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Analysis of Table shows that compound b in which the
2021-06-17
Analysis of Table 1 shows that compound 7b, in which the biphenyl scaffold does not bear any substituent, displays its inhibitory potency in the micromolar range (IC50 = 11 μM). If the amide bridge is moved from position 1 to 3 of the biphenyl system, product 7c is yielded, whose potency is about 4
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To be a qualified non specific CYP inhibitor used as
2021-06-17
To be a qualified non-specific CYP inhibitor used as an in vitro or in vivo screening tool to distinguish CYP involvement in the overall metabolism, a complete inhibition of the entire metabolism catalyzed by CYPs in a simple experiment is desired. Based on our results, 100 μM atipamezole can comple
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br Material and methods br Results Diagrammatic representati
2021-06-17
Material and methods Results Diagrammatic representations showing the bilateral injection sites in the BNST of all animals used in the present study are presented in Fig. 1. Discussion The present results provide the first evidence that both CRF1 and CRF2 receptors in the BSNT are involved
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Completion of h of education was significant in virtually
2021-06-17
Completion of 150 h of education was significant in virtually all prior studies of the 150-h requirement (Allen and Woodland, 2006, Boone et al., 2006 and others). While the 150-h requirement applies to licensure, students are often permitted (as in California) to sit for the CPA exam with fewer tot
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The absence of an observable time dependence of kobs on
2021-06-17
The absence of an observable time dependence of kobs on inhibitor concentration for TC-H 106 receptor 3 with AChE and compounds 1, 3 and 4 with BuChE parallels a similar absence of time dependence for some related fluoro ketones with AChE. Nair et al. found that trifluoromethyl acetophenones with sm
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Thus the understanding of the various
2021-06-17
Thus, the understanding of the various mechanisms of action of estrogen and SERMs is an important medical challenge and could help to develop an “ideal” SERM, preserving the beneficial effects of estrogen in the bone and urogenital system, and reducing the unwanted side effects, mainly increased ris
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Other studies have investigated the role of HDAC inhibitors
2021-06-17
Other studies have investigated the role of HDAC inhibitors in particular signaling pathways mediated by EWS–FLI1 (Matsumoto et al., 2001). A recent investigation, showed a physical association of EWS–FLI1 and HDAC1 that helps mediate a disruption in the p53 activation of downstream targets (Li et a
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EphB appears to be a low affinity
2021-06-17
EphB4 appears to be a low-affinity receptor for rhEpo based on the biochemical data. The concentration of rhEpo used for the biological experiments (50 IU/ml) corresponds to 10–15 nM, which is 1% to 2% of the KD value (KD = 881 nM) for the binding of rhEpo to EphB4, as measured in the MST assay. The
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br Introduction Cerebral stroke causes an efflux
2021-06-17
Introduction Cerebral stroke causes an efflux of various groups of progenitor and stem cells from bone marrow to bloodstream and the levels of these cells correlate with neurological status of stroke patients (Gójska-Grymajło et al., 2012, 2018). It is thought that paracrine factors produced by t
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Although enantioselective accumulation of metalaxyl in
2021-06-17
Although enantioselective accumulation of metalaxyl in organisms is an integrated outcome of bio-process including absorption, transportation, and transformation, it is observed in our study that catalysis of CYP450 may lead to the enantioselective accumulation of metalaxyl. However, the mechanisms
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br Conclusions Mulan is a mitochondrial E
2021-06-16
Conclusions Mulan is a mitochondrial E3 ubiquitin ligase with diverse roles in cell growth, cell death, and mitophagy. To better understand the mechanism of Mulan's function we used a modified yeast two-hybrid system to isolate proteins that interact with its cytoplasmic RING domain (amino acids
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br Experimental section br Author contributions br Acknowled
2021-06-16
Experimental section Author contributions Acknowledgements Introduction Many tnf alpha inhibitors in cells are sequential enzymatic reactions where the product of one enzyme serves as the substrate of a second enzyme (1, 2). Experimental evidence suggests that some of these consecutive
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br Results br Discussion The most relevant overall finding
2021-06-16
Results Discussion The most relevant overall finding was that DDR1 is present in myelin and is probably synthesized by oligodendrocytes. This result was supported by three different approaches. First, we detected presence of DDR1 mRNA in myelin by ISH. Second, the pattern of DDR1 immunostainin
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br DDR role in kidney Thirty
2021-06-16
DDR1 role in kidney Thirty-eight papers are reported in PubMed upon the keyword search “DDR1 AND kidney”. Careful examination of those papers shows that only 31 are related to DDR1's role in glomerulosclerosis and renal fibrosis, 24 of those being research and the rest review articles. Since the
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Calcium dependence of CaM target interaction was analyzed us
2021-06-16
Calcium dependence of CaM/target interaction was analyzed using a titration matrix in which both Ca2+ and CaM concentrations were changed. This gave us access to different parameters characterizing the interaction and namely to the number of bound Ca2+ required for the interaction to occur. Our app
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