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Firstly the impact on activity and selectivity was made by
2021-12-28
Firstly, the impact on activity and selectivity was made by replacing the 2, 3-di-F substitution of ring A with 2,3-OCHO- () and 2-NO () substitutions, and replacing the 3, 5-di-F substitution of ring B with 3,5-di-OMe () and 3,5-di-Me () substitutions. Compound kept moderate activity (EC = 220 nM)
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The mD plasmid containing CD domain
2021-12-28
The mD1.2 plasmid containing CD4 domain 1 gene under the control of a promoter was obtained as a gift from Dr. Dimiter S. Dimitrov. The mD1.2 plasmid was digested using restriction endonuclease I (New England BioLabs, USA) to release the mD1.2 gene. The gene encoding the mD1.2 protein was elongated
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Compared to methadone or morphine
2021-12-28
Compared to methadone or morphine, buprenorphine is a partial mu-opioid agonist, which shows high affinity for, and slow dissociation from, mu-opioid receptors. This maintenance of homeostasis may help to counter the development of an overt withdrawal syndrome, and may explain the lower risk of deve
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Finally the formation of a regular network of
2021-12-28
Finally, the formation of a regular network of fusion glycoproteins in their post-fusion state is not exclusive of vesiculovirus G. More or less regular networks have been also observed with other class III fusion glycoproteins such as pseudorabies gB [85] and several class II fusion glycoproteins [
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Post translational ubiquitination has been shown
2021-12-28
Post-translational ubiquitination has been shown to regulate a wide range of cellular responses, such as the synaptic trafficking and turnover of neurotransmitter receptors (Rape, 2018). Ubiquitination is also engaged in the modification of protein-protein interaction and intracellular signaling tra
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Further explorations at the ortho and meta positions of
2021-12-28
Further explorations at the ortho- and meta-positions of the phenyl in the tail proceeded on the basis of the preliminary results. First, we investigated the fluorine group at the meta- (13p) and ortho-positions (13q) of the phenyl group, with both compounds being slightly less potent than 13o. Surp
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br Materials and methods br Results
2021-12-28
Materials and methods Results Discussion In the CNS, GLP-1R is associated with G-protein signal transduction pathways, which can activate adenylyl cyclase and protein kinase A by cyclic adenosine monophosphate, and mediates neuronal activities implicated in various pathophysiological change
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br Material and methods br Results br Discussion Functional
2021-12-28
Material and methods Results Discussion Functional characterization of naturally occurring GCK mutations in patients with impaired glucose homeostasis has widened our knowledge of the catalytic and regulatory mechanisms of this enzyme [3]. In this work, we have biochemically characterized a
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Acknowledgements br Introduction Alzheimer s disease
2021-12-27
Acknowledgements Introduction Alzheimer's disease (AD) is a devastating neurodegenerative disorder and the leading cause of dementia. There is currently no treatment available to slow or halt disease progression. The underlying mechanisms of AD on the cell and molecular levels are still not comp
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FGF signals can be transduced to the signaling cascades
2021-12-27
FGF signals can be transduced to the signaling cascades of RAS-MAPK or PI3K-AKT through FRS2 and GRB2, to the pathways of PKC or PKD via PLCγ and DAG, and to Ca2+-releasing cascade via PLCγ and IP3, finally affecting cellular proliferation, cellular survival, and angiogenesis [48]. By increasing syn
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In order to estimate the influence
2021-12-27
In order to estimate the influence of mitochondrial hypo-polarization on generated OMP, IMP was changed from the normal value of Δψi = −140 mV (Fig. 4A, D, G) to Δψi = −100 mV (Fig. 4B, E, H), resulting in lower magnitudes of calculated OMP for hypo-polarized dopamine antagonist (Fig. 4B). Similarl
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G P also plays a critical
2021-12-27
G6P also plays a critical role in regulating HK2 binding to mitochondria. Elevated levels of intracellular G6P weaken HK2 binding to mitochondria, causing the enzyme to translocate to the cytoplasm and facilitate anabolic glucose metabolism. Acidosis similarly induces HK2 translocation from mitochon
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Metal organic frameworks MOFs have emerged over the past two
2021-12-27
Metal–organic frameworks (MOFs) have emerged over the past two decades with the potentials to act as promising materials in gas storage, chemical separation, catalyst, magnetism, sensing, and drug delivery etc (Du et al., 2013, Zhou and Kitagawa, 2014). Additionally, the secondary interactions, such
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Eastern Guangdong is a Teochew dialect area We found that
2021-12-27
Eastern Guangdong is a Teochew dialect area. We found that subtype 1b (3.1%) in this region was significantly lower than in other areas. Subtype 1b began its spread from the central part of China out into the whole country through illegal blood donation in the mid-1990s (Lu et al., 2013) and is now
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Here we investigate the structural and
2021-12-27
Here we investigate the structural and biochemical properties of the N-GTPase domain of p190RhoGAP-A. We determine the crystal structure and find that N-GTPase adopts an extended GTPase-like fold with six unique inserts that seem to preclude its ability to bind typical GAP, GEF, or am680 molecules.
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