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br Drug design Over the past decades the development of
2021-11-20
Drug design Over the past decades, the development of synthetic, direct fXa inhibitors has undergone four phase. Although these fXa inhibitors possess various scaffolds, most of them bind to the active site in a characteristic l-shaped conformation. In other word, they have a three-component syst
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The IN gene of the HIV
2021-11-20
The IN gene of the HIV isolate from Papua (CRF01_AE isolate) contains genetic polymorphisms (Fig. 1A) that encode for variant amino acids in the IN protein, based on the Stanford HIVdb mutation interpretation database (Fig. 1B). These variations slightly changed the three-dimensional structure of IN
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While histone modifications can alter inter
2021-11-20
While histone modifications can alter inter-nucleosomal interactions that govern the compaction state of a chromatin fiber (Francis et al., 2004, Kalashnikova et al., 2013, Lu et al., 2008), the potential impact of histone modifications on higher-order chromosome organization beyond chromatin-fiber
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br Methods br Transfollicular penetration of herbs and their
2021-11-20
Methods Transfollicular penetration of herbs and their active constituents used for hair loss treatment The transfollicular administration of pharmacologically active molecules is recognised as a significant element for therapeutic interest, mainly with regard to delivery to specific sites of
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More recently several groups have
2021-11-20
More recently, several groups have characterized a role for GPR120 signaling via omega-3 fatty acids in amelioration of alcoholic hepatic injury and non-alcoholic fatty liver disease (NAFLD) [18], [19]. Nakamoto et al. demonstrated protective effects of the omega-3 fatty DAPI hydrochloride mg docosa
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In the present study both experimental and theoretical studi
2021-11-20
In the present study, both experimental and theoretical studies were performed to explore the inhibitory mechanisms of indomethacin and its analogues towards GLOI. A remarkable correlation (=0.974) was derived for the four structurally similar NSAIDs and two curcumins between the experimental bindin
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br Introduction Herpes viruses are members
2021-11-20
Introduction Herpes viruses are members of Herpesviridae family. This family consists of DNA viruses and it is a very large family. The viruses related to this family cause many diseases in animals and humans [1]. Herpes simplex viruses cause mucocutaneous lesions in the affected humans. These le
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TXA has been shown to
2021-11-20
TXA has been shown to be a competitive antagonist on the GABAA receptor and potentially also the glycine [7], [12], [15] receptor. Furtmuller et al. showed that TXA right-shifted the GABA CRC by one order of magnitude [7], while in our study TXA similarly right-shifted the GABA EC50 value from 0.33
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Because of the relationship between carbohydrate consumption
2021-11-20
Because of the relationship between carbohydrate consumption and chronic diseases such as obesity and type II diabetes (Hu, van Dam, & Liu, 2001), there is mounting interest to evaluate the quality of Hordenine receptor through analysis by glycemic index (GI) and Englyst assay, for example (Englyst
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Given the proposed importance of
2021-11-19
Given the proposed importance of conformational dynamics to GCK's allosteric regulation, a number of biophysical methods have been utilized to probe the enzyme's dynamic structural landscape. Investigations into the mechanism of ulixertinib binding, using changes in the enzyme's intrinsic fluoresce
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br Ferroptosis modulators With the
2021-11-19
Ferroptosis modulators With the recognition that the small molecule erastin targets system xc- and thereby specifically triggers this form of death and that ferrostatin-1 prevents erastin-induced ferroptosis [2], it has become evident that ferroptosis is a druggable pathway with a number of trac
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In cardiomyocytes mechanical stress builds up via FAs
2021-11-19
In cardiomyocytes mechanical stress builds up via FAs and the related costamere structures, and excessive stress can cause cardiac hypertrophy. Cardoso et al. (2016) report a comprehensive study that demonstrates the link between stress-induced FAK activation and a FAK-mediated initiation of a trans
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Literature review suggests a strong presence of central hist
2021-11-19
Literature review suggests a strong presence of central histaminergic transmission in the SCF, murine recombinant protein areas targeted by caffeine to induce its behavioral actions. Interestingly, it is reported that caffeine administration increases the histamine neuronal activation and release o
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br Introduction The role of histamine in allergic responses
2021-11-19
Introduction The role of histamine in allergic responses, anaphylaxis, and gastric oicr mg secretion has been well described in both human and veterinary medicine. New roles for histamine and its receptors, however, have been elucidated over the last two decades (Smuda and Bryce, 2011), and nove
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The H autoreceptors distributed mainly in the
2021-11-19
The H3 autoreceptors distributed mainly in the CNS act as a negative feedback on histamine synthesis and release from histaminergic neurons. Histamine is involved in many physiological functions such as sleep-wake regulation, circadian and feeding rhythm, thermal regulation, locomotion, learning, co
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