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There has been growing interest over computational methods t
2023-07-31
There has been growing interest over computational methods to predict the biological activity by chemical structure, so as to decide whether it Senegenin has objective qualities or not. In this contribution, the well-known method, which is called quantitative structure–activity relationship (QSAR)
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br Results br Discussion Dopamine regulates behavioral respo
2023-07-31
Results Discussion Dopamine regulates behavioral responses to nicotine in Drosophila (Bainton et al., 2000), but neurochemical measurements of dopamine after nicotine stimulation had not been made. Here, we demonstrate for the first time that the stimulation of nAChRs causes dopamine release i
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The relatively high concentration of HT
2023-07-31
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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opioid receptor br Experimental procedure br Funding
2023-07-31
Experimental procedure Funding The present study was supported by the Grant Russian Foundation for basic research (project no. 16-04-01517). Introduction 5-HT, a monoaminergic neurotransmitter, is synthesised from l-tryptophan catalysed by the enzymes tryptophan hydroxylase (Tph) and aroma
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Autophagy is a highly conservative intracellular
2023-07-31
Autophagy is a highly conservative intracellular bulk degradation process including three major forms namely microautophagy, chaperone-mediated autophagy and macroautophagy. A large number of evidence has depicted a pivotal role for autophagy in the maintenance of cardiac geometry and contractile fu
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Song et al reported series of triazolylsalicylamide derivati
2023-07-31
Song et al. reported series of 1,2,3-triazolylsalicylamide derivatives and screened over kinase panel and found compound 31 as most potent which inhibited Aurora-A, specifically with IC50 of 0.37 μM. Compound 31 was about 10-fold more active for Aurora-A than for Aurora-B (IC50 = 3.58 μM reported s
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While it is known that circulating
2023-07-31
While it is known that circulating LDL-C levels are largely regulated by either controlling the rate of hepatic production of its triglyceride-rich precursor VLDL particle or the rate of LDLR-mediated LDL particle clearance [58], it should be noted that important differences exist between rodents an
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Many ruthenium complexes were tested as potential anticancer
2023-07-31
Many ruthenium complexes were tested as potential anticancer agents and two complexes, namely NAMI-A (trans-[imH] [RuCl4(dmso-S)(im)]; im, imidazole) and KP1019 (trans-[indH][RuCl4(ind)2]; ind, indazole) have successfully entered clinical trials [27], [28]. NAMI-A is selectively active against metas
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Recruitment of the Rad BP mediator to chromatin
2023-07-31
Recruitment of the Rad9/53BP1 mediator to egfr inhibitor involves multiple pathways (Fig. 2). In unperturbed conditions, Rad9 is already bound to chromatin via interaction between its Tudor domain and methylated histone H3 at lysine 79 [82], [83], [84], [85]. This constitutive Rad9 recruitment to c
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br Antifungal resistance what is in a
2023-07-31
Antifungal resistance, what is in a name? Antifungal resistance is an emerging and hot topic in the field of medical mycology. Microbiological resistance is identified by determining minimal inhibitory concentrations (MICs) in vitro for a given antifungal and interpreting this value according to
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In this study we have
2023-07-31
In this study, we have generated new FRET reporters to screen all submembrane domains of AT1R for interactions with CaM. We identified a new CaM-binding domain on the receptor’s SMD2 (a.a. 125 – 141), confirmed interactions at SMD4JM (a.a. 309 – 327) and characterized the full interacting domain in
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NS3694 Earlier studies with SERMs identified that distinct
2023-07-31
Earlier studies with SERMs identified that distinct chemical scaffolds have the ability to induce unique conformational changes in the ER, resulting in interaction with different cofactor subsets. The same has been demonstrated with SARMs, which induce distinct conformational changes compared to tes
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Introduction The burden of cardiovascular
2023-07-31
Introduction The burden of cardiovascular disease (CVD) is undisputed, accounting for approximately a third of global deaths (17.5 million people in 2012) (WHO, 2012). Atherosclerosis leads to the development of coronary heart disease (CHD) which accounts for more than 40% of these deaths (WHO, 201
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There are several reports providing evidences that
2023-07-31
There are several reports providing evidences that functional and mechanistic connection between Sirt1 and LKB1/AMPK in metabolic regulation [26], [32], [33]. It has been reported that the deacetylation of LKB1 by Sirt1 is one of the determining factors of the subcellular localization of LKB1. In ag
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br Materials and methods br Results br Discussion
2023-07-31
Materials and methods Results Discussion The transcriptional activity of PGC-1α is regulated by a number of stimuli, exemplifying the range of settings in which mitochondrial biogenesis is induced. The mechanisms governing this regulation have been extensively studied and have been determin
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