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The first rationally designed dual mPGES LO inhibitor
2023-01-31
The first rationally designed dual mPGES-1/5-LO inhibitor was reported in 2008 and represents a structural derivative of pirinixic 77 9 - a synthetic agonist of PPARα with lipid-lowering properties (Koeberle et al., 2008b). Further α-alkyl- and α-aryl-substituted derivatives have been synthesized a
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Matrix metalloprotease inhibitors are increasingly available
2023-01-31
Matrix metalloprotease inhibitors are increasingly available and tested for other indications in clinical trials. The present study suggests that either ADAM10 or TACE inhibition alone will not maximally restore leukocyte Axl function. We found that lower doses of ADAM10/TACE inhibitors exhibit simi
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Docking studies were performed on the selected compounds to
2023-01-31
Docking studies were performed on the selected compounds to explore their binding patterns and to examine SAR in more detail. The co-crystal structure of ATX in complex with PF-8380 (PDB code: ) was selected for the docking studies due to structural similarity of the most potent compound with PF-83
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Introduction The first use of
2023-01-31
Introduction The first use of the term “autophagy” by a French physiologist, M. Anselmier, in a short article describing the effects of fasting in mice published in 1859, took place almost a century before Christian De Duve described it from a mechanistic point of view in a symposium on lysosomes i
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Introduction The MMR system keeps the fidelity of replicatio
2023-01-31
Introduction The MMR system keeps the fidelity of replication by repairing replication errors such as base-base mispairs and insertions/deletions. It plays a substantial role in restoring the fidelity of DNA and contributing to genome integrity [1]. The components of MMR are conserved in a broad ra
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MRS1523 That increased longevity was not
2023-01-30
That increased longevity was not the exclusive result of blood pressure reduction. This was demonstrated by analysis of life-long, whole body deletion of AT1A receptors in normotensive mice. These animals exhibited a very significant increase in lifespan when compared to wild- type mice [159], [160]
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br Introduction The development and plasticity of synapses
2023-01-30
Introduction The development and plasticity of synapses involve the timely recruitment of a plethora of proteins on both pre- and postsynaptic sides through ill-defined mechanisms. At excitatory synapses, two of the major proteins that are dynamically recruited postsynaptically are the Ca2+/calmo
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gap26 A central question that arises in this
2023-01-30
A central question that arises in this discussion is whether enhanced neurobehavioral responses to food cues emerge as a consequence of weight gain, or whether there are intrinsic differences in the motivational responses to food cues that precede weight gain. In support of pre-existing differences,
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A disfun o cognitiva p s
2023-01-30
A disfunção cognitiva pós‐operatória é uma síndrome perioperatória bem reconhecida, consequência da anestesia e cirurgia cuja causa exata permanece por esclarecer. De que forma RHC 80267 disfunção cognitiva pós‐operatória e a doença de Alzheimer podem estar ligadas permanece uma questão em estudo.
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HsALDH enzyme has been purified for the first time
2023-01-30
HsALDH enzyme has been purified for the first time in our laboratory from human saliva and has been kinetically characterized using different aromatic substrates [35]. Also, the effect of some common substances frequently encountered by the enzyme in the oral cavity (such as ethanol, hydrogen peroxi
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It has been largely demonstrated that several clinico
2023-01-30
It has been largely demonstrated that several clinico-pathological factors influence ovarian cancer patients' prognosis, including residual tumor at primary cytoreductive surgery, FIGO stage, tumor grading, cancer histology and performance status [3,4]. Nevertheless, the recent awareness achieved in
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According to their structures and substrate specificity MMPs
2023-01-30
According to their structures and substrate specificity, MMPs are divided into five major groups: collagenases (e.g., MMP1), gelatinases (e.g., MMP2, MMP9), stromelysins (e.g., MMP3, MMP10), matrilysins (e.g., MMP7), and membrane-type MMPs [7]. Among them, MMP1 is a major collagenase that degrades t
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To confirm a role of OCT in corticosterone induced potentiat
2023-01-30
To confirm a role of OCT3 in corticosterone-induced potentiation of cocaine-primed reinstatement, we examined the interaction of corticosterone and cocaine in the reinstatement of cocaine conditioned place preference (CPP) in wild type mice, and transgenic OCT3-deficient mice. These mice express a t
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br Methods br Results br Discussion Chronic stress renders i
2023-01-30
Methods Results Discussion Chronic stress renders individuals vulnerable to diseases, and this effect might be, at least partially, mediated by stress hormone-induced immunosuppression. Therefore, investigating the effects of catecholamines on immune Cytochalasin J synthesis is of high rel
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As we previously observed in
2023-01-30
As we previously observed in the NSFT (Fukumoto et al., 2014), the effect of LY341495 in the FST was also inhibited by a 5-HT1A receptor antagonist, indicating the role of the 5-HT1A receptor in the actions of LY341495. Among the 5-HT1A receptors, which exist both presynaptically and postsynapticall
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