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Having taken a step back from
2024-10-31
Having taken a step back from affinity to gain better exposure and solubility, we started work to replace the unstable oxazolinone, and address the selectivity over the hERG channel. Keeping in mind the binding mode of the series from crystal structures, triazole was identified as another mildly aci
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rilpivirine Molecular docking quantitative structure activit
2024-10-30
Molecular docking, quantitative structure–activity relationship (QSAR) and high-throughput virtual screening (HTVS) studies have a very widespread use in computer-assisted drug design.25, 26, 27, 28 Suvannang et al. used the published X-ray crystallographic data to examine known aromatase inhibitors
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br Physiology of the apelin pathway
2024-10-30
Physiology of the apelin pathway Role of apelin in heart disease Both apelin and apelin receptor null mice manifested moderate reduction in cardiac contractile function under basal conditions and their exercise capacity was markedly reduced (Table 1) [56]. Apelin has direct effects on the prop
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Vascular interventional radiology VIR laboratories perform a
2024-10-30
Vascular interventional radiology (VIR) laboratories perform a myriad of procedures ranging from simple tunneled peripherally inserted central catheter lines to complex transjugular intrahepatic portosystemic shunt placements. Infections are a common complication in the VIR environment; thus, the pr
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Finally intracrine androgen synthesis metabolism can be acti
2024-10-30
Finally, intracrine androgen synthesis/metabolism can be activated thus allowing S/GSK1349572 receptor to bypass the low levels of androgens in the circulation by producing androgens themselves (Cai and Balk, 2011, Rahman et al., 2004). Moreover, changes in AR co-regulators like the overexpression
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PD 151746 receptor br Depletion of serum amino
2024-10-30
Depletion of serum amino acids Currently, the only anticancer agents that directly target amino PD 151746 receptor metabolism are bacterial l-asparaginases (from Escherichia coli and Erwinia chrysanthemi), which are FDA-approved for treatment of pediatric and adult ALL. A potential complication
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br ABCA and cancer drug response Overall the expression of
2024-10-30
ABCA2 and cancer drug response Overall, the expression of ABC transporters has been linked with multidrug resistance phenotypes through the efflux of drugs via ATP-dependent transport. For example, 13 distinct transporters (ABCA2, ABCB1, ABCB4, ABCB11, ABCC1–6 ABCC10, ABCC11 and ABCG2) have been
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G has been shown to
2024-10-30
Gβγ has been shown to participate in various MT-dependent processes such as cell growth and differentiation [15,[21], [22], [23], [24], [25], [26]]. G-protein β-subunit anti-sense oligonucleotides have been shown to inhibit cell proliferation and cause disorganization of the mitotic spindle in mamma
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br Detection and possible treatments for prostate
2024-10-30
Detection and possible treatments for prostate cancer PC can be diagnosed, by screening for prostate-specific antigen (PSA) and after diagnosis, treatments may include intense observation, radical prostatectomy, radiation, chemotherapy, hormone therapy or vaccination depending on the type and sta
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The next level of possible
2024-10-29
The next level of possible correlation and comparison between the α7 and 5HT3 receptors is at the subunit arrangement and protein folding. Crystal structures of the nicotinic and serotoninergic pacap receptors [45], [46] reinforced the concept of similarities between these families of receptors. Na
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In an effort to determine
2024-10-29
In an effort to determine if one 5ARI was more effective than the other, the Enlarged Prostate International Comparator Study (EPICS) [17] compared treatment with finasteride and dutasteride in 1630 men over the age of 50 and concluded that after one year of treatment, both groups had statistically
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br Materials and methods br Results br Discussion Prostate c
2024-10-29
Materials and methods Results Discussion Prostate cancer represents an ideal candidate for chemoprevention because of its high incidence and long latency to clinically significant disease [17]. The precancerous lesion PIN may also be a suitable target for ablation in chemoprevention strateg
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Drug resistance development often involves structurally
2024-10-29
Drug resistance development often involves structurally un-related drugs and, specifically both conventional and targeted agents. IGROV-1/Pt1 VX-11e mg are characterized by resistance to cisplatin and reduced sensitivity to inhibitors of EGF-R and MEK, the up-stream activator of ERK1/2, associated
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Autophagy is finalized through the
2024-10-29
Autophagy is finalized through the coordinated positioning and fusion of autophagosomes with lysosomes, during which an array of common and specific membrane traffic-associated proteins is mobilized. Among these proteins, small GTPases, like Rab7, Rab34, or Arl8, and their PRT-060318 australia prot
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ras pathway Previously using a P lacZ
2024-10-29
Previously, using a P-lacZ reporter gene system, it has been shown that the β-galactosidase activity was 9-fold higher in the stationary phase ras pathway when compared with those of the exponential phase [15]. Furthermore, inositol supplementation did not have a major effect on the expression of β
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