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These studies suggested that PV PVH might promote bone forma
2019-08-23

These studies suggested that PV/PVH might promote bone formation activities and/or inhibit bone resorption activities probably due to its anti-inflammation activity; however, the underlying mechanism remained unknown. Furthermore, it is unclear if PVH shows better activity than that of PV; this is i
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Compounds that interact with MDR can do
2019-08-23

Compounds that interact with MDR1 can do so by different mechanisms. Verapamil is known to modulate drug resistance by acting as a competitive MDR1 substrate [36]. Interestingly, NU7441 has similar growth inhibitory activity in the sensitive and resistant progesterone receptor and there was no obse
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DNA bound Ku proteins recruit DNA PKcs and thereby
2019-08-23

DNA-bound Ku proteins recruit DNA-PKcs; and thereby translocate into the duplex by one helical turn, leaving DNA-PKcs near the DNA terminus to assist in tethering the broken ends together [25]. In addition to keeping the DSBs in close proximity, DNA-PKcs may prevent exonucleolytic degradation of the
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Although DGK is a lipid modulating enzyme the
2019-08-23

Although DGKγ is a lipid-modulating enzyme, the role of DGKγ in integral cell metabolism has not been reported. We found that DGKγ made a difference on cell metabolism profile in HCC cells, which may be caused partially by the downregulation of GLUT1. Glucose is a major source of energy, and decreas
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Targeting both PARP and DHODH for anti cancer therapy
2019-08-23

Targeting both PARP-1 and DHODH for anti-cancer therapy would certainly be beneficial as these enzymes share a common role in the DNA replication and repair mechanisms which are involved in the hyper-proliferation of cancer cells. Since benzimidazole-containing compounds have been reported to show
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br Materials and methods br Results br
2019-08-23

Materials and methods Results Discussion GOS potently inhibited SRD5A1 in COS-1 cells (Fig. 4A) and rat Leydig cells (Fig. 4B), possibly attenuating testosterone activation into DHT. It has been reported that gossypol inhibited human SRD5A1 with IC50 of 7 × 10−6 M [28]. Interestingly, gossy
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Beside the previously reported Topo
2019-08-23

Beside the previously reported Topo I inhibition, time and concentration dependent CRM1 inhibitory properties of klavuzon derivatives have been shown as a second mechanism of action in this work. Especially, compounds 3 and 20 are the most effective derivatives and they completely inhibit CRM1 activ
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In rats exposed to day of nicotine withdrawal h after
2019-08-23

In rats exposed to 1 day of nicotine withdrawal (24 h after the last nicotine administration) we expected a decrease of general locomotor activity and a decrease of global striatal dopamine release, which were assessed in a previous study following 14 days of nicotine exposure and 24 h of nicotine w
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br Conclusions Taken together a
2019-08-23

Conclusions Taken together, a distinct contrast is observed between ERK1/2 phosphorylation in hypothalamic and extra-hypothalamic Difopein regions. The hypothalamus is the only brain region where ERK1/2 phosphorylation was increased 15minutes after the OF stressor. In SD rats CRFR1 expression wa
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P H is a nonheme iron II dioxygenase that uses
2019-08-23

P4H is a nonheme iron(II) dioxygenase that uses O2 and α-ketoglutarate as co-substrates (Fig. 1A). The three-dimensional structure of mammalian P4H is unknown. We reasoned that an electrophilic analog of α-ketoglutarate could serve as an irreversible inhibitor of the enzyme and, hence, a useful prob
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From the results of previous experiments with the
2019-08-23

From the results of previous experiments with the purvalanol B affinity matrix, it is not clear whether the selective capture of parasite CK1 enzymes is a reflection of their high abundance or rather their affinity for the ligand compared with other kinases present in the lysates. Based on compariso
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Replacement of the saturated propoxy group in
2019-08-23

Replacement of the saturated -propoxy group in compound with the unsaturated allyloxy group to obtain compound resulted in 10-fold decrease in ET receptor antagonism and more than 20-fold decrease in ET-selectivity. Analogous unsaturated allyloxy compound in the tetrazole series was found to have
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Diacylglycerol kinase was one of the hits identified from th
2019-08-22

Diacylglycerol kinase was one of the hits identified from the RNAi screen. Diacylglycerol kinases are conserved across a Sotalol of species with more complex, multicellular organisms possessing several DGKs with differing protein domains, expression patterns and functions [61], [62], [63]. Some of
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There are some limitations to
2019-08-22

There are some limitations to our study. First, the small sample size, even if comparable or higher than most studies, did not offer the possibility to consider other variables, such as frequency of use or age of onset. Second, since most subjects did not report current use, we could not analyze sep
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br Discussion Immune response to CMV is a
2019-08-22

Discussion Immune response to CMV is a series cell-mediated immune response initiated by innate innate NK cells, followed by adaptive CD8+ and CD4+ T cells and humoral immunity by B cell [3]. Prior to transplant, measurement of humoral immune responses (CMV serology) of donor and recipient is com
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