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br Conclusions In this paper we
2020-11-06

Conclusions In this paper we describe the recombinant expression and characterization of ParI, a C5-DNA-MTase from P. arcticus 273–4. To our knowledge, this is the first characterization of an orphan C5-DNA-MTase from a psychrophilic bacterium. The C5-DNA-MTase could not be expressed in regular E
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Cell migration and invasion are
2020-11-06

Cell migration and invasion are central processes in the development and metastasis of cancer. The regulation of cell migration by DDR1 has been reported in many types of cancer cell lines; however, conflicting results have been reported regarding the inhibitory as well as promotive effects of DDR1
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p Kip is a critical component of the cell cycle
2020-11-06

p27Kip1 is a critical component of the cell cycle machinery [15]. As an inhibitor of cyclin E-Cdk2, p27Kip1 plays a pivotal role in controlling cell proliferation, S-phase entry, and G1-phase exit during development and tumorigenesis [16]. p27Kip1 is predominantly regulated via posttranslational mod
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Prenylation may turn a flavonoid
2020-11-06

Prenylation may turn a flavonoid from an agonist to an antagonist and improve the selectivity to both ERs depending on the position of the substitution. C-8 prenylation appears to promote antagonism to a larger extent than C-6 in ERα due to steric hindrance against generation of agonistic conformati
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Binding affinity was measured by a scintillation proximity b
2020-11-06

Binding affinity was measured by a scintillation proximity binding assay using [H]4-OHT (ERRγ) or [H]estradiol (ERα/β) as radioligand. In all cases, the ERβ affinity was not significantly different from ERα. Compounds were compared to , which showed high affinity for both receptors and moderate (six
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br Material and methods br Results and discussion
2020-11-06

Material and methods Results and discussion Conclusions Prostanoid-E receptor selective antagonists that inhibit EP2 or EP4 receptor activities may be used as a pharmacological strategy to limit cyst formation and ADPKD progression. Our study follows on from our previous observations of the
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br Acknowledgements This work was financially supported by I
2020-11-06

Acknowledgements This work was financially supported by Industrial Technology Institute, Sri Lanka through funds received from Sri Lankan Government Treasury (TG13/69). G. D. Liyanaarachchi received postgraduate research scholarship grant from National Science Foundation Sri Lanka (NSF/SCH/2017/0
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br Results br Discussion The ubiquitin
2020-11-06

Results Discussion The ubiquitin system has in recent years become an exciting area for drug discovery (Cohen and Tcherpakov, 2010), as multiple enzymatic steps within the ubiquitylation process are druggable. The potential of targeting the ubiquitin-proteasome pathway was first demonstrated i
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Increasing evidence supports that the
2020-11-06

Increasing evidence supports that the B-cell lymphoid malignancies develop from various stages of B-cells, hijacking the mechanisms that drive B-cell differentiation and activation [27]. For instance, mantle cell lymphoma (MCL) and chronic lymphocytic leukemia (CLL) originate from the pre-germinal c
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Protein degradation via UPP involves two steps
2020-11-06

Protein degradation via UPP involves two steps. One step is the conjugation of multiple ubiquitin to a substrate. The other step is the degradation of tagged protein by the downstream 26S proteasome complex. Protein ubiquitination is the E1–E2–E3 enzymatic cascade (Hershko & Ciechanover, 1998). E1-a
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We have previously reported DAPK
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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To date the role of CRF and CRF
2020-11-05

To date, the role of CRF and CRF1+ neurons within the amygdala in the expression of anxiety-like behavior and conditioned fear, and the place where these cell populations fit into the fear-related microcircuitry already identified in the CeA, have not been fully characterized. Recent evidence suppor
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Accumulated evidence indicates that apelin plays a
2020-11-05

Accumulated evidence indicates that apelin plays a protective role in ischemic stroke, contributing to post-stroke recovery (Yang et al., 2014; Chen et al., 2015; Xin et al., 2015; Yan et al., 2015). Apelin gene (APLN) encodes prepro-apelin with 77 amino acids, while the C-terminal 23 SB408124 sale
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br Discussion Variable estradiol effects
2020-11-05

Discussion Variable estradiol effects on cell proliferation have been reported according to animal species, tissues, and type of estrogen receptor [16,21,22,[29], [30], [31]]. In the kidney, 17βE was found to increase [3H]-thymidine incorporation in primary rabbit kidney proximal tubule 520 3 [30
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In addition to the ESIs identified that target both EPAC
2020-11-05

In addition to the ESIs identified that target both EPAC1 and EPAC2, ESI-05 and ESI-07 were identified as compounds that selectively antagonise EPAC2, displaying almost no inhibition of EPAC1 at concentrations up to 100μM [99]. Both compounds were effective inhibitors EPAC2 GEF activity towards Rap1
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