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In vitro studies with soman inhibited
2024-04-28
In vitro studies with soman-inhibited, non-aged AChE revealed a species dependent reactivating potency of HI-6 and MMB-4. With guinea pig AChE second order reactivation rate constants of 0.051 and 0.038mM−1min−1 were determined for HI-6 and MMB-4, respectively (Luo et al., 2007). Corresponding value
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Indanone and its analogues are useful intermediates for
2024-04-28
1-Indanone and its analogues are useful intermediates for the synthesis of compounds some of which have applications as pharmaceuticals, especially as analgesic and antihypertensive as well as tobacco flavoring agents. Indanones are commonly used as starting agent for the synthesis of ninhydrin whic
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The relatively high concentration of HT
2024-04-28
The relatively high concentration of 5-HT used in this study (100 µM) is consistent with the concentrations used in other published ex vivo studies (Ropert and Guy, 1991, Passani et al., 1994, Shen and Andrade, 1998). In our paradigm 5-HT was focally applied at the surface of the slice via a fast pe
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In conclusion we have produced some highly potent
2024-04-28
In conclusion, we have produced some highly potent inhibitors of P450 in comparison to the standard (+)-Aphidicolin KTZ. Also, due to the limited specificity of these compounds against lyase in comparison to the 17α-OHase component, these compounds would be expected to have a major impact on cortic
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In order to improve the methodology
2024-04-28
In order to improve the methodology of the synthesis of steroidal derivatives, our goal was the investigation of aza-Michael addition of different N-nucleophiles to 16-dehydropregnenolone in the presence of [DBU][OAc] as catalyst and reaction medium. Michael addition of electron deficient steroidal
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For the NSCLC patients with EGFR activating mutations EGFR
2024-04-28
For the NSCLC patients with EGFR-activating mutations, EGFR-TKIs (gefitinib and erlotinib) are effective clinical therapies [21], [22]. However, approximately 10% of patients harboring EGFR-sensitizing mutations exhibit intrinsic resistance, and up to 40% do not attain a major response to treatment
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CHK has been reported to be the
2024-04-27
CHK1 has been reported to be the kinase responsible for H3.3S31 phosphorylation in human ALT cancer sodium channel blockers . However, in our study, knockdown of CHK1 in HEK293F (Figs. S1c and S6) or HeLa S3 (data not shown) cells did not result in a significant decrease in H3.3S31ph, which is in a
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Comparison of the GLUT positive plus
2024-04-27
Comparison of the GLUT1-positive plus ACLY negative group with the GLUT1-negative plus ACLY positive group indicated no significant difference with respect to disease-free survival and overall survival. However, some obvious differences in histological types were found in their formation. A previous
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Secondly leptin has been shown to enhance aromatase mRNA
2024-04-27
Secondly, leptin has been shown to enhance aromatase mRNA expression, aromatase content and its enzymatic activity in epithelial breast cancer Beta-Lapachone by inducing promoters II and I.3 via an enhanced binding of transcription activator protein 1 (AP-1) complex to specific DNA sites in the pro
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br Epidemiology br Genetics The dominantly
2024-04-27
Epidemiology Genetics The dominantly inherited PrP cerebral amyloidoses are genetically transmitted with a penetrance of almost 100%. Early linkage analysis studies helped to established the relationship between GSS and mutations in the PRNP gene. PRNP is located on the short arm of chromosome
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br Conclusions br Declarations br Introduction The classical
2024-04-27
Conclusions Declarations Introduction The classical term of endocrine disruption includes any agent that interferes with the action of hormones within the human body; these agents are therefore named endocrine disruptors. Among these agents, that are mainly environmental chemicals (pollutan
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br Concluding Remarks and Future Perspectives Herein
2024-04-27
Concluding Remarks and Future Perspectives Herein, we have highlighted our current understanding of the role of the LKB1-AMPK pathway and its related kinases in β cell biology. β cell-specific genetic models have been particularly useful in delineating precise roles for individual family members
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In this study using pure enzyme preparations
2024-04-27
In this study, using pure enzyme preparations of human placental recombinant AR (hAR) and of AR isolated from bovine lens (bAR), which behave as Michaelis Levodopa with glyceraldehyde as substrate, is shown that an apparent negative cooperativity action for glucose still occurs. We present evidence
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Tenovin-6 mg Among all the compounds the novel L derivative
2024-04-27
Among all the compounds, the novel L-748,337 derivative (23d) showed the potent human β3-AR antagonist activity and high lipolysis inhibitory activity in vitro. The Tenovin-6 mg 23d displayed 23-fold more potent β3-AR antagonist activity (EC50 = 0.5117 nM) than that of L-748,337 (EC50 = 11.91 nM) a
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The synthetic route to M
2024-04-27
The synthetic route to M100907 developed by Rice was utilized, however, the chiral resolution was carried out at an earlier stage to provide the possibility of introducing different substituents onto the piperidinyl group. The conditions for this resolution were different from previously reported.
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