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br Rho family GTPases are
2021-09-10

Rho-family GTPases are molecular switches; most which cycle from an ‘on’ GTP bound state to an ‘off’ GDP bound state, driven by GEFs (guanine nucleotide exchange factors) and GAPs (GTPase-activating proteins) respectively. Association with lipid membranes through a lipid (farnesyl or geranylgerany
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Among prostaglandins PG PGD remained the most elusive specie
2021-09-10

Among prostaglandins (PG), PGD2 remained the most elusive species for a long time and was initially regarded as having negligible biological activity [1]. In 1974 its inhibitory effect on platelet aggregation was discovered by Smith et al. [2] and Mills & McFarlain [3], and both pressor and depresso
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Treatment with probiotics can also
2021-09-10

Treatment with probiotics can also be used to alter the microbiota profile of CF patients. One study reports that administration of the probiotic Lactobacillus Reuteri improved digestive health and inflammation [112]. The fecal microbial profile changed, showing a decrease in Proteobacteria and an i
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We also explored various nitrogen substituents with
2021-09-10

We also explored various nitrogen substituents with an aim toward modulating sterics and basicity within the ABH series. No glycine uptake inhibition was detected with non-basic bicycles (data not shown). Isopropyl was the best compromise between desired on-target effect and clearance, however, eff
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AFB Fapy dG has been long recognized as
2021-09-10

AFB1-Fapy-dG has been long recognized as a substrate for nucleotide excision repair [24,25]. However, we recently demonstrated that this lesion is removed by Gastrodin excision repair. We showed that DNA glycosylase NEIL1, a member of the Fpg/Nei glycosylase family, could excise AFB1-Fapy-dG from si
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The occurrence of MDR in cancer patients
2021-09-10

The occurrence of MDR in cancer patients undergoing chemotherapy can be mimicked in the laboratory by culturing cancer Neratinib in the presence of chemotherapeutic drugs, thereby enforcing the evolution of acquired drug resistance. This has been described in multiple model systems including the rh
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Structural analysis of the MD open state unveils
2021-09-09

Structural analysis of the MD-open state unveils that the transmembrane domain features a symmetric organization of the pore-lining helices M2 similar to the semi-open structure but with a local asymmetry at the constriction point, which is critical for chloride permeation. The atomistic simulations
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Since the isoflavone emerged as privileged scaffold in Hh
2021-09-09

Since the isoflavone emerged as privileged scaffold in Hh inhibition, based on molecular modeling predictions and prior studies [17,22], here we designed a number of isoflavones able to interact preferentially with the Smo receptor or the Gli protein. Molecules were synthesized by means of a novel s
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pi3k akt pathway It is possible that regulation
2021-09-09

It is possible that regulation of adiposity and glucose homeostasis by GIP are in part mediated by altering leptin levels and/or leptin signaling. However, we are unaware of reports that support this mechanism of action of GIP. In addition, leptin levels in GIP receptor knockout mice [12], [52] and
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Lonidamine In this study we saw change
2021-09-09

In this study, we saw change in GHS-R1a mRNA expression in fasting condition. It is noteworthy that changes in ghrelin and GHS-R1a mRNA expression synchronized in organs were examined. In the Lonidamine and pituitary, gene expression increased 4days after fasting, and the increased level declined u
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Based on the collective experience to date
2021-09-09

Based on the collective experience to date, it is likely that a much more comprehensive assessment of GSI selectivity for inhibition of multiple substrates, as well as biomarkers to track inhibition of non-APP substrates in vivo will be needed to support future efforts to develop substrate selective
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Microglia after activation can show prominently pro
2021-09-09

Microglia after activation can show prominently pro-inflammatory but also anti-inflammatory characteristics [46]. Although the ageing process is not a pathological process, many of the age-associated changes resemble those observed under pathological conditions. An increase number of pro-inflammator
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Myelination by oligodendrocytes is required for saltatory ne
2021-09-09

Myelination by oligodendrocytes is required for saltatory nerve impulse conduction and proper CNS function (Bercury and Macklin, 2015). Defects in myelination and remyelination impair saltatory nerve conduction and functional connectivity leading to cognitive, behavioral, and motor deficits in neuro
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br HO regulation and physiology The catabolism of cellular
2021-09-09

HO-1: regulation and physiology The catabolism of cellular heme in humans and other species is mediated by the heme oxygenase (HO) family of enzymes (E.C. 1:14:99:3; heme-hydrogen donor:oxygen oxidoreductase). The HOs localize primarily to the endoplasmic reticulum (ER) where they serve, in conce
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br Mechanism of HH pathway activation in NSCLC Despite the
2021-09-09

Mechanism of HH pathway activation in NSCLC Despite the role of the HH pathway in basal cell carcinoma and medulloblastoma, it has been postulated that epithelial tumors do not demonstrate cell autonomous HH ligand activity. The main evidence comes from the study by Yauch et al showing no correla
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