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MMV s distinct mode of inhibition addresses key impediments
2021-11-02
MMV019313's distinct mode of inhibition addresses key impediments in the development of PfFPPS/GGPPS inhibitors as antimalarial drugs. First, it is the first non-bisphosphonate inhibitor of Plasmodium FPPS/GGPPS with drug-like physicochemical properties satisfying the “Rule of 5” (Van Voorhis et al.
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Several classes of small molecule
2021-11-02
Several ABT199 of small-molecule inhibitors of FBPase have been reported. These inhibitors can be structurally classified into two groups; non-phosphorus-based inhibitors and phosphorus-based inhibitors. In the former group, several chemotypes including anilinoquinazoline, indole dicarboxylic acid,
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br H R agonists In search for potent and
2021-11-01
H2R agonists In search for potent and selective H2R agonists, comprehensive structure–activity relationship studies have been conducted and led to the first H2R agonists, e.g. 4(5)-methylhistamine (16) which is actually now used as selective H4R agonist (Fig. 4) (Durant et al., 1975, Lim et al.,
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Mirtazapine synthesis A recent novel and important finding i
2021-11-01
A recent novel and important finding is that YAP connects cellular growth with anabolism; YAP suppresses the transcriptional induction of genes which importantly regulate gluconeogenesis in the liver; namely glucose-6-phosphatase catalytic subunit (G6PC) and phosphoenolpyruvate carboxykinase 1 (PCK1
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The transcription factor Nrf is a
2021-11-01
The transcription factor Nrf2 is a master regulator of cytoprotective responses to endogenous and exogenous stresses caused by reactive oxygen species (ROS) and electrophiles [6]. Nrf2 promoter polymorphisms are significantly associated with the development of gastric mucosal inflammation, either in
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br Acknowledgments Authors are thankful to the participants
2021-11-01
Acknowledgments Authors are thankful to the participants of the study for their cooperation. Financial support from Higher Education Commission (HEC) of Pakistan is highly acknowledged. AZ is supported by indigenous PhD fellowship from HEC. Indigenous PhD Fellowship for 5k Scholars batch 2 PIN NO
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In an attempt to gain
2021-11-01
In an attempt to gain increased molecular insights into in vivo transmigration of neutrophils, we applied an aseptic inflammatory skin chamber model. In this model, recruitment of neutrophils is typically associated with phenotypic changes of many plasma membrane localized adhesion receptors in peri
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Several studies have found that
2021-11-01
Several studies have found that GPR55 possesses a distinct pharmacology from that of CB1 and CB2, and that only certain cannabinoids act at this receptor. In transfected myelin basic protein synthesis expressing hGPR55, out of more than 20 synthetic and endogenous cannabinoids evaluated, only 2 com
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For a long time the mechanism for the
2021-11-01
For a long time, the mechanism for the TG-lowering effect of nicotinic TCS 359 has been thought that the lowered NEFA substrate from adipose tissue limits TG production from the liver (so-called NEFA hypothesis) [[1], [2], [3], [4]]. However, recent emerging evidences have suggested the involvement
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Introduction Molecular imprinting technology is a method tha
2021-11-01
Introduction Molecular imprinting technology is a method that combines the material chemistry, biochemistry, and polymer chemistry and has the ability to specifically identify target analytes on shape, size and functional groups. Molecular imprinting polymer (MIP) is developed based on molecular i
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br Expression of GlyT in the spinal cord in
2021-11-01
Expression of GlyT in the spinal cord in response to neuropathic pain Twelve days after sham injury or CCI, GlyT1 and GlyT2 mRNA expression in rat spinal cord was analyzed using qPCR. Here, no significant changes in expression of the transporters in our CCI model of neuropathic pain compared with
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br Methods and materials br Results To
2021-11-01
Methods and materials Results To examine the fear conditioning effects of the pre-exposure, drug, and sex factors in the total latency time, a 2 × 3 × 2 three-way ANOVA indicated that WEHI-539 significant differences occurred in the drug (F2109 = 14.44, p 0.05) and pre-exposure × sex (F1109
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br Acknowledgment br Introduction Positive and negative rein
2021-11-01
Acknowledgment Introduction Positive and negative reinforcement are known as the two pivotal components in various models of drug dependence. Compulsive drug seeking behavior results from both the euphoric effects of drug use (positive reinforcement) and the unpleasant withdrawal signs followi
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Although EAAT may not be involved in the induction of
2021-11-01
Although EAAT3 may not be involved in the induction of morphine-induced CPP, our results suggest that other EAATs may play a role in the behavior because riluzole, an EAAT activator (Frizzo et al., 2004, Fumagalli et al., 2008), abolished morphine-induced CPP. Consistent with this suggestion, a few
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Activation of Akt signaling is common
2021-11-01
Activation of Akt signaling is common in nearly all of the human malignancies (Altomare & Testa, 2005). It has been reported that microRNA-200c targets Akt signaling pathway to inhibit cell apoptosis of pituitary adenoma (Liao et al., 2014). In addition, Akt signaling pathway regulates the expressio
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