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Among the various delivery strategies in the
2021-12-29
Among the various delivery strategies in the field of nano-DDS, developing smart targeted nanocarriers has long been a research focus for pharmaceutical scientists11., 12.. The ideal drug delivery outcome must be precisely delivering the therapeutic agents to their sites of action, especially for an
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To further investigate if GPR was
2021-12-29
To further investigate if GPR40 was the functional target of these phenylpropiolic Free Fatty Acid Quantification Colorimetric/Fluorometric Kit receptor analogs, GW-1100, a selective antagonist of GPR40-mediated Ca2+ elevations in HEK293 cells with an IC50 value equal to 1 μM, was used to inhibit ag
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Oleandrin Sexual size dimorphism has been
2021-12-28
Sexual size dimorphism has been observed in European eel and half-smooth tongue sole (Cynoglossus semilaevis), as females have a faster growth rate than males, (Degani, G., et al., 2003, Ma, Q., et al., 2012). Ma et al. 2011 reported that the mRNA level of GH was higher in the pituitary gland of bot
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In a series of experiments the clotrimazole
2021-12-28
In a series of experiments, the clotrimazole concentration was varied and the NSVDC channel conductances were calculated from Eq. (1) to obtain the dose-response relation (Fig. 3). The data were fitted to the Michaelis–Menten-type activation curve (Eq. (3)) and gave an EC50 value of 14 μM and a dose
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Although exhibited high inhibitory activity was found
2021-12-28
Although exhibited high inhibitory activity, was found to be metabolically unstable due to the hydrolysis of the phosphate group (data not shown), which prompted us to modify the phosphate moiety of . Comparison of the activities between three compounds bearing no or different spacer groups (, , a
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br Conclusion Discovery of an ideal
2021-12-28
Conclusion Discovery of an ideal orally active antithrombotic drug has remained elusive till date. Research efforts in this direction led to the discovery of numerous coagulation enzyme inhibitors including various thrombin and FXa inhibitors. Several preclinical studies have highlighted the impo
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br Materials and methods br Results br Discussion Several
2021-12-28
Materials and methods Results Discussion Several histamine H3 receptor antagonists have progressed into clinical development for indications including Alzheimer's disease, schizophrenia, pain and narcolepsy. Each of the compounds studied herein has been extensively characterized in its own
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br Introduction Chronic hepatitis C CHC caused by hepatitis
2021-12-28
Introduction Chronic hepatitis C (CHC) caused by hepatitis C virus (HCV) infection affects approximately 170 million individuals worldwide [1]. HCV and human immunodeficiency virus (HIV) have similar routes of transmission, including blood-to-blood contact, sharing of injection equipment, and sex
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Substrate affinity and specificity can be enhanced by dockin
2021-12-28
Substrate affinity and specificity can be enhanced by docking interactions, in which regions distal to the site of SR1078 bind to grooves, pockets, or surfaces outside of the kinase catalytic cleft 1, 2, 5, 6. Like catalytic site interactions, docking interactions can involve recognition of short li
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Recently several groups reported that four orphan receptors
2021-12-28
Recently, several groups reported that four orphan receptors, GPR40, GPR41, GPR43, and GPR120, can be activated by free fatty acids. Short-chain fatty acids are specific agonists for GPR41 and GPR43 . Medium and long-chain fatty acids can activate GPR40 and GPR120 . Our previous report showed that
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Nimodipine The HRTOF MS of showed a quasi molecular ion
2021-12-28
The HRTOF-MS of showed a quasi-molecular ion peak at / 525.3044 [M+Na], corresponding to a quasi-molecular formula of CHNONa (Calcd for CHNONa: 525.3053). IR absorptions at 1680 and 1522cm suggested the presence of amide functions. Based on an analysis of 1D and 2D NMR spectra, the presence of one
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Introduction l Glutamate is a major excitatory neurotransmit
2021-12-28
Introduction l-Glutamate is a major excitatory neurotransmitter in the mammalian central nervous system (CNS) that contributes not only to fast synaptic neurotransmission, but also to complex physiological processes like memory, learning, plasticity, and neuronal cell death [30], [81]. Glutamate is
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br Introduction Alzheimer s disease AD
2021-12-27
Introduction Alzheimer's disease (AD) affects ca. 46 million people worldwide [1] and it is expected that the number will double or triple by 2030 or 2050, respectively, while no significant progress has been made in research for early diagnosis and new efficient therapies. Currently available me
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Classical drugs target the viral enzymes reverse transcripta
2021-12-27
Classical drugs target the viral Griseofulvin reverse transcriptase (RT), protease and integrase (IN) [[4], [5], [6]]. Raltegravir (ISENTRESS/MK-0518) is the prototypical integrase strand transfer inhibitor (INSTI) leading to an extremely strong reduction in viral load [7] and it has been approved f
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Several studies have reported that the genotype
2021-12-27
Several studies have reported that the genotype and allele frequencies of S267F vary considerably between different study groups and geographical regions (Ezzikouri et al., 2017, Hu et al., 2016, Lee et al., 2017, Li et al., 2014, Pan et al., 2011, Peng et al., 2015, Yang et al., 2016, Zhang et al.,
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