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The physiologic conditions and signaling mechanisms that reg
2023-02-13

The physiologic conditions and signaling mechanisms that regulate apelin secretion and APLNR expression in malignant tissues appear to be multifactorial. Previous studies have shown that hyperplastic and neoplastic cholangiocytes secrete a variety of hormones, peptides, and growth factors that help
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br Model Fig demonstrates the block scheme of
2023-02-13

Model Fig. 1 demonstrates the block-scheme of main interactions between variables of the model under investigation. These interactions are described below in details and are expressed in mathematical form as well, where all variables are the functions of space and time coordinates, r and t, which
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A phase I trial has recently evaluated enzalutamide
2023-02-13

A phase I trial has recently evaluated enzalutamide, an anti-androgen agent, in patients with ER- and AR-positive advanced BC to estimate safety and tolerability of enzalutamide therapy alone or in association to anastrozole, exemestane or fulvestrant [65]. The results of major clinical trials with
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A number of studies indicate the
2023-02-13

A number of studies indicate the involvement of the classical AR or a splice variant that translocate to the membrane, via a palmitoylation mechanism, similar to ERα (Acconcia et al., 2005, Acconcia et al., 2004, Acconcia et al., 2003), since AR equally contains the required nine amino Phenytoin sod
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In this study for the first instant we report
2023-02-13

In this study, for the first instant we report the characterization, production and in silico structural analysis of BADH1 gene in B. haloduranss SMBPL06 isolated from the salt pan. Moreover, the sequence analysis of betaine aldehyde dehydrogenase from B. haloduranss SMBPL06 displayed several base s
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Unexpectedly under pathological pain conditions
2023-02-13

Unexpectedly, under pathological pain conditions, inhibition of spinal glutamate transporter activity can produce antinociceptive effects. For example, intrathecal injection of the transportable inhibitor trans-pyrrolidine-2,4-dicarboxylic 5 alpha reductase inhibitor (t-PDC) or antisense oligonucle
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During the course of our ACK inhibitor program a high
2023-02-13

During the course of our ACK1 inhibitor program, a high-throughput screening (HTS) campaign of our internal sample collection was conducted. A series of -aryl pyrimidine-5-carboxamides of the general structure () was identified. Earlier studies of the structure–activity relationship (SAR) of ident
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AMN-107 HT receptors are distributed throughout the brain wi
2023-02-13

5-HT3 receptors are distributed throughout the brain, within the brainstem (e.g., nucleus tractus solitarius, area postrema and spinal trigeminal nucleus) and AMN-107 (e.g., hippocampus, amygdala, nucleus accumbens, putamen and caudate) (Abi-Dargham et al., 1993, Barnes et al., 1989, Bufton et al.,
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NP118809 exemplifies three of the compounds
2023-02-10

exemplifies three of the compounds investigated in the selection for a candidate drug (CD). Our first criteria was an IC NP118809 as such did not show any genotoxicity in the SOS/umu assay, but this does not say anything about any possible genotoxicity of its metabolites or degradation products. A
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Human lipoxygenase exists in two forms named
2023-02-10

Human 15-lipoxygenase exists in two forms, named 15-LOX-1 (also named 12/15-LOX, 15-LO-1) and 15-LOX-2. Several reports indicate that 15-LOX-1 has a pathophysiological role in respiratory inflammatory diseases, in particular asthma. Increased activity of 15-LOX-1 is displayed in the respiratory trac
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Plant defensins Vriens et al and linear AMPs
2023-02-10

Plant defensins (Vriens et al., 2014) and linear AMPs (Domingues et al., 2015, Liu et al., 2008) have been shown to present several modes of action. Among these different mechanisms, permeabilization of the fungal membrane has been described as a secondary effect of plant defensin action (Vriens et
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The reasons why antibiotic treatment may be detrimental are
2023-02-10

The reasons why antibiotic treatment may be detrimental are diverse. First, it may result in disruption of multifaceted microbe–microbe, as well as microbe–host, interactions that are key for the maintenance of homeostasis within this ecosystem. This can lead to the expansion of pathogenic microorga
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phenanthroline br cDNA cloning gene structure and chromosoma
2023-02-09

cDNA cloning, gene structure and chromosomal localization The cDNA for the leukocyte-type 12S-lipoxygenase was first cloned from porcine leukocytes [9], and later from mouse [10], [11], rat [12], [13], bovine [14] and rabbit [15] sources. The cDNA for the platelet-type 12S-lipoxygenase cDNA has b
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CTX0294885 For patients who have taken
2023-02-09

For patients who have taken advantage of the anti-TKIs and whose follow-up has been succeeded, some partial response has been noticed with 45% (9/20) for gefitinib, 39% (9/23) for erlotinib and 56.5% (13/23) for crizotinib. A disease progression has also been observed with 35% (7/20) for gefitinib,
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In the late s Solvay Pharmaceuticals discontinued the
2023-02-08

In the late ‘90s, Solvay Pharmaceuticals discontinued the Phase 2 development of a promising potent and highly selective A1AR antagonist based on the pyrrolopyrimidine scaffold, SLV320 [43] (2, Chart 1, also named derenofylline; Ki hA1AR = 1 nM), for the treatment of acute heart failure [24]. In the
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