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br Casein Kinase II CK Casein Kinase II
2020-11-09
Casein Kinase II (CK2) Casein Kinase II (CK2) is a ubiquitous serine/threonine-selective pro-oncogenic protein kinase that has become a more prominent target for research due to its effects and key role in tumorigenesis (Gowda et al., 2017a, Pinna, 2002). CK2, a well-conserved, pleiotropic kinase
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br Results and discussion br
2020-11-09
Results and discussion Conclusion In this investigation, pharmacophore models of CK1 inhibitors were developed using a pharmacophore modeling protocol proposed by us. The optimal pharmacophore hypothesis, Hypo2, was adopted to retrieve potential CK1 inhibitors from the commercial chemical data
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The inhibition of CYP activity by NOR was and
2020-11-09
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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br In addition to the classic
2020-11-09
In addition to the classic nuclear genomic action, estrogens have been found to induce rapid effects occurring within minutes following administration. These effects are mediated through a subpopulation of estrogen receptors associated with the plasma membrane, a process usually termed “membrane-i
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By using live imaging of an ERK
2020-11-09
By using live imaging of an ERK fluorescence resonance energy transfer (FRET) sensor, the authors show that ERK activity propagates in a stepwise manner from the center to the periphery of the tracheal placode. This row-by-row propagation of ERK activity fits a relay model in which each row activate
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Apoptosis Inhibitor receptor The work described by Dong Grov
2020-11-09
The work described by Dong, Groves, and co-workers (11) tested the hypothesis that neural stem cell development is sensitive to the clustering and mechanical state of the EphB4:ephrin-B2 receptor-ligand complex. They show that the quality of ephrin-B2-ligand signaling depends on its biophysical stat
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Just as Dorin et al
2020-11-09
Just as Dorin et al. [2] and Nguyen et al. [3] write in regard to their models, our static model can be used to estimate the affinities of A769662 to albumin and CBG. Dorin et al. [2] estimates the K, but not K, since they find that their model is not particular sensitive towards changes in K. Our s
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900 80 mg Introduction Myclobutanil MCL RS chlorophenyl H tr
2020-11-09
Introduction Myclobutanil (MCL), (RS)-2-(4-chlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)hexanenitrile (Fig. 1), is a broad-spectrum systemic triazole fungicide with protective, eradicative, and curative action (University of Hertfordshire, 2018). It is employed to control pests such as powdery mild
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br Introduction The Epstein Barr virus
2020-11-09
Introduction The Epstein–Barr virus induced gene 2 (EBI2 also known as GPR183) is a G protein-coupled seven-transmembrane (7TM) receptor that is predominantly expressed in B and T cells [1,2]. It regulates the trafficking of ethionamide within lymphoid tissues and is highly important for the gen
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MuRF interacts with four and a half LIM
2020-11-09
MuRF3 interacts with four-and-a-half LIM domain (FHL2) and γ-filamin leading to their degradation via UPS [64]. Conversely, abnormal aggregation of these proteins was observed in mice lacking MuRF3. Moreover, MuRF3-/- mice were found more prone to cardiac rupture after acute myocardial infarction (A
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br Acknowledgements This work was supported by
2020-11-09
Acknowledgements This work was supported by National Natural Science Foundation of China (No. 81400241). Introduction Fluoride, as a member of the halogen group of elements, naturally existed in water, soil, animals, and plants around the world (Singh et al., 2018), and it is present in trace
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A range of inhibitors were therefore synthesized containing
2020-11-06
A range of inhibitors were therefore synthesized containing either carboxylic glucagon like peptide or ester functionality at the ‘tail’ group as well as variations in the ‘head.’ These were assayed in vitro using the DCIP assay for binding affinity against and human DHODH at 50μM, respectively ().
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Targeting both PARP and DHODH for anti cancer therapy would
2020-11-06
Targeting both PARP-1 and DHODH for anti-cancer therapy would certainly be beneficial as these enzymes share a common role in the DNA replication and repair mechanisms which are involved in the hyper-proliferation of cancer cells. Since benzimidazole-containing compounds have been reported to show
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Keratin K has been identified as the first intermediate
2020-11-06
Keratin 8 (K8) has been identified as the first intermediate filament expressed during development in amphibians and mammals. In zebrafish, a type II cytokeratin 8 (zf-K8) cDNA has been cloned. zf-K8 gene was maternally inherited and expressed in all surface cells throughout the embryonic stages old
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notch inhibitor We have previously reported DAPK inhibitors
2020-11-06
We have previously reported DAPK inhibitors discovered through our structure-based virtual screening (SBVS) research program. In this paper, we describe the general protocol of our in silico approach, and the strategy used to develop hit compounds. In addition, the studies conducted on the structure
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