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summarizes FAAH inhibition data for a series of benzofuran y
2022-05-27

summarizes FAAH inhibition data for a series of 4-[2-benzofuran]2-yl-pyrimidines substituted with a pyrrolidine, piperidine or homopiperidine bearing a methyl-ketobenzimidazole unit. As indicated, the 3-(keto-benzimidazole-3-yl)piperidine displayed potent inhibition of hFAAH and moderate inhibitio
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Several studies have also shown that HK
2022-05-27

Several studies have also shown that HK2 may be an important downstream herpes simplex virus 1 of the PI3K/AKT/mTOR signaling pathway and may contribute to the development of cancer [15]. In our previous study, we found AKT2 expression was positively correlated with HK2 expression in primary colon
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br Statistical analysis The mean standard deviation median
2022-05-27

Statistical analysis The mean, standard deviation, median, range, frequency, and percentage were used for data description. The chi-square (x2) test was used for analyses the differences in categorical variables in the 2-way table. Overall survival (OS) was defined as the time interval between t
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The rationale for developing HDACi as anticancer agents was
2022-05-27

The rationale for developing HDACi as anticancer agents was based on their ability to induce the hyperacetylation of histones and nonhistone proteins, resulting in increased differentiation, apoptosis, and Diclofenac mg arrest of cancer cells 1, 2, 3. HDACi have been used in the treatment of hemato
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Among RASs observed in patients from group RAS T S
2022-05-27

Among RASs observed in patients from group 2, RAS T54S was identified in one patient infected with subtype 1b. This mutation had been shown to cause resistance to boceprevir and telaprevir, but not to simeprevir [36]. This was confirmed here since this patient achieved SVR after 12 weeks of treatmen
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The discovery that the physiological functions of
2022-05-27

The discovery that the physiological functions of LPI are associated with the activation of specific GPR55 membrane receptor [4] has launched a new era of research on this lysophospholipid. However, the activation of membrane receptors by lysophospholipids is extremely complex due to the multitude o
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br Clinical development of anti NASH drug therapies The curr
2022-05-26

Clinical development of anti-NASH drug therapies The current understanding of NASH pathogenesis has led to broad efforts to target several features of the disease, alone or in combination, even in the absence of liver-guided therapies. Therefore, drug development in NASH is a rapidly changing fie
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br Acknowledgements This work was supported by Slovak Academ
2022-05-26

Acknowledgements This work was supported by Slovak Academy of Sciences grants VEGA 2/0052/10 and 2/0045/10. Both clinical observations and preclinical studies suggest that hypofunction of -methyl--aspartate (NMDA) receptor is implicated in the pathophysiology of schizophrenia. Thus, therapeuti
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The following are the supplementary data related to this art
2022-05-26

The following are the supplementary data related to this article. Author contribution Conflict of interest Introduction Thrombosis (arterial and venous) is a major cause of vascular obstructive diseases including myocardial infarction, cerebral infarction and pulmonary embolism. Glycoprote
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muscarinic The molecular identity of RA s
2022-05-26

The molecular identity of RA’s target during LTP induction was determined by pharmacological testing. The inhibitory effects of CNQX and niflumic acid on LTP induction remained even in the presence of RA, indicating RA did not affect either the AMPA receptor nor chloride channel (Fig. 2B and D) [26]
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br Acknowledgements This research was funded by Ministry
2022-05-26

Acknowledgements This research was funded by Ministry of Education Malaysia (MOE), and supported by the Department of Nutrition, Exercise & Sports, Department of Drug Design, University of Copenhagen, Denmark and Universiti Malaysia Pahang (UMP), Malaysia. HPLC equipment used for high-resolution
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Caspase-1, human recombinant proteinase australia While CART
2022-05-26

While CART increased circulating levels of GIP and GLP-1 in vivo, we were unable to detect any effect of exogenous CART on GIP and GLP-1 mRNA expression or GLP-1 secretion in vitro. There is no ready explanation for this discrepancy. The CART doses used (both in vivo and in vitro) have been shown to
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Inhibitors of the G rdos effect include
2022-05-26

Inhibitors of the Gárdos effect include the Ca2+-channel blocker nitrendipine with an IC50 of ∼103nM (Ellory et al., 1992, Ellory et al., 1992); its mode of action is likely to be from direct blockage of K+ flux through the Gárdos channel (Ellory et al., 1992, Ellory et al., 1992), and the peptidic
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Ro 32-3555 br FXR FGF in the control of BAs
2022-05-26

FXR–FGF15/19 in the control of BAs synthesis The nuclear receptor FXR is the master regulator of BAs homeostasis, modulating their synthesis, Ro 32-3555 and uptake [15]. FXR decreases BA de novo hepatic biosynthesis by reducing the expression of CYP7A1. At the canalicular membrane, newly-synthes
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However at variance with the well studied R form
2022-05-26

However, at variance with the well-studied R form of FBP1 which is flat, the R state of FBP2 is diametrically different, with a perpendicular orientation of the upper and lower dimers (Barciszewski et al., 2016). The cruciform-like R state of FBP2 is stabilized by a unique hydrophobic motif called ‘
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