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Transporters are important ta http www apexbt
2022-02-26
Transporters are important targets for devising new therapies, optimizing existing therapies, and helping understand the toxicities of certain drugs. Given the well-documented role of transporters in restricting the distribution of drugs, modulating the relevant transporters could enhance the permea
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br Biologically active non peptide galanin receptor ligands
2022-02-26
Biologically active non-peptide galanin receptor ligands The first successful attempt in overcoming these weaknesses was undertaken by Saar et al. (2002). Screening of galanin sequence established that Trp-2, Asn-5, Tyr-9 were pharmacophores, responsible for biochemical action of the peptide. Bas
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br The interrelationship between obesity and galanin Numerou
2022-02-26
The interrelationship between obesity and galanin Numerous studies revealed that obesity and galanin may promote each other. On the one hand, galanin may increase the possibility of obesity of subjects via boosting their appetite and food intake. Acute injection with galanin or its agonist, galan
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Sumoylation is involved in regulating protein protein
2022-02-26
Sumoylation is involved in regulating protein-protein interactions, subcellular protein localization, protein stability, and transcriptional factor activity (reviewed in [29]). The small ubiquitin-like modifier (SUMO) protein is covalently attached to a lysine residue in a Ψ-K-X-D/E consensus sequen
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Our biological data also showed that in presence of
2022-02-26
Our biological data also showed that, in presence of LEDGF/p75, R or S of glycerol T instead of T4, T8 or T12 loop in the T30695-GQ differently affected the integration activity of the enzyme (Table 2), whereas the position but not the chirality of glycerol T affected the inhibitory efficiency of T3
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NeuroHIV is initiated by HIV crossing the blood brain
2022-02-26
NeuroHIV is initiated by HIV crossing the blood–brain barrier (BBB) to enter the CNS. This is thought to occur primarily via the transmigration of infected CD14+CD16+ monocytes (Williams, 2014), using the monocytes as “Trojan Horses” (Peluso, 1985), although some studies suggest alternate routes of
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A phase I clinical trial has
2022-02-26
A phase I clinical trial has been completed for assessing CEP-26401 in cognitive impairment in healthy individuals without disclosing any results (NCT01903824). Although CEP-26401 is under clinical trial study, several projects are in progress for synthesizing novel irdabisant analogs in order to im
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br Statistical analysis The mean standard deviation median
2022-02-25
Statistical analysis The mean, standard deviation, median, range, frequency, and percentage were used for data description. The chi-square (x2) test was used for analyses the differences in categorical variables in the 2-way table. Overall survival (OS) was defined as the time interval between t
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In this new therapeutic era
2022-02-25
In this new therapeutic era, nucleic Bilirubin receptor amplification tests (NAATs) remain critically useful. NAATs are recommended to detect HCV RNA in blood following initial serologic diagnosis of HCV infection, to distinguish between spontaneous resolution and progression to chronic infection [7
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Lomerizine HCl In contrast to sGC stimulators sGC activators
2022-02-25
In contrast to sGC stimulators, sGC activators promote enzymatic activity of sGC containing oxidized heme iron (Fe3+) or missing the heme group. A-350619 is one of the oldest activators of sGC to be discovered. A-350619 increased sGC activation in a non-additive manner with respect to YC-1, leading
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Our observations with RBC in human platelets suggested a
2022-02-25
Our observations with RBC8 in human platelets suggested a more wide-ranging role for Rals in platelet function compared to our observations in Ral deficient mouse platelets. Using lumi-aggregometry, 10 μM RBC8 significantly reduced platelet aggregation and ATP secretion responses in both WT and DKO
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Emodepside br Conclusions br Acknowledgement br Introduction
2022-02-25
Conclusions Acknowledgement Introduction The macrophage is an important cell species that plays key roles in innate immune responses and inflammatory reactions through phagocytosis of foreign bodies and secretion of inflammatory mediators such as interleukin (IL)-1, tumor necrosis factor (T
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As part of our discovery efforts searching
2022-02-25
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 fragme
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In addition analysis of the functional elements in the
2022-02-25
In addition, analysis of the functional elements in the GnRH promoter region also identified other transcription factor binding sites, such as those for GATA-1 and Oct-1. However, those sites were not further validated in this study. Nevertheless, it has been reported that transcription factors such
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Cichlasoma dimerus as most teleost fish species present neur
2022-02-25
Cichlasoma dimerus, as most teleost fish species, present neurons expressing GnRH3 (Pandolfi et al., 2005). As in most MG-132 species, the neurons expressing GnRH3 are mainly located in the NOR, although few neurons were detected in the olfactory bulb, ventral telencephalon and the POA (González-Ma
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