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The aniline R group was extensively explored and
2019-07-05
The aniline R2 group was extensively explored and a large variety of substitution was tolerated at several positions on the aryl ring (). Notably, substitution at the 3-position often gave increased potency. Increasing lipophilic bulk at this position gave increasing potency within an ether series (
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One possible explanation for differences
2019-07-05
One possible explanation for differences in the binding ability of monomeric versus dimeric forms of DDR2 ECD to collagen could be that the monomeric form only binds to the primary GVMGFO site, whereas dimeric (and oligomeric) DDR2 ECD binds to additional sites on the collagen triple-helical molecul
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DAPK is involved in the p dependent apoptotic pathway and
2019-07-05
DAPK-1 is involved in the p53 dependent apoptotic pathway and it is a mediator of γ-interferon induced apoptosis. DAPK-1 is also involved in other death signaling pathways (tumor necrosis factor-α, CD95 and transforming growth factor-β) and it blocks tumor metastasis in vivo. The loss of DAPK mRNA R
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br Limitations of the study br Possible conflicts of interes
2019-07-05
Limitations of the study Possible conflicts of interest Dr. Fayemiwo or SAF has received full financial support from Europe Gilead Sciences Ltd. for his M.Sc. degree programme in Medical Mycology and has been paid for talks on behalf of AstraZeneca and GSK. Caroline Moore or CBM has received
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br Multi hierarchical structure of collagen Protein structur
2019-07-05
Multi-hierarchical structure of collagen Protein structure is the foundation of protein functions and properties. It is generally accepted that the protein has biological function only when it has tertiary structure or above. Among the identified 28 types of collagen, most is known about type I c
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In addition to PDCA we also tested other
2019-07-05
In addition to 2,4-PDCA, we also tested other broad-spectrum 2OG oxygenase inhibitors as vCPH inhibitors. N-Oxalyl glycine (NOG, IC50 = 21.2 ± 2.1 µM), a close 2OG isostere, and IOX1 (IC50 = 47.2 ± 2.7 µM), which is a relatively broad-spectrum JmjC demethylase inhibitor, were not as potent in inhibi
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Here two labs that helped
2019-07-05
Here, two labs that helped characterize these two pathways have worked together to further test whether these apparently parallel pathways from β-AR to CaMKII-RyR might be related in series. Much of the work leading to the Epac pathway involved measurement of Ca sparks as an index of SR Ca leak, oft
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br Chondroitin sulfate proteoglycans CSPGs are major compone
2019-07-05
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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SPR was used to measure biomolecular kinetic interactions be
2019-07-05
SPR was used to measure biomolecular kinetic interactions between TERRA G-quadruplex and ligand in the present study. SPR is a widely used method, but cannot tell which specific type of interaction happened. Compounds with similar structures probably have similar mechanism of interaction, while comp
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Recent studies have shown that some CLC
2019-07-05
Recent studies have shown that some CLC genes participate in plant salt tolerance and have speculated that they function by mediating Cl− transport across the tonoplast. For instance, AtCLCc, a vacuolar anion transporter, is shown to be involved in the regulation of stomatal movement and to contribu
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Repulsive interactions towards undesirable substrates
2019-07-05
Repulsive interactions towards undesirable substrates are arguably a very efficient means to implement specificity [8]. In particular, it could be assumed that discrimination against a substrate that is larger than the cognate substrate may be achieved easily by restricting the active site and explo
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Our earlier experimental studies showed neutral
2019-07-05
Our earlier experimental studies showed \"neutral\", i.e. non-proliferative, effects of progesterone but a large increase in proliferation using certain progestins; however, this was only in the presence of PGRMC1 [[13], [14], [15], [16], [17], [18], [19]]. The next step was to investigate whether t
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ER redox imbalance leads to the accumulation of misfolded pr
2019-07-05
ER redox imbalance leads to the accumulation of misfolded proteins, which might trigger the unfolded protein response (UPR) [17]. In the initiation of UPR, GRP78 preferentially binds to unfolded proteins, shifting the binding equilibrium away from IRE-1, PERK, and ATF-6, the initiators of UPR [18].
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In general cellular senescence is considered
2019-07-05
In general, cellular senescence is considered a programmed response to stress that can be activated by oxidative stress, irradiation or action of substances or drugs. These stressors cause DNA damage and, through the action of specific proteins (p53 and p21), lead to cell senescence (di Fagagna, 200
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Fatty acid oxidation plays a crucial role in maintaining bod
2019-07-04
Fatty Ponceau S Staining Solution β-oxidation plays a crucial role in maintaining body energy homoeostasis mainly during catabolic states. It mainly occurs in mitochondria and involves a cyclical series of reactions that result in the shortening of fatty acids. Fatty acids comprise an efficient sou
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