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A pooled overall survival analysis at year showed no differe
2022-09-16

A pooled overall survival analysis at 1year showed no difference in survival between the two study arms, although these studies were not designed or powered to demonstrate a survival benefit. Among the 979 total patients in both ROMANA 1 and 2, about 55% continued on to the ROMANA 3 trial. That tria
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Many natural flavonoids have been identified as influencing
2022-09-15

Many natural flavonoids have been identified as influencing ionotropic GABA receptors through bioassay-guided fractionation of plant extracts (Fig. 4). HPLC-based activity profiling of extracts the traditional Chinese herbal drug Kushen (Sophora flavescens root) led to the identification of the 8-la
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The schematic diagram of the antagonistic interactions of Zn
2022-09-15

The schematic diagram of the antagonistic interactions of Zn2+ and neurosteroids (NSs) at GABA-A receptors is summarized in Fig. 7. Neurosteroids exhibit powerful seizure protective effects against experimental seizures probably through the potentiation of synaptic and extrasynaptic GABA-A receptor-
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Similarly spectrophotometric titrations were carried out
2022-09-15

Similarly, spectrophotometric titrations were carried out under conditions identical to those used for the fluorescence titrations. exhibited a predominant proton pump inhibitor band at around 493 nm. The titrations with all G-quadruplex DNAs resulted in a hypochromic effect along with a bathochromi
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VS strategies have been building momentum in G drug
2022-09-15

VS strategies have been building momentum in G4 drug discovery both as a low-cost enrichment step and as a lead development step in the discovery pipeline, which our laboratory has previously discussed [31]. Whereas traditional HTS methods rely on obtaining and screening hundreds or thousands of com
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Consistently with the above discoveries it has
2022-09-15

Consistently with the above discoveries, it has been also shown that in cardiomyocytes with shRNA-down-regulated FBP2, mitochondria are more susceptible to depolarisation (Gizak et al., 2012a) and H2O2-induced oxidative stress (Wiśniewski et al., 2017). In R547 overexpressing FBP2 (cardiomyocytes a
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br Methods and materials br
2022-09-15

Methods and materials Results Discussion In this study we demonstrate that CF epithelial Dorsomorphin exhibit features of apoptosis in their basal, unstimulated state including increased caspase (-3 and -8) activation compared to non-CF epithelial cells. Analysis of factors responsible for
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Combination inhibitors of FAAH TRPV and or COX
2022-09-15

Combination inhibitors of FAAH, TRPV1, and/or COX2 may have the advantage of effective pain relief with a high therapeutic index. For example, arachidonoyl serotonin (AA-5-HT) inhibits both FAAH (IC=1–12μM) and TRPV1 (IC=37–270nM against 100nM capsaicin in HEK-293 cells)., In mice, AA-5-HT had grea
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CDX is also a tumor
2022-09-15

CDX1 is also a tumor suppressor gene; the ablation of CDX1 and CDX2 results in a significant increase in tumor formation in the colon. CDX1 is regulated by epigenetic modification; the hypermethylation of the CpG island at the promoter is positively associated with severe clinical phenotypes. In add
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Introduction Histamine Imidazolyl ethylamine is an important
2022-09-15

Introduction Histamine [2-(4-Imidazolyl)-ethylamine] is an important mediator of many physiological and pathological processes including inflammation, gastric QNZ secretion, neuromodulation, regulation of immune function, cell proliferation and differentiation, among others. Histamine exerts its bi
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br Neurodystrophic effects of HO It is well
2022-09-15

Neurodystrophic effects of HO-1 It is well known that neonatal hyperbilirubinemia (jaundice) may lead to irreversible neurological injury in children (kernicterus). This outcome can be prevented by photodegradation of circulating bilirubin or treatment with metalloporphyrin inhibitors of HO enzym
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cb 839 receptor Over the last years numerous
2022-09-13

Over the last 15 years, numerous studies gave insights into sGC activation and binding of activators: Photoaffinity labelling studies with cinaciguat suggested the N-terminus of the β1 subunit as target region for this new drug [17]. Schmidt et al. identified the amino acids tyrosine 135, serine 137
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We found few differential effects on lung
2022-09-09

We found few differential effects on lung function for exposure to mother’s and father’s smoking in relation to GSTM1 and GSTT1. However, effects related to mother’s or father’s smoking may differ because mothers tend to spend greater amounts of time with young children and mothers may also smoke du
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As part of our discovery efforts searching for small molecul
2022-09-09

As part of our discovery efforts searching for small molecule GPR119 agonists, we analyzed active pharmacophores of known agonists from the literature, and found that -methylsulfonylphenyl and substituted 4-hydroxyl piperidine are common fragments. In our initial efforts, we linked these two fragmen
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We tested this hypothesis with two experiments
2022-09-09

We tested this hypothesis with two experiments. In the first experiment OVX monkeys implanted with an E2 Raltitrexed (this results in LH levels similar to the level during the follicular phase) were treated with daily injections of letrozole for 1 week and then EB was injected systemically mimickin
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