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br Prostaglandins meet Hippo The prostaglandins lie
2022-06-27
Prostaglandins meet Hippo The prostaglandins lie at the crossroads between inflammation, regeneration and tumorigenesis (Figure 3). Prostaglandins are synthesized from archidonic CPI-455 by Cox1 and Cox2 enzymes [40, 41] and in the gut, prostaglandin E2 (PGE2) protects against DSS-induced colitis
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A revolution in cancer immunotherapy has
2022-06-27
A revolution in cancer immunotherapy has recently emerged with the development of novel immunomodulatory antibodies, classified as immunostimulatory agonist monoclonal 2-Deoxyadenosine 5-diphosphate (mAbs) or checkpoint blocking mAbs. CD40/CD40L, as an important costimulatory pathway, mediates a br
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glucose transport proteins br Neurodystrophic effects of HO
2022-06-27
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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Radicicol Cyclopamine a steroidal alkaloid type secondary me
2022-06-27
Cyclopamine, a steroidal alkaloid type secondary metabolite from Veratrum californicum Durand (Melanthiaceae), serves as an anti-Hh constituent blocking the activation of Smo [96,100]. According to previous studies, cyclopamine was shown to inhibit the development of human hepatocellular carcinomas
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Lastly haspin inhibitor was assessed against a panel of kina
2022-06-27
Lastly, haspin inhibitor was assessed against a panel of 292 kinases at 10μM. At this high concentration, the Rosiglitazone inhibited thirteen kinases, in addition to haspin, ⩾90%., These kinases were CaMK2b, CaMK2d, CDK7-CycH-Mat1, cGK2, CK1d, CLK1, CLK2, DYRK1A, DYRK1B, DYRK3, PASK, PIM1 and PK
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Over the last years numerous
2022-06-27
Over the last 15 years, numerous studies gave insights into sGC activation and binding of activators: Photoaffinity labelling studies with cinaciguat suggested the N-terminus of the β1 subunit as target region for this new drug [17]. Schmidt et al. identified the amino acids tyrosine 135, serine 137
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The number of small molecule GSK inhibitors is continuously
2022-06-27
The number of small molecule GSK-3 inhibitors is continuously rising and many have been tested in animals. These studies have provided additional support for specific roles of GSK-3 in neuronal functions under both normal and pathological conditions. Inhibition of GSK-3 has profound effect on neurop
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G protein coupled receptors GPCRs constitute
2022-06-27
G-protein coupled receptors (GPCRs) constitute a large family of 7 trans-membrane-spanning proteins that activate internal signal transduction cascades through binding to different ligands including neurotransmitters, peptides, and lipids [7]. This family of receptors has therapeutic potentials in t
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br Materials and methods br Results br Discussion To
2022-06-27
Materials and methods Results Discussion To understand the molecular basis for how ghrelin secretion is regulated at the cellular level, we identified the full repertoire of 7TM receptors and G proteins in gastric ghrelin 350 and functionally characterized the majority of the receptors whi
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br Introduction br Mitochondrial dysfunction and cancer
2022-06-27
Introduction Mitochondrial dysfunction and cancer Lactate and succinate as oncometabolites Intracellular actions of lactate and succinate as tumor promoters Cell-surface receptors for lactate and succinate and their role in cancer GPR109A as the receptor for butyrate and β-hydroxybu
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Gap junctions mediate electrical coupling
2022-06-24
Gap junctions mediate electrical coupling between cells by conducting direct ionic currents and thereby modulate their electrical activity (Hormuzdi et al., 2004). In the nervous system, electrical coupling organizes network activity by amplifying and synchronizing neuronal firing (Galarreta and Hes
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In summary this study demonstrated the
2022-06-24
In summary, this study demonstrated the cDNA cloning and characterization of the galanin type II receptor (GalR2) and a novel GalR2-like receptor (GalR2-L) in chickens, in which these two receptors are possibly originated from a gene prostaglandin e1 synthesis event that occurred in the early verteb
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This excellent tolerability is especially interesting in the
2022-06-24
This excellent tolerability is especially interesting in the light of the fact that intravenous administration of liposomal ponatinib was predicted to yield much higher plasma concentrations as compared to the orally administered free drug. In addition, liposomal drug dose in absolute numbers was te
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In the current study we report the
2022-06-24
In the current study, we report the properties of P. anserina mutants carrying mutations in a gene encoding the bi-functional enzyme 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase (PFK-2/FBPase-2). This enzyme catalyzes two opposite reactions (Pilkis et al., 1995, Rider et al., 2004): synthesi
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GS-9973 sale By measuring the accumulation of unprenylated
2022-06-24
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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