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In our previous research we have focused
2020-06-17

In our previous research, we have focused on the discovery of novel VEGFR-2 inhibitors as anti-angiogenesis agents. Numbers of biphenyl-aryl urea incorporated with salicylaldoxime including BPS-7 have been developed as potent and selective VEGFR-2 inhibitors (Fig. 3) [12], [13], [14], [15], [16], [1
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In conclusion this study indicated that D
2020-06-17

In conclusion, this study indicated that D. tripetala and A. melengueta extracts inhibited CYP 3A enzyme both in vitro and in vivo. Although these inhibitions may appear to be weak from the US FDA classification point of view, caution must be applied in the concurrent use of herbal preparations cont
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In contrast to SQLE HMGCR could be efficiently degraded
2020-06-17

In contrast to SQLE, HMGCR could be efficiently degraded in Boc-D-Asp(OtBu)-OH.DCHA lacking UBE2J2. However, this was not the case in cells devoid of UBE2G2, as these cells were unable to support 25-hydroxycholesterol (25-HC)-stimulated degradation of HMGCR (Fig. 1C). This finding is consistent wit
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Inflammatory action of certain cytokines can influence
2020-06-17

Inflammatory action of certain cytokines can influence cell proliferative routes (Deshmane et al., 2009). When mTOR is inhibited, for instance by the action of Rapa, TGF-β1, which has an anti-inflammatory action, is increased. The relationship between high levels of TGF-β1 and Cy3 azide arrest has
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A previous report demonstrated that
2020-06-17

A previous report demonstrated that DA-dependent oxidative stress may be the initial event in MA neurotoxicity (Cubells et al., 1994). Oxidative burdens at early stage might be a prerequisite for neurotoxic scenarios induced by 3-FMA, and they are in line with MA case (Shin et al., 2012, Shin et al.
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During the past decade it became increasingly
2020-06-16

During the past decade, it became increasingly clear that the affinity and efficacy of small agonists acting on the orthosteric binding site of a GPCR can be modulated by ligands that bind to a topographically distinct (allosteric) binding site on the same GPCR molecule 33, 39, 40, 41, 42. This allo
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Compound was advanced to a chronic efficacy study in
2020-06-16

Compound 52 was advanced to a chronic efficacy study in db/db mice maintained on a high fat diet. Animals were dosed with 0.5% methylcellulose vehicle, ion channel 52 (1, 3 or 15mg/kg, po, Q.D.) or 1 (0.3mg/kg) for 14days. Over the course of the study body weight and food intake were measured daily
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The data in our manuscript confirm
2020-06-16

The data in our manuscript confirm previous data on the origin of CMV-specific T HOSu receptor following TCD alloSCT in CMV seropositive patients transplanted with a CMV seronegative donor (R+D−) and demonstrate that also recipient CMV-specific memory T-cells are able to survive alemtuzumab based T
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Many PIM inhibitors have been
2020-06-16

Many PIM inhibitors have been reported to date [7], [8], [9] however, none of them has been marketed so far. SGI-1776 is a representative first-generation PIM inhibitor, which had been under clinical trials for leukemia and prostate cancer [10]. While most of the first-generation PIM inhibitors are
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Thus the exact mechanisms responsible for progestogen
2020-06-16

Thus, the exact mechanisms responsible for progestogen-induced changes in immune response are not known but the effects are believed to be exerted through receptor-mediated interactions. Since the mPR α is known to be a G protein-coupled receptor in fish, downstream signaling cascades via secondary
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br Materials and methods br Results br Discussion Endothelia
2020-06-15

Materials and methods Results Discussion Endothelial cells are crucial for both vascular homeostasis and protecting the vasculature against atherogenic insults [3]. OxLDL-mediated injury to endothelial cells is crucial for endothelial dysfunction in the pathogenesis of atherosclerosis and a
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In addition to cleaving ubiquitins off modified proteins DUB
2020-06-15

In addition to cleaving ubiquitins off modified proteins, DUBs can also cleave between ubiquitin moieties within a polyubiquitin chain to edit the ubiquitin signal. DUBs employ different strategies to recognize polyubiquitin (Figure 1). DUBs that rely only on interactions on the S1 site tend to be E
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br Acknowledgments Grant support was
2020-06-15

Acknowledgments Grant support was provided by the Leading Academic Discipline Projects of Shanghai Municipal Education Commission (J5028) (J50201) to Dr. Mi, the China National Science Foundation Project (81072076) to Dr. Mi, the China National Science Foundation Project (31000349) to Dr. Shen, a
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In this contribution herein we report our newly devised
2020-06-15

In this contribution, herein we report our newly devised molecular probes with a triazole linked benzimidazole-indole-thiazolium mixed heterocyclic framework as depicted in Scheme 1. Their architecture was designed to achieve the advancement in selectivity and specificity toward DNA matrix over RNA
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We used two different VSMCs cell lines KSB
2020-06-15

We used two different VSMCs cell lines, KSB and CSD (isolated from two different thoracic aortas). Rat aortic VSMCs were isolated from medial segments from thoracic rate lcz696 from Wistar-Kyoto rats (six to eight weeks old, Charles River Wiga GmbH) and cultured over several passages as described .
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