Formation of PRRSV-induced SGs was observed in MARC145 BI-1356 (Chen et al., 2018) and P
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br Materials and methods br Results
2021-01-07
Materials and methods Results and discussion Conflict of interest Acknowledgments This work was supported by grants from National 973 Project (2015CB755700) and the Doctoral Starting up Foundation of Henan University of Science and Technology (13480033). Introduction Progression thro
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In contrast to SQLE HMGCR could be efficiently
2021-01-07
In contrast to SQLE, HMGCR could be efficiently degraded in (R)-baclofen receptor lacking UBE2J2. However, this was not the case in cells devoid of UBE2G2, as these cells were unable to support 25-hydroxycholesterol (25-HC)-stimulated degradation of HMGCR (Fig. 1C). This finding is consistent with o
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Several reports have exploited the application of HRM
2021-01-07
Several reports , , , , have exploited the application of HRM for detecting differentially methylated DNA. Even though DNA methylation analysis by HRM cannot determine the methylation status of individual CpGs, it does provide a robust and inexpensive method to differentiate DNA based on the overal
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