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The general synthetic routes leading to aspartate and diamin
2022-06-08
The general synthetic routes, leading to aspartate and 2,3-diaminopropionate analogs, are shown in . As outlined in , aspartic rucaparib mg analogs – were synthesized through standard carbodiimide-mediated coupling between an amine and an appropriately protected aspartic acid. It is worth mentionin
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br Conflict of interest br Acknowledgements br Introduction
2022-06-08
Conflict of interest Acknowledgements Introduction Second generation antipsychotic drugs (SGAs) such as olanzapine are widely used in treating individuals with schizophrenia and bi-polar disorder and are increasingly prescribed for other conditions such as anxiety (Pringsheim and Gardner, 2
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It is noted that knee swelling was milder and
2022-06-07
It is noted that knee swelling was milder and the intensity of IL-4 staining (MFI) in the vehicle-treated group was lower in the second (Fig. 7a and d) than the first (Figs. 1a and 3f) AIA experiment. The variation in joint swelling between the two studies is most likely due to the models being perf
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Further our data demonstrate a role for mitochondrial AIF
2022-06-07
Further, our data demonstrate a role for mitochondrial AIF in oxidative cell death induced by RSL3. We found that AIF knockdown using siRNA completely protected the National Survey against RSL3 induced oxidative stress. Similar to other pathways of caspase-independent programmed cell death, mitoch
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Receptor activator of NF B ligand RANKL and macrophage
2022-06-07
Receptor activator of NF-κB ligand (RANKL) and macrophage colony-stimulating factor (M-CSF) stimulate the generation of osteoclast Gemfibrozil [10], [11], [12], [13]. In response to sphingosine 1-phosphate (S1P) signaling, osteoclasts then attach to regions of bone undergoing resorption [14]. In RA
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Accordingly and in animal models a high fat diet
2022-06-07
Accordingly and in animal models, a high-fat diet rich in CO (CO-HFD) impeded ventricular function and induced cardiac cell death and remodeling, at least, by down-regulating cell antioxidant defense systems and induction of oxidative stress [28], [29], [30], [31]. Interestingly, long chain fatty ac
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Next we were interested in replacing the ketobenzimidazole f
2022-06-07
Next, we were interested in replacing the ketobenzimidazole fragment of our inhibitors with a noncarbonyl bearing heterocycle. We reasoned that if we could replace the carbonyl while maintaining comparable FAAH inhibition, it would provide evidence for a noncovalent mechanism of action. Thus, we eva
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NCT-503 Although unexpected based on our predictions
2022-06-07
Although unexpected based on our predictions, low baseline and post-stress cortisol being associated with high anxiety has been previously documented in both clinical and healthy populations of humans (Beaton et al., 2006; Jezova et al., 2004; Shirotsuki et al., 2009; Vingerhoets et al., 1996), and
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Loss of EZH function as a consequence of nonsense
2022-06-07
Loss of EZH2 function as a consequence of nonsense or frameshift mutations has also been detected in a cohort study conducted by Jankowska et al. in chronic myelomonocytic leukemia (CMML) patients, as an early event in cancer development [43]. Although, a recent study in Japan described increased le
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In addition to the regulation of
2022-06-07
In addition to the regulation of SV exo- and cholecalciferol vitamin d3 by Ca2+ influx retrieval of SV membranes depends on the exocytic insertion of SV components into the presynaptic membrane: If exocytic SV fusion in neurons is abrogated by genetic inactivation of the core release machinery (e.g.
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Noticeably aminopyrimidine analogs are the most widely
2022-06-07
Noticeably, aminopyrimidine analogs are the most widely published H4R antagonists and it was Bayer who first disclosed two series of 2-aminopyrimidine compounds possessing significant H4R functional activity. Subsequently, further 2-aminopyrimidine H4R antagonists were published by Pfizer (ZPL-38937
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In conclusion re evaluation of HER status is necessary to
2022-06-07
In conclusion, re-evaluation of HER2 status is necessary to determine the appropriate use of anti-HER2–targeted therapy beyond disease progression. EGFR and c-met amplification, as well as PIK3CA mutation, are rarely associated with acquired resistance. Our results highlight the importance of formal
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Accessibility and physico chemical features of cysteine resi
2022-06-07
Accessibility and physico-chemical features of cysteine residues define their redox-reactivity and the 3-dimensional structure of GSNOR allows to identifying such surface-exposed, redox-sensitive cysteine residues. GSNOR crystal structures are available from human (Protein Data Bank code: 1MP0), tom
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Decreasing GSK activity has therapeutic benefits in animal
2022-06-07
Decreasing GSK-3β activity has therapeutic benefits in animal model of colitis [45] and traumatic URB597 injury [46] and ischemia/reperfusion injury [47,48]. In brain, activation of GSK-3β promotes Aβ toxicity by elevating APP expression and its amyloidogenic cleavage, and by dysregulating Aβ clea
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After the synthesis of methylsulfonyl or tetrazole surrogate
2022-06-07
After the synthesis of methylsulfonyl or tetrazole surrogate derivatives, compounds synthesized by introducing hydrogen, fluoro, and methyl groups into the head group of GPR119 agonists were synthesized. Compounds – were synthesized by reacting hydroxybenzaldehyde with fluorine, hydrogen, or a methy
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