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Activity of compound in rat brain tissue highlights
2021-09-30
Activity of compound 10 in rat Wang Resin mg tissue highlights the potential to use this new class of allosteric sGC inhibitors to study the role of the NO—sGC—cGMP signalling pathway in the brain. Reducing amounts of cGMP in cells would have implications in downstream signalling proteins, such as
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GPR co localizes with ghrelin in the duodenum gustducin in
2021-09-30
GPR120 co-localizes with ghrelin in the duodenum [17], α-gustducin in the small intestine and type II taste bud cells 18, 19, neuropeptide Y centrally in the arcuate nucleus [20] and glucagon-like peptide 1 (GLP-1) in the colon and circumvallate papillae taste bud cells 6, 21, 22. Interestingly GPR1
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br Membrane transporters as a novel therapeutic
2021-09-30
Membrane transporters as a novel therapeutic target in pediatric TBI The concept of targeting membrane transporters began with identifying a neuroprotective drug and a corresponding transporter inhibitor. Somewhat serendipitously, we discovered that N-acetylcysteine (NAC), a cysteine donor for GS
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In conclusion starting from the weakly potent GSM exploratio
2021-09-30
In conclusion, starting from the weakly potent GSM , exploration of various spacer groups between the triazole ring and the aromatic Methyllycaconitine citrate led to the discovery of a new series of potent gamma secretase modulators, with an improved drug-like profile—compared with the originally
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Interestingly GAL has also been shown
2021-09-30
Interestingly, GAL has also been shown to be co-expressed and/or secreted in luteinizing hormone releasing hormone (LHRH) (Merchenthaler et al., 1991, Marks et al., 1994) and kisspeptin (KISS) neurons (Porteous et al., 2011). Furthermore, GAL was shown to stimulate luteinizing hormone (LH) secretion
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G quadruplex structures can be resolved by helicases Consist
2021-09-30
G-quadruplex structures can be resolved by helicases. Consistently, many helicases are aberrantly expressed in cancer TH588 synthesis [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 discovere
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Cy5 EGFP mRNA br Conclusions br Conflicts of interest
2021-09-29
Conclusions Conflicts of interest Funding The research work was partially supported by National Science Center (Contract Grant Number: UMO-2015/19/B/NZ1/00332). Introduction Frusectose-1, 6-bisphosphatase (FBPase) has long been recognized as a potential therapeutic target for the treatm
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By measuring the accumulation of unprenylated Rap
2021-09-29
By measuring the accumulation of unprenylated Rap1a as a surrogate marker for the inhibition of FPPS [8], [9], [10], [11], we found that upregulation of FPPS expression in Hela cells reduced the accumulation of unprenylated Rap1a in response to 24h' treatment with 0–50μM ZOL. As expected, cells cult
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Compounds that induce exocytosis in cultured cells include C
2021-09-29
Compounds that induce exocytosis in cultured AM251 include Ca2+-dependent [14] or Ca2+-independent [15] mechanisms. Ca2+-dependent exocytosis releases soluble enzyme content from lysosomes [16] operating by increasing the cytosolic concentration of Ca2+[13] by recruiting extracellular Ca2+[14], lib
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In order to establish proper folding and enzymatic activity
2021-09-29
In order to establish proper folding and enzymatic activity, G9a and GLP methyltransferases each contain four structural zinc ions. Both Enzalutamide contain two distinguishable types of zinc fingers; three Zn(II) ions are chelated in a triangular cluster by 9 cysteines (b, top left), whereas one Zn
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br Discussion The aim of the present study was
2021-09-29
Discussion The aim of the present study was to extend the list of ASIC ligands and to check if histamine receptors ligands can also affect ASICs. The novel finding is that not only histamine but also thioperamide, 1-metylhistamine and Nα-methylhistamine are active ASIC1a potentiators, while other
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Azaperone Wolf et al then proceed to interrogate the mechani
2021-09-29
Wolf et al. (2016) then proceed to interrogate the mechanism by which NAG activates the NLRP3 inflammasome. When examining potential triggers previously implicated in NLRP3 activation, they found that both PGN and NAG trigger appearance of mitochondrial DNA (mtDNA) in the cytosol, which led them to
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br Neurodystrophic effects of HO It is well
2021-09-29
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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br Discussion By using ultra deep sequencing
2021-09-29
Discussion By using ultra-deep sequencing, we conducted a thorough assessment of HCV-NS3 protease variants in chronic PI-naïve patients infected with HCV-1a and HCV-1b under telaprevir-based triple therapy at baseline and after 4weeks of treatment. Several synonymous and non-synonymous substituti
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Cysteine Cys residues are frequently
2021-09-29
Cysteine (Cys) residues are frequently found to be highly conserved within functional, regulatory, catalytic, or binding sites of proteins. Thiol or thiolate chemistry imparts active sites with unique properties like nucleophilicity, high affinity metal binding, and disulfide bond assisted multimeri
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