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The finding of histamine action
2021-11-08
The finding of histamine action on ASICs also raises the question about possible action of other histamine receptor ligands. In the present work we selected several compounds and performed electrophysiological testing of their action on recombinant homomeric ASIC1a and ASIC2a. Nα-methylhistamine is
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br Although there are growing bodies of
2021-11-08
Although there are growing bodies of research dealing with diverse non-imidazole based compounds, they are not free from obstacles in their development pipeline and hence the design of these compounds is complicated by various factors briefly discussed below. One of the problems in designing H3R a
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DIDS The overall characteristic of RNA
2021-11-08
The overall characteristic of RNA profile of Leydig cell is still a mystery. Variation in total RNA will cause subsequent difference in protein expression and phenotypic modulation [16]. In this study, we used a murine nicotine exposure model coupled with next generation RNA sequencing (NGS) and fou
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Miconazole br METHODS br RESULTS br Discussion Numerous stud
2021-11-06
METHODS RESULTS Discussion Numerous studies have proposed various hypotheses and models to explain how neuroinflammation could contribute to the chronic fatigue, postexertional fatigue, and cognitive deficits observed in patients with ME/CFS.12, 13, 14, 15 Although neuroimaging studies have
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br Materials and methods br Results
2021-11-06
Materials and methods Results Discussion According to the literature, zaprinast is a high-affinity agonist of GPR35 (Berlinguer-Palmini et al., 2013, Divorty et al., 2015, Taniguchi et al., 2006, Zhao et al., 2010). GPR35 Nifedipine has been identified within discrete regions of the nervou
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Both GPR A and GPR
2021-11-06
Both GPR109A and GPR81 are located on chromosome 12q24 [3] and mediate anti-lipolytic effects through coupling to Gi-type G proteins [17]. It is important to note that with the recent deorphanization of these receptors, there has been a recommendation to the International Union of Basic and Clinical
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The discovery that GLUT in the microvasculature represents
2021-11-06
The discovery that GLUT1 in the microvasculature represents an important target of VEGF thereby affecting ISO-1 function is highly relevant. The work of Jais et al. identified VEGF as a determining player in the regulation of cognitive performance and provides an important link to the unfavorable e
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G quadruplex structures can be resolved
2021-11-06
G-quadruplex structures can be resolved by helicases. Consistently, many helicases are aberrantly expressed in cancer Butyrolactone 3 australia [47]. In this study, we correlated HOXC10 expression with that of all helicases using a microarray dataset derived from 759 breast cancer patients [36] and
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Considering together the conformational docking
2021-11-06
Considering together the conformational, docking and SAR results of this and of previously published papers, a three points pharmacophore model can be developed considering the indispensable residues of SRSRY derived antagonists, namely Arg89, Arg91 and Tyr92. This model is shown in Fig. 10, and req
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br Clinical assessment of iron chelation br Towards
2021-11-06
Clinical assessment of iron chelation Towards the new concept of conservative iron chelation: iron scavenging and redeployment For any chelator to be of clinical value in disorders of regional siderosis they ought to be endowed with a requisite accessibility to the relevant sites and different
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br Other strategies for ferroptosis In addition to ROS
2021-11-06
Other strategies for ferroptosis In addition to ROS-generating and GPX4 inactivating nanomaterials, small molecules and genetic manipulation targeting key factors in the ferroptosis pathway have also been tested for their anticancer effects [39,47,48]. Among a myriad of proteins involved in ferro
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br Acknowledgments I thank Takeshi Sakaba for critical readi
2021-11-06
Acknowledgments I thank Takeshi Sakaba for critical reading of the manuscript and helpful comments. This work was supported by JSPS/MEXT KAKENHI Grant Numbers 17K19466, 17H03548. Introduction The oral route of drug application is the main route in pharmacology since it is easy to handle and o
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Importantly the regulation of the Hippo pathway
2021-11-06
Importantly, the regulation of the Hippo pathway by metabolic networks, such as by glycolysis39, 40, hexosamine biosynthesis41, 42, and mevalonate synthesis43, 44, as well as by nutrient-sensing pathways including AMP-activated protein kinase (AMPK) 40, 45, 46 and mTOR 47, 48, 49, 50, was recently d
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br Methods br Results br
2021-11-05
Methods Results Discussion Peptide therapeutics represents a unique class of biopharmaceuticals that continues to evolve in drug discovery and development. We and others have been particularly interested in bioengineering innovative pGC-A and/or pGC-B peptide activators. This has been succ
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br S NO signalling during the plant immune
2021-11-05
(S)NO signalling during the plant immune response Redox signalling molecules must exhibit specificity for their target substrate. Moreover, a given redox-based modification must be reversible to ensure transient signalling. Oxidative cysteine (Cys) modifications are integral to a variety of redox
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