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It is interesting to note that our results
2021-01-23
It is interesting to note that AS-605240 our results show a very similar behavior in binding of DDR2 ECD to immobilized a-telo (bovine-dermal) versus telo- (rat-tail) collagen I as a function of its oligomeric state. Thus, the telopeptide region of tropocollagen exerts little influence on DDR2-colla
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In conclusion this study indicated that D tripetala and
2021-01-23
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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Herbal products may alter the metabolism
2021-01-23
Herbal products may alter the metabolism of certain drugs and, likewise, the metabolism of components of herbal products may be altered by some drugs, specifically those that affect cytochrome P450 Tranilast (CYP). These can bring about an alteration of the pharmacokinetics and pharmacological activ
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PHA-793887 The current study demonstrates a link between
2021-01-23
The current study demonstrates a link between heme metabolism and mitochondrial Co-I, which deficits instigate abnormalities in the metabolism of heme and its downstream targets both in-vitro in patients and healthy subjects derived LCLs and in-vivo in brains of SZ-rat model. A further study of the
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From a mechanistic standpoint the BCL
2021-01-23
From a mechanistic standpoint, the BCL6 RD2 domain represses the GPR183 and S1PR1 loci by recruiting HDAC2, but not MTA3-NuRD, to suppress the enhancer activation mark H3K27ac at their distal regulatory elements. However, these data do not exclude the possibility that other as yet unknown corepresso
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Collectively our results indicate that GSK A functions as a
2021-01-23
Collectively, our results indicate that GSK682753A functions as a competitive antagonist and binds to the receptor in the same region as 7α,25-OHC. First, we observe linearity in the Schild plot analysis (Fig. 2B). Second, GSK682753A is highly dependent on F111 at position III:08/3.32 in TM-III (Fig
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Although our knowledge of the biochemical and biological
2021-01-23
Although our knowledge of the biochemical and biological functions of E3 ubiquitin ligases has increased in B-cell malignancies, a deeper characterization of cell-context dependent substrate regulation and biological relevance is needed. The recent approval of a general proteasome inhibitor, VELCADE
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br Results and discussion br Conclusion We have
2021-01-23
Results and discussion Conclusion We have constructed a series of potent and greatly selective DPP-4 inhibitors with pyrazolo[1,5-a]pyrimidin-7(4H)-one core surrogates. The modification of the core led us to b2 which has IC50 of 80 nM and > 1000 fold selectivity over DPP-8 and DPP-9. We utiliz
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Addressing whether impaired activation of D and
2021-01-23
Addressing whether impaired activation of D1 and D2 receptors regulates memory capacity is relevant for all human pathologies that lead to reduced activation of these NVP 231 pathways, such as ageing [39], certain genetic polymorphisms [40] and neurodegenerative disorders. In this study, we have te
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Given the widespread occurrence of
2021-01-22
Given the widespread occurrence of oncogene-induced RS and the increasing clinical interest in small molecule inhibitors that further exacerbate RS in human cancers (such as ATR inhibitors), our findings point to a protective role for RAD52 in the maintenance of cancer cell viability. As such, RAD52
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To elucidate the potential mechanism underlying osteosarcoma
2021-01-22
To elucidate the potential mechanism underlying osteosarcoma cell growth decrease by CDK4 inhibition, flow cytometry analysis was used to determine oxygenase and apoptosis in human osteosarcoma cells after palbociclib treatment. The results showed that osteosarcoma cells were arrested in G1 phase o
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br Materials and methods br Results br Discussion
2021-01-22
Materials and methods Results Discussion In this study, we investigated two novel candidate therapeutics, the related CRM1-inhibiting SINEs KPT-185 and KPT-276, in treatment of NHL. The results showed that KPT-185 induced growth inhibition, cell-cycle arrest, and apoptosis in tumor AZD1152
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Nicotine is the main psychoactive component of tobacco that
2021-01-22
Nicotine is the main psychoactive component of tobacco that causes addiction. Besides the regulation of the stress responses, CRF has been implicated in nicotine addiction based on several lines of evidence (Bruijnzeel and Gold, 2005, Sarnyai et al., 2001). First, acute administration of nicotine, l
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ppar pathway Introduction The carnitine choline acyltransfer
2021-01-22
Introduction The carnitine/choline acyltransferase family is a family of enzymes that play diverse roles, ranging from (the regulation of) ppar pathway and fuel metabolism in mitochondria and peroxisomes to the generation of the neurotransmitter acetylcholine. In mammals, this family consists of s
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During the past decades HT had been widely prescribed with
2021-01-22
During the past decades HT had been widely prescribed with the expectation of both osteoporosis and cardiovascular disease prevention. The results of the Women's Health Initiative (WHI) trial, however, indicated that long-term HT use is associated with a small but significant increase of cardiovascu
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