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stavudine synthesis The action of pt PGE as an
2021-06-28
The action of 17-pt-PGE2 as an EP1 receptor agonist [34] was demonstrated in several experimental settings, including cancer, neurons, vascular system, kidney and was confirmed by application of EP1 receptor selective antagonists [35], [36], [37], [38], [39], [40], [41]. Receptor binding studies in
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Another interesting finding regarding substrate
2021-06-28
Another interesting finding regarding substrate selectivity of iPLA2-VIA in whole cellular systems stems from the observation that some of the major species hydrolyzed by the enzyme contain a 16:1 fatty Artemisinine synthesis at the sn-2 position [57,119], raising the possibility that iPLA2-VIA may
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A novel series of DHODH inhibitors was developed
2021-06-28
A novel series of DHODH inhibitors was developed by us based on a lead that was discovered during a docking procedure and medicinal chemistry exploration. The activity of the initial lead was improved by a QSAR method and yielded low nanomolar inhibitors. Introduction The most common metabolic h
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ck1 inhibitor Our recent discovery M P H R A
2021-06-28
Our recent discovery (M.P., H.R., A.S.) of a highly selective and in vivo active DDR1 small-molecule inhibitor provides evidence that DDR1 is a druggable pharmaceutical target, and some details of our efforts are provided below. To avoid the repurposing of known kinase inhibitor structural motifs, w
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The significant CRF increase in the
2021-06-28
The significant CRF increase in the DS and the overall changes in the CRF system observed in the VM and DS during the development of sensitization suggest that this neuropeptide (and possibly urocortin) contributes to the specific molecular alterations occurring in the mesolimbic pathway that suppor
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br Materials and methods br Results br Discussion
2021-06-25
Materials and methods Results Discussion Persimmon tannin has been reported to have the bile acid binding ability in vitro (Matsumoto et al., 2011) and hypolipidaemic effects in animals (Matsumoto et al, 2008, Zou et al, 2012). Our previous study also proved that persimmon tannin promoted t
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More recently it was discovered that BChE hydrolyzes the
2021-06-25
More recently, it was discovered that BChE hydrolyzes the neuropeptide gut hormone, ghrelin [25], [26], [27], [28]. Nonetheless, because the enzyme reaction is very slow, those who first reported this finding were initially reluctant to attribute a real physiological role for that phenomenon. Our ow
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alcohol inhibitor Here we report for the first time
2021-06-25
Here, we report for the first time that EphB4 contains two NLS sequences and localises to the nucleus. This is mediated via an importin-α pathway and we show that EphB4 could potentially have a direct role in gene regulation. These data provide new insight into Eph receptor localisation and action a
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Among the down regulated genes were several of interest
2021-06-25
Among the down-regulated genes were several of interest. Coronin2a (Coro2a), a component of the nuclear receptor co-repressor complexes, contributes to de-repression of inflammatory response genes (Huang et al., 2011). Mill1, an MHC family member expressed in hair follicles, represses wound healing
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Related with the studies by Zizza
2021-06-25
Related with the studies by Zizza et al. described above [66], work by Ward et al. [68] suggested that the C2 domain of cPLA2α, which binds to zwitterionic membranes with high affinity in a Ca2+-dependent manner, has a high membrane remodeling activity, producing dramatic changes in membrane curvatu
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This relative lack of ET expression
2021-06-25
This relative lack of ET-1 expression in highly malignant epithelial fxr agonist could be explained by marked cellular anaplasia and cellular dysfunction; we also suggest that the high levels of VEGF, which have been evidenced in highly malignant mammary tumours (Restucci et al., 2002) may suppress
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Collectively the results presented here provide new insights
2021-06-25
Collectively, the results presented here provide new insights into ligand binding, clustering, spatial distribution, and phosphorylation of DDR1b and DDR2 in response to soluble collagen I. As depicted in the cartoon of Scheme 1, we postulate a model in which the spatial distribution and assembly of
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br Conclusions br Introduction The terms
2021-06-25
Conclusions Introduction The terms endocrine active and endocrine disruptive have been used to describe an ever-expanding list of naturally-occurring and synthetic compounds that interact with mammalian hormonal systems, and in particular, the reproductive system. These compounds have been ass
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Moving forward the new mathematical
2021-06-25
Moving forward, the new mathematical model opens doors for understanding the SCF network, where activity of a component is blunted through mutation or altered in expression in diseased states, and during therapeutic intervention. Computational modeling could reveal underappreciated secondary or tert
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SC 79 br Materials and methods br Results br
2021-06-25
Materials and methods Results Discussion Plant U-box E3 Ub ligases regulate diverse plant-specific cellular processes [1], [2], [3], [4]. However, structural and functional relationships between U-box E3s and their E2 partners are largely unknown in higher plants [24], [25]. In this study,
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