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Drug drug interactions are frequently attributed to function
2020-03-21
Drug-drug interactions are frequently attributed to functional alterations in CYP enzymes, including inhibition and induction (Chen et al., 2014, Wang et al., 2013). Mechanism-based inhibition is an irreversible form of enzyme inhibition and could form a stable inhibitor-enzyme complex, which is tho
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br Additional CDKs with a role in cancer br Small
2020-03-21
Additional CDKs with a role in cancer Small molecule CDK inhibitors The majority of protein kinase inhibitors developed to date are type I inhibitors: they bind at the ATP–binding site, are ATP-competitive and target the kinase in its active state; with the activation loop DFG motif in the ‘in
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br Materials and methods br Results br Discussion We
2020-03-21
Materials and methods Results Discussion We confirmed the published cDNA and protein sequence of feline CSF-1R and stably cloned the cat receptor into the Ba/F3 cell line. Activation of feline CSF-1R by recombinant human CSF-1 was previously tested by Woolford et al. [14]. Expression of onc
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The synthesis of tricyclic analogs is described in Scheme Ox
2020-03-21
The synthesis of tricyclic analogs 28–33 is described in Scheme 3. Oxidative C–C bond cleavage of the terminal olefin of 39i afforded a tricyclic product 52 without isolation of an aldehyde expected as an intermediate. Aminolysis of the chloride 52 with optionally substituted anilines afforded 28–30
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br Making the BN Cox
2020-03-21
Making the BN-Cox model computationally efficient One of the challenges to applying the BN-Cox model is an exponential growth of the conditional probability tables (CPT) corresponding to the survival variables, as the number of risk factors increases [22]. When the number of risk factors is high,
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br Materials and methods br Results br
2020-03-20
Materials and methods Results Discussion Here we show expression of the EP1 receptor in the hippocampus of mice and the functional influence of the EP1 receptor on kainic AV-951 induced seizures. Mice lacking a functional EP1 receptor gene displayed a lower tendency to enter status epilept
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br Cytochrome P monooxygenases Cytochrome P monooxygenases P
2020-03-20
Cytochrome P450 monooxygenases Cytochrome P450 monooxygenases (P450s) belong to one of Nature’s most versatile group of enzymes for C–H functionalization and are able to perform challenging regioselective and stereoselective activations of remote, unactivated C(sp3)–H bonds, for which there are o
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Since ET was discovered first and showed a wide variety
2020-03-20
Since ET-1 was discovered first and showed a wide variety of actions not only on the cardiovascular system but also on various other tissues, much information has accumulated on ET-1 compared with the two other peptides. The method for measurement of ET-1 levels in plasma or various tissues by mean
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dihydroxycholesterol OHC was recently identified by classic
2020-03-20
7α,25-dihydroxycholesterol (7α,25-OHC) was recently identified by classic analytical methods as a high-affinity ligand for EBI2 (Hannedouche et al., 2011; Liu et al., 2011). 7α,25-OHC was previously identified as an intermediate in the alternate pathway of hepatic bile Canagliflozin synthesis (Russe
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Our data furthermore suggest that Ch h induced
2020-03-20
Our data furthermore suggest that Ch25h-induced oxysterols could play an important role in modulating the immune cell migration. Mechanistically, we observed impaired trafficking of CD44+CD4+ T cells in mice deficient for Ch25h. CD44+CD4+ T cells lacking EBI2, the receptor of 7α-25OHC, were delayed
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Spectinomycin hydrochloride hydrate br Materials and methods
2020-03-20
Materials and methods Results Discussion CDK and their regulatory cyclins form a family of heterodimeric kinases that are particularly important for regulation of Spectinomycin hydrochloride hydrate progression and transcription in tumor cells. These kinases therefore constitute biomarkers
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A phenylacetic acid derivative discovered in a high
2020-03-20
A phenylacetic Protease Inhibitor Cocktail (EDTA-Free, 200X in DMSO) derivative (), discovered in a high throughput screen for CRTH2, inhibited the binding of H-PGD to CRTH2 receptors on 293 cells with an IC of 0.010μM, and inhibited the binding of H-PGD to DP receptors with an IC of only 8.3μM ()
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By live imaging of GUL GFP we observed the
2020-03-20
By live imaging of GUL-1-GFP, we observed the kinetics of aggregate movement within the cell. One of the marked characteristics of GUL-1-GFP cytosolic (but not nuclear-associated) aggregate motion was a “comet-like” movement that was found to be dependent on the presence of properly polymerized micr
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Furthermore the determination of downstream target genes ind
2020-03-20
Furthermore, the determination of downstream target genes induced by CdCl2 is noteworthy and can help to define its underlying carcinogenesis mechanism. Therefore, we evaluated c-fos and c-jun expression which are stimulated by estrogen through ERK/MAPK pathway. These are not only proto-oncogenes wh
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Introduction Breast cancer is a
2020-03-20
Introduction Breast cancer is a highly prevalent malignancy. There are some recognized risk factors for breast cancer, like early menarche or late menopause, which increase the length of the exposure to hormones, as a result of a higher number of ovarian cycles [1]. Moreover, there is evidence supp
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