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br Acknowledgements This work was supported in part by JSPS
2020-07-03
Acknowledgements This work was supported in part by JSPS KAKENHI Grant Number 26292031. Introduction The Cys-loop receptors constitute an important superfamily of ligand-gated ion S63845 (LGICs) and mediate synaptic transmission in both invertebrate and vertebrate nervous systems (Jones et a
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ClC is not only a chloride ion channel but also
2020-07-03
ClC-3 is not only a chloride ion channel but also a regulatory protein involved in the regulation of multiple signaling pathways. The PI3K/AKT/mTOR signaling pathway plays a crucial role in regulating cell growth, migration, invasion, and distant metastasis [13,14]. Although abnormal PI3K/AKT/mTOR a
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An ideal CHK inhibitor would be minimally cytotoxic while
2020-07-03
An ideal CHK-1 inhibitor would be minimally cytotoxic, while enhancing the anti-tumor effect of a real cytotoxic agent that would be used in combination with the inhibitor. Our CHK-1 inhibitors have shown excellent selectivity over a panel of kinases including those regulating the cell cycle, but th
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Due to its several industrial applications
2020-07-02
Due to its several industrial applications, the recombinant production of collagen and all its derivatives as gelatins has been pursued for many years in different biological systems as mammalian GYKI 52466 dihydrochloride (Toman et al., 1999), tobacco plants (Ruggiero et al., 2000), silkworms (Tom
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br Concluding remarks A crucial
2020-07-02
Concluding remarks A crucial step in the microbial degradation of steroids is the 1(2)-dehydrogenation of the steroid nucleus by FAD-dependent Δ1-KSTDs. This step is required to initiate the opening of the steroid nucleus under both aerobic and anaerobic conditions. A large variety of steroid-deg
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br DDR in atherosclerosis and
2020-07-02
DDR1 in atherosclerosis and vascular disease The Canadian group of Bendeck, explored the role of DDR1 in repair following arterial injury in rats [30]. DDR1 protein levels, assessed via Western blots prepared from arterial extracts taken at various times after injury, showed DDR1 protein dramatic
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Testosterone is inactivated through hydroxylation and conjug
2020-07-02
Testosterone is inactivated through hydroxylation and conjugation pathways [3], [4]. 6β-Hydroxylation is the main pathway among testosterone hydroxylation processes in the liver microsome. Testosterone 6β-hydroxylation is mainly catalyzed by cytochrome P450 3A (CYP3A) [5], [6], which is expressed in
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An important strength of our study is the use
2020-07-01
An important strength of our study is the use of an elastic net regression model to select the variable and construct the model, which performed ideally in terms of both predictive accuracy and sparsity for the high-dimensional datasets [16]. As a result, the apparent predictive effect of multiple c
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In summary the loss of seven
2020-07-01
In summary, the loss of seven Cyp3a genes lead to sexual dimorphic changes during the eight weeks of high fat diet treatment with Cyp3a-null female mice showing a healthier acclimation to a high fat diet through decreased weight gain, higher adiponectin, lower B-OHB levels, and a better response to
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Compounds were screened for their activity against
2020-07-01
Compounds were screened for their activity against the hERG channel, with the 2,3-Cl compounds more active here than the 2,4-F compounds. The homopiperazine examples (, , , ) showed increased hERG activity relative to the corresponding piperazines. The cell data for the 6,7-dimethoxyquinoline compo
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We have previously disclosed the discovery of a azaindole ac
2020-07-01
We have previously disclosed the discovery of a 7-azaindole-3-acetic SCH 23390 hydrochloride receptor CRTh2 antagonist chemotype 1 from HTS and its subsequent optimization to give 2 as a potent and orally bioavailable inhibitor of eosinophil shape change (SC) in human whole blood. Subsequent to dis
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Collectively these data suggest the potential clinical utili
2020-07-01
Collectively, these data suggest the potential clinical utility of COMT inhibitors for the treatment of addiction disorders. Similar to current pharmacotherapies such as naltrexone, tolcapone\'s effects were not ethanol specific, therefore tolcapone may be effective in reducing other drug reinforced
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apomorphine receptor br Acknowledgements br Introduction Pro
2020-07-01
Acknowledgements Introduction Protein–tyrosine phosphorylation, catalyzed by protein–tyrosine kinases and protein–tyrosine phosphatases, has a pivotal role in the regulation of a wide variety of cellular processes. Similar numbers of tyrosine kinases and tyrosine phosphatases are encoded by th
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The Fontan circulation When first
2020-07-01
The Fontan circulation When first described in 1971, the Fontan operation ushered in a new paradigm in the care of children born with the varied forms of complex congenital AEBSF mg disease (CHD) characterized by a single effective pumping chamber.1., 2. This procedure, which creates a total cavopu
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Cetylpyridinium Chloride br Non cyclic nucleotide EPAC regul
2020-07-01
Non-cyclic nucleotide EPAC regulators Despite the success of 007 as a tool molecule, few studies to date have led to the identification of further EPAC-selective agonists. The most studied and controversial group of small-molecule EPAC regulators are the sulfonylurea (SU) family. SUs (Table 1) su
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