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The ADME profile of AAT was
2021-03-15
The ADME profile of AAT-008 () was very promising, with high stability in HLM. The pre-clinical pharmacokinetic properties of AAT-008 were also assessed in rats (Sprague-Dawley, male), dogs (beagle, male), and monkeys (cynomolgus, male). The experimentally determined parameters are summarized in .
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br Introduction The development of
2021-03-15
Introduction The development of non-melanoma skin cancer (NMSC) is a complex process characterized by the acquisition of altered proliferation and invasiveness. These changes are classically defined as occurring in stages, i.e., initiation, promotion, and progression. In the two-stage model of in
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Another important new result that has expanded
2021-03-15
Another important new result that has expanded the range of functions of iPLA2-VIA in physiology and pathophysiology is its implication in macrophage polarization under stimulation conditions. Ashley et al. [129] described in peritoneal macrophages from Pla2g6−/− mice that the absence of iPLA2-VIA f
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Another enzyme class that has emerged as a
2021-03-15
Another enzyme class that has emerged as a potential alternative to P450s are the so-called ‘unspecific peroxygenases’ (UPOs). They also contain a heme but are extracellularly expressed fungal enzymes that are often more stable than P450 monooxygenases. Importantly, UPOs use H2O2 instead of O2 as th
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In vasculature NADPH oxidases NOXs are the
2021-03-15
In vasculature, NADPH oxidases (NOXs) are the main sources of O2− generation that involve in the transfer of electrons to molecular oxygen. Endothelin-1 [25] and thromboxane A2 [26] were reported to induce eNOS uncoupling via upregulation of NOXs. Additionally, inhibition of p47 phox, a subunit of N
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We propose that unlike other autophagy genes the
2021-03-15
We propose that, unlike other autophagy genes, the specific increase in the expression of IRGM by pEIF2A plays a major role as a checkpoint allowing host cell survival by autophagy or host cell elimination by necroptosis. The localization of IRGM to the mitochondrial inner membrane, its ability to i
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br STAR Methods br Microenvironmental niches for
2021-03-15
STAR★Methods Microenvironmental niches for naïve and activated B cells Secondary lymphoid organs, such as the spleen and lymph nodes, are structurally and functionally compartmentalized to provide a set of microenvironmental niches that support the survival of resting B cells, as well as the a
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Likewise the conserved cysteine in the E protein is
2021-03-15
Likewise, the conserved cysteine in the E2 protein is the only residue shown to be essential for the transfer of Ub/Ubl from E2 to the HECT ligases (Dye and Schulman, 2007, Wu et al., 2003). However, all other terminal Ub/Ubl transfer reactions involving E2 enzymes suggest a critical role for the ta
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These studies established IAP proteins as dimeric RING E
2021-03-15
These studies established IAP proteins as dimeric RING E3 ligases, but did not account for the essential role of dimerization. In IAPs and related E3s, such as RNF4 and MDM2, dimerization not only depends on contacts from the core RING domain but also residues N- and C-terminal to the RING domain (B
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br Results and Discussion br Conclusions Understanding the c
2021-03-15
Results and Discussion Conclusions Understanding the connections between function and fitness is a primary goal of many biological disciplines including systems biology and molecular evolution. While sound approaches have been developed to understand the connections between function and fitnes
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DPP is show two relevant benefits in the clinical management
2021-03-15
DPP-4is show two relevant benefits in the clinical management of type 2 diabetic patients: negligible risk of severe hypoglycemia, particularly when compared with sulphonylureas [[33], [34]], and weight neutrality, in contrast with the weight gain generally observed with insulin therapy, sulfonylure
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Ro 5-3335 br General mechanism of NHEJ NHEJ is an amazingly
2021-03-15
General mechanism of NHEJ NHEJ is an amazingly versatile pathway that can select specific enzymes which bind to, process, and finally mediate the direct re-ligation of a wide range of DSBs including those that are complex, have incompatible ends, and contain Ro 5-3335 damages [7], [8], [9], [10]
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br Discussion The differences in the kinetic properties of L
2021-03-15
Discussion The differences in the kinetic properties of L-AmDH and LeuDH presented herein reflect a different kinetic mechanism. When compared to its parent enzyme, L-AmDH displayed a different substrate binding order, lower affinity for the keto substrate, and stronger product inhibition. The tw
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Similarly LTD concentration dependently enhanced AQP express
2021-03-15
Similarly, LTD4 concentration-dependently enhanced AQP4 expression in astrocytes (Fig. 3). The LTD4-enhanced AQP4 expression was not affected by pranlukast but inhibited by Bay u9773, a non-selective CysLT1/CysLT2 receptor antagonist [33]. Because no selective CysLT2 receptor antagonists are current
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Acknowledgments br Introduction Various researches have
2021-03-15
Acknowledgments Introduction Various researches have been made in the field of the treatment of cancer and inflammatory diseases. Different mechanisms are involved in the progression of cellular damage that gives an idea about new drug targets. There are always some efforts to improve efficacy,
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