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Tacrine an aminoacridine derivative Fig
2024-06-26
Tacrine, an aminoacridine derivative (Fig. 1, A), was the first AChE inhibitor approved for treatment of AD [12], [13]. This compound was withdrawn from the market due to its hepatotoxicity [14]. In spite of tacrine's side effects, it is still an attractive lead compound for medicinal chemists due t
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This study was funded and supported by
2024-06-26
This study was funded and supported by Tehran University of Medical Sciences and Health Services; and Iran National Science Foundation. Introduction The enzyme acetylcholinesterase (AChE) plays a central role in the signal transduction in the nervous system, hydrolyzing the neurotransmitter acet
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GSK 2830371 The difficulty of characterizing nAChRs in
2024-06-26
The difficulty of characterizing nAChRs in the central nervous system is also exemplified by early observations that nicotine caused no detectable effect when applied on a brain slice and it is only with the focal and high time resolution of more recent experiments that the effects of nicotinic neur
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However although in vitro studies
2024-06-26
However, although in vitro studies in heterologous systems have provided very important indications of potential novel pharmacology, the studies with endogenous receptors in native tissues are essential to provide evidence for GPCR heteromerization in vivo and to confirm its physiological relevance.
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The most potent compounds within the current series of
2024-06-26
The most potent compounds within the current series of compounds were therefore , , , , and , with ace inhibitors possessing the best selectivity towards the lyase reaction in comparison to the hydroxylase reaction, indeed, this compound was found to possess an IC value of 1210nM against the 17α-
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br The cytochrome P enzyme hydroxylase lyase
2024-06-26
The cytochrome P450 enzyme 17α-hydroxylase/17,20-lyase (P450) is involved in the production of the C containing androgen precursors from the C containing steroids such as the pregnanes and progestins (). Steroids such as androstenedione (AD) and dehydroepiandrosterone (DHEA) are therefore synthesi
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br Cytochrome b br Cytochrome P hydroxylase lyase P A
2024-06-26
Cytochrome b5 Cytochrome P450 17α-hydroxylase/17,20-lyase (P450 17A1) A number of P450s involved in steroid biosynthesis are multifunctional as they carry out two or more sequential hydroxylation reactions on the same substrate(s). P450 17A1 is a dual function endoplasmic reticulum enzyme enco
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Among the AXL positive tumors that we screened the
2024-06-26
Among the AXL-positive tumors that we screened, the TNBC cell line MDA-MB-231 showed the highest AXL expression level. Additionally, AXL protein levels were higher in TNBC patient samples than in other breast cancers. Considering the difficulty of, and the urgent need for, effective treatments of TN
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In our previous report we synthesized derivatives
2024-06-26
In our previous report, we synthesized derivatives with some straight chain residues on the 2-position of the 3-cyanopyridine ring of compound 1. In this time we tried to introduce aromatic ring on the chain of the 2-position. Namely, we replaced the hydroxyl-alkylamino group in the position 2 of t
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orexin sale There are increasing repeated reports of amphote
2024-06-26
There are increasing repeated reports of amphotericin B-resistance in pathogenic fungi including Candida spp. [35], [36]. Nolte et al. characterized some fluconazole and amphotericin B-resistant Candida albicans isolates from leukemia patients [37]. Fan-Havard et al. (1991) have shown multi-antifung
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Plerixafor Mass spectrometry MS analysis and
2024-06-25
Mass spectrometry (MS) analysis and selective enrichment methods of phosphorylated proteins are powerful tools that can help address these challenges. Recent advances in MS have made it possible to analyze signaling pathways by facilitating high-throughput identification of phosphorylation sites wit
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The direction of research then turned to investigating
2024-06-25
The direction of research then turned to investigating the long-term effects of adiponectin on insulin resistance. Adiponectin transgenic mice showed a reduction in insulin resistance and diabetes [5,6], while adiponectin-deficient mice showed mild insulin resistance with glucose intolerance, as wel
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selective serotonin reuptake inhibitor In conclusion the res
2024-06-25
In conclusion, the results of this investigation suggest that the involvement of PGE2 in the pathogenesis of pulpal inflammation and repair may be related to its induction of cAMP production. PGE2-induced cAMP production in dental pulp cells is mediated by binding to the EP2 receptor, activation of
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br Materials and methods br Results and discussion
2024-06-25
Materials and methods Results and discussion Conclusion Amino-functionalized mesoporous TiO2-NH2 microparticles were used to immobilize ADA, followed by GLU cross-linking. The mesopores provided a natural microenvironment with sufficient room for the enzyme to efficiently perform its cataly
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In the present study the alternative splicing of several nAC
2024-06-25
In the present study, the alternative splicing of several nAChR subunits was identified in the oriental migratory locust (Locusta migratoria manilensis Meyen), a serious worldwide pest to agricultural production and also a model insect species [5]. Several α subunits were tried to co-express with ra
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