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CHR2797 Dipeptidyl peptidase inhibitors DPP is or gliptins s
2019-08-28
Dipeptidyl peptidase-4 inhibitors (DPP-4is or gliptins) stimulate both post-meal insulin secretion and inhibit CHR2797 secretion in a glucose-dependent manner, rendering the risk of hypoglycaemia minimal [10]. They are weight-neutral or may even induce slight weight loss. Their good efficacy has be
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Calpeptin The other interesting observation made during this
2019-08-28
The other interesting observation made during this study relates to the differences between the discrete IR-induced γH2AX foci and the robust H2AX phosphorylation observed during apoptotic DNA fragmentation. The pattern of H2AX phosphorylation observed during DNA fragmentation possibly reflects the
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Herein in continuation of our interest in designing new DNA
2019-08-28
Herein, in continuation of our interest in designing new DNA photocleavage agents [18], we report the synthesis, characterization and DNA binding and cleaving properties of a novel compound: trans-N,N-dimethyl-10,11-di(pyridin-4-ium)-10,11-dihydro-9,12-dioxobenzo[e]phenanthrene tetrafluoroborate (1)
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Multiple sequence alignment of the proteins in the
2019-08-28
Multiple sequence alignment of the proteins in the DGAT1 sub-family shows that there are about 41 conserved amino channel modulator residues distributed over seven sequence motifs [74]. Unlike DGAT2, a large number of DGAT1 residues, including a majority of the conserved residues, are found in a lo
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We found that both DDR and
2019-08-27
We found that both DDR1 and DDR2 ECD increased matrix mineralization as compared to native cells, with the effect of DDR2 ECD being more prominent. Both soluble (DDR2/ECD) and membrane-bound DDR2 ECD (DDR2/-KD), when compared to wild-type cells, induced larger mineral deposits. In this regard, a re
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br Conclusions br Acknowledgements br Protein tyrosine kinas
2019-08-27
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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Therefore HNE is an attractive therapeutic
2019-08-27
Therefore, HNE is an attractive therapeutic target and the design of new HNE inhibitors is a demanding field that has been extensively investigated in order to provide inhibitors with new molecular architectures, including the potent oxo-β-lactam class [14]. In the present work, a coumarin-based oxo
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br Results br Discussion Many studies have
2019-08-27
Results Discussion Many studies have shown that intrinsic properties of the E2 enzyme govern the nature of the Ub modification, including both the multiplicity of the Ub modification and the specific Manumycin A kinase type in the case of polyubiquitin chains [3], [4], [9], [14]. Whereas previ
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Mulan is one of three E ubiquitin ligases that
2019-08-27
Mulan is one of three E3 ubiquitin ligases that are present in the mitochondria along with MARCH5/MITOL (membrane associated RING-CH5) and RNF185 [14], [15], [16], [17]. Mulan is a 352-residue polypeptide that crosses the mitochondrial outer membrane (OMM) twice, its amino-terminus, which includes t
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br Results br Discussion Adaptive drug resistance is a
2019-08-26
Results Discussion Adaptive drug resistance is a major challenge to the clinical success of cancer therapies. Incomplete inhibition of oncogenic signaling allows survival of “drug-tolerant” tumor cells, which persist in that state for variable periods before acquiring additional genetic mutati
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As illustrated in Table monocyclic acid analogs were synthes
2019-08-26
As illustrated in Table 3, monocyclic toll like receptors analogs were synthesized and evaluated. 2-Oxido-3H-1,2,3,5-oxathiadiazol analog 8 showed 15-fold less potent EP1 receptor affinity relative to 2b, while it showed 2.2-fold more potent antagonist activity. Oxadiazole-5-one analog 9 exhibited n
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Interestingly our analyses of human PBMCs using
2019-08-26
Interestingly, our analyses of human PBMCs using a monoclonal antibody against EBI2 showed that the expression pattern of human EBI2 is largely overlapping with that in mice. Especially Th17 Lauric Acid pathway showed homogeneous high expression of EBI2 compared with Th1 cells, which contained a fra
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It was reported that the
2019-08-26
It was reported that the expressions of DPP-4 and SDF-1α increase through HIF-1α [27], [28]. Myocardial ischemia by MI enhanced the DPP-4 and SDF-1α levels in myocardium in the present study. SDF-1α is released from cardiomyocytes and has beneficial effects on cardiomyocytes through SDF-1α/CXCR4 aft
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br Experimental methods br Results and discussion br Conclus
2019-08-26
Experimental methods Results and discussion Conclusion Rational design of highly selective fluorescent probes to detect G-quadruplexes is of profound importance for basic research. On this basis, we designed and synthesized a series of N-alkylated styrylquinolinium dyes Ls-1, Ls-2 and Ls-3.
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Studies of LRRK tagged with green fluorescent
2019-08-26
Studies of LRRK2 tagged with green fluorescent protein revealed the presence of monomeric LRRK2 in the TCS PIM-1 1 of living cells, while LRRK2 oligomers were found in the proximity of the plasma membrane, suggesting that both oligomerization status and compartmentalization of LRRK2 defines its fun
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