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br Concluding Remarks The effects of
2025-01-10
Concluding Remarks The effects of point mutations of the four ARs on ligand binding affinities, functional potencies, and efficacies constitute a valuable source of pharmacological information. We analyzed the existing data and mapped it on the collection of available AR crystal structures, allow
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Despite functional studies demonstrating the role of HT in
2025-01-09
Despite functional studies demonstrating the role of 5-HT in ureteral contractility, the source of endogenous 5-HT in the ureter is unclear. Since 5-HT-containing enterochromaffin cells, which are present in the gastrointestinal tract, could not be found in the ureter (Nocito et al., 2007, Ripoche,
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The c C T mutation identified
2025-01-09
The c.286C>T mutation identified in subject K20-1 was also reported in other ethnic groups, including Brazilian, French-Canadian, Italian, and Arabs from the United Arab Emirates [20], [21], [22], whereas c.318A>G mutation in subjects K10-1 was previously reported in Asian and Caucasians [13], [23],
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The first description of autophagy as a tumour suppression
2025-01-09
The first description of autophagy as a tumour suppression process arises from the observation that the initial step regulatory gene, Atg6/BECN1, was monoallelically lost in 40% to 75% of human prostate, breast, and ovarian cancers [31]. However, while BECN1 heterozygous mutant mice develop, with lo
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Over the past decade extensive research has been directed to
2025-01-09
Over the past decade, extensive research has been directed toward the discovery of Aurora-selective small-molecule inhibitors. As a result, a handful of Aurora inhibitors has been identified. Among them, 1 (VX-680) and 2 (SNS-314) have entered human clinical trials as pan-Aurora kinase inhibitors (F
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Here we report discovery of highly
2025-01-09
Here we report discovery of highly selective pan-Aurora kinase inhibitors through phenotypic screening. The co-crystal structure of (R)-PFI 2 hydrochloride australia bound in the ATP binding site of Aurora A is described, and provides insight into the possible structural basis for the selectivity
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The LO has so far
2025-01-09
The 15-LO-1 has so far only been found in humans and rabbit reticulocytes [3], [20] and the rabbit 15-LO-1 protein demonstrate 81% identity to the human 15-LO-1. However, rabbit monocytes express an enzyme with mainly 12-LO activity [20], [21]. The high degree of sequence conservation between these
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To introduce in a simple way the variability
2025-01-09
To introduce in a simple way the variability in the concentration of the proteins involved in the process, and to consider possible stochastic effects due to possible finite sizes of the populations involved in the problem, the dynamics of each cell is studied using the Gillespie’s algorithm (Gilles
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Therefore we have further investigated
2025-01-09
Therefore, we have further investigated the anti-oxidant activity of isogarcinol in vitro by measuring the scavenging of 2,2′-diphenyl-1-1picrylhydrazyl (DPPH) and 2,2′-azino-bia (3-ethylben-zothiazoline-6-sulphonicacid) (ABTS), and determining its reducing power and ability to prevent lipid peroxid
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In conclusion there are only
2025-01-09
In conclusion, there are only a few experimental reports evaluating the influence of Group I mGluR antagonist on allergy. With the exception of studies using macrolides, most point to their harmful effect on the severity of this disease. Future studies will be crucial to define the impact of antibi
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br AR mediated actions in cells of the vascular
2025-01-09
AR-mediated actions in SU(VAR)3-9 inhibitor of the vascular wall Sex hormones may influence the size and composition of atherosclerotic lesions indirectly by modifying systemic cardiovascular risk factors such as plasma lipids profiles and insulin sensitivity; this aspect of their action is disc
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The evidence points toward a role
2025-01-09
The evidence points toward a role for 12/15-LO activity in WAT in modulating chronic local inflammation and subsequent systemic metabolic decline in the obese state. However, little is known as to the role of 12- and 15-LOs in BAT. Indeed, in addition to WAT, platelet- and leukocyte-type 12-LO are e
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Blocking the action of CREB with the C inhibitor together
2025-01-09
Blocking the action of CREB with the C646 inhibitor together with increasing Akt activation with the SC79 agonist is particularly interesting as it significantly reduced wound closure time from 7 days (which is required for complete closure of control hTECs exposed to DMSO) to only 4 days (when hTEC
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br Rapid nongenomic effects of corticosterone in an
2025-01-08
Rapid nongenomic effects of corticosterone in an amphibian model Studies in the model organism, the roughskin newt, Taricha granulosa, over 30 years ago led to the discovery that stress can rapidly (within minutes) suppress sexual behavior (amplectic clasping) of male T. granulosa, an effect that
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To examine whether the interaction between mGlu and adrenerg
2025-01-08
To examine whether the interaction between mGlu7 and α1-adrenergic receptors could be confirmed at a behavioural level, we performed the FST in mice. This test has value in predicting the antidepressant-like effect of drugs or environmental manipulations (Krishnan and Nestler, 2008, Krishnan and Nes
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