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Our co IP data show that
2023-11-03
Our co-IP data show that 5HT1A or 5HT2A receptors do not heterodimerize with mGluR1α receptors. Given that both 5-HT and mGlu receptors are GPCRs and produce anxiolytic effects, a degree of cooperativity via a functional cross-talk may still exist between these receptors [11]. In addition to the fun
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Compound was docked into the active site of Aurora B
2023-11-03
Compound was docked into the active site of Aurora B kinase using Tripos sybyl-X ver. 2.1.1. The crystal structure of human Aurora B kinase cocrystallized with its potent inhibitor VX-680 was used for the docking analysis (PDB ID: ). The most likely binding conformations were selected based on the d
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The take home message here is that although Aurora
2023-11-03
The take-home message here is that, although Aurora A phosphorylated on T288 is the activated isoform of Aurora A, measuring the level of phosphorylation of T288 does not reflect Aurora A kinase activity (Figure 5). What would be the most appropriate readout for an in vivo Aurora A kinase activity
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Although plant Aurora kinases can be clearly grouped into fu
2023-11-03
Although plant Aurora kinases can be clearly grouped into functional clades, the roles of the respective clades does not seem to be evolutionarily conserved. AtAurora 1 labels kinetochore microtubules [19], similarly to mammalian Aurora A, while its targeting to the cell plate resembles features of
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Pamidronate Disodium br Materials and methods br
2023-11-03
Materials and methods Results Discussion In this study, the orphan receptor GPR25 was cloned from several representative vertebrate species including zebrafish. Although the overall amino Pamidronate Disodium sequence identity among these species is not high (38–52%), our synteny analysis
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The putative residue apelin proprotein
2023-11-03
The putative 55-residue apelin proprotein (proapelin or apelin-55) is processed from a 77-residue preproprotein through removal of a 22-residue signal peptide (Table 1). Apelin-55 is further processed into bioactive isoforms of 36, 17, or 13 residues, likely through protease-mediated mechanisms. To
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br Introduction Sustained over activation of neurohormonal s
2023-11-03
Introduction Sustained over-activation of neurohormonal systems is a hallmark in the pathophysiology of cardiac dysfunction following myocardial infarction (MI) and heart failure (HF). Inhibitors of the renin-angiotensin SU11274 receptor system (RAAS) constitute cornerstones of pharmacotherapy f
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An important observation is that
2023-11-03
An important observation is that this patient has been on ALK inhibitor for more than 4 years (51 months: 27 months on crizotinib+24 months on alectinib and on-going) and there was no evidence of disease progression in the central nervous system. The other potential driver mutation in this patient’
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Gratifyingly compound also demonstrated improved physicochem
2023-11-03
Gratifyingly, compound also demonstrated improved physicochemical properties with significant improvement in aqueous solubility. Compound was sufficiently potent to determine its pharmacokinetic (PK) and pharmacodynamics (PD); data is summarized in . shows ADME characteristics for compound and
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ataluren br Discussion With recently improved understanding
2023-11-03
Discussion With recently improved understanding of the role of βARK1 in the progression of HF and as a potential therapeutic target in HF, we explored the relationship between plasma βARK1, as a marker of chronic sympathetic overactivation, and physical symptoms in HF. Our main findings were 1) e
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IC values were obtained for an expanded
2023-11-02
IC50 values were obtained for an expanded version of the fragment library using the previously described mobility shift assay. Subsequently, Ki values were estimated from IC50 values to allow better comparison of the activity against targets which were measured at different substrate concentrations
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In pancreatic islets we found an increase
2023-11-02
In pancreatic islets we found an increase in protein expression of leukocyte 12/15-LO that paralleled the metabolic decline characterized by severe hyperglycemia and reduced islet numbers. Similar increase in 12/15-LO expression by Western blot was found in the control mice, which have a normal meta
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Besides Arg overexpression our data revealed that AGEs could
2023-11-02
Besides Arg2 overexpression, our data revealed that AGEs could decrease eNOS mRNA levels, which is considered a significant cause for attenuated NO production and vasodilation. It was found recently that AGEs significantly reduce eNOS expression levels and NO bioavailability in human carotid artery
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Go 6976 Introduction Enzymatic browning degrades quality saf
2023-11-02
Introduction Enzymatic browning degrades quality, safety, and nutritional values of various fruits or vegetable products. For example, the color of apple or potato is generally yellowish, representing freshness. However, they are extremely susceptible to enzymatic browning because of abundant polyp
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Despite the absence of disulfide bonds in its
2023-11-02
Despite the absence of disulfide bonds in its linear structure, KT43C displays antifungal and antibacterial activity. Disulfide bonds are determinants of defensins' integrity and have been reported to increase the antimicrobial activity (Jenssen et al., 2006). However, some linear derivatives of AMP
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