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It has been reported that the
2022-06-22
It has been reported that the pathway upstream of YAP phosphorylation is operative in a tissue or context-specific manner. LPA or S1P bound to their corresponding membrane GPCRs and act through Rho GTPases to activate YAP/TAZ [11]. Consistently, another report showed that activation of PAR1 (a GPCR)
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Dual H H receptor antagonists developed
2022-06-22
Dual H1/H3 receptor antagonists developed by GlaxoSmithKline have also reached clinical trials at various stages. These candidates are useful for alleviating the symptoms associated with allergic rhinitis(Daley-Yates et al., 2012). GSK-1004723, 4-[(4-chlorophenyl)methyl]-2-( (2R)-1-[4-(4- [3-(hexahy
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br Biochemical properties and post translational modificatio
2022-06-22
Biochemical properties and post-translational modification of GCAPs GCAPs are hydrophobic proteins that are likely permanently bound to their GC target under physiological conditions [5]. They interact with the photoreceptor GCs through the intracellular domains (reviewed in [17]). GCAP1 has been
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Alzheimer s disease AD is a neurodegenerative
2022-06-22
Alzheimer's disease (AD) is a neurodegenerative disorder and characterized by the presence of abnormal filamentous protein inclusions in nerve cells of the brain [2]. The neuropathological hallmarks of AD were first reported by Alois Alzheimer and date back to 1907 [3], [4]. These inclusions are for
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Importantly lactate and H exert
2022-06-22
Importantly, lactate and H+ exert some of their biological effects independently of each other, though sometimes through redundant pathways leading to a same biological effect, as for angiogenesis. In other cases, they can have antagonist effects: lactate was shown to stimulate extracellular matrix
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Based on the results of compound appeared to have the
2022-06-21
Based on the results of , Ergosterol appeared to have the best overall profile, so our efforts were then devoted to using 5-(-propyl)pyrimidine as the right-hand nitrogen attachment to optimize the R group of (). Analog was synthesized using the reaction conditions from , while analogs and were synt
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GPR is present primarily in the
2022-06-21
GPR119 is present primarily in the pancreas and the intestine. Activation of GPR119 increases insulin, GLP-1, GIP and PYY secretion. GPR119 agonists stimulate insulin release in a glucose-dependent manner. The glucose dependent insulin secretion (GIDS) mechanism makes GPR119 an attractive target for
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br Funding M I is
2022-06-21
Funding M.I. is supported by European Research Council (ERC) Consolidator Grant 725038, Italian Association for Cancer Research (AIRC) Grant 19891, Italian Ministry of Health (MoH) Grant GR-2011-02347925, Lombardy Foundation for Biomedical Research (FRRB) Grant 2015-0010, the European Molecular B
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br Investigations br Genetics GLUT is a membrane
2022-06-21
Investigations Genetics GLUT1 is a membrane-bound glycoprotein that provides base-rate glucose transport across blood-tissue barriers. It is constituitively expressed in erythrocytes, GW-1100 receptor microvessels and astroglia. The gene exclusively associated with GLUT1 is SLC2A1, located on
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In order to elucidate the
2022-06-21
In order to elucidate the reasons of high efficacy of , we evaluated the BOC group itself and the linkage between the BOC group and the benzene ring of A-part. Urea moiety (), the replacement of an oxygen diltiazem hydrochloride of the BOC group to a nitrogen atom, decreased the activity (EC = 0.12
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A number of models have been
2022-06-21
A number of models have been proposed in order to explain the mechanisms of protein transport through nuclear pore complexes. One theory is that the transport is mediated by specific peptide signals known as NLSs. The classical NLSs are short sequences containing a high proportion of the positively
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br Contributions br Acknowledgements This research was
2022-06-21
Contributions Acknowledgements This research was supported by Natural Sciences and Engineering Research Council (NSERC) Discovery grant No. 341538 and Ontario Graduate Scholarships to HM and VS. Introduction Sexual size dimorphism describes size difference between male and female individua
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br Conflict of interest statement br Introduction br Gap jun
2022-06-21
Conflict of interest statement Introduction Gap junction assembly Induced disassembly of gap junctions The regulation of connexin and gap junction turnover are still not well understood. This is, in part, due to the fact that while the overall turnover of connexin molecules is fairly con
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Most of the above mechanisms
2022-06-21
Most of the above mechanisms are implicated in attenuation of myocardial I/R injury. However, the role of GalR2 receptor activation in cardioprotection remains unclear because of the lack of receptor subtype selectivity of peptides G2 and G3. It has been shown that Ala5-galanin (2–11) (G4) has a hig
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In soft agar colony formation assay transformed cells
2022-06-21
In soft agar colony formation assay, transformed brdu indicate anchorage-independent growth and colony formation without attachment on the bottom of cell culture plate. This assay can investigate transformation and tumorigenic activities [24]. Our recent study showed that the long-term 5-FU treatmen
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