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In vitro studies have described the kinetic parameters
2022-01-03
In vitro studies have described the kinetic parameters of the KDM4A catalytic site (cKDM4A) (Figure 1C) (23); the kcat/KM (kcat as the catalytic constant and KM as the Michaelis constant) values represent how fast the enzyme reacts with the substrate once it encounters the substrate, where the value
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TRAPP Transport Protein Particle complexes share
2021-12-31
TRAPP (Transport Protein Particle) complexes share a common core architecture and function in sirtuin 1 and autophagy (Kim et al., 2016). In yeast, the core complex has GEF activity for the Rab1 ortholog Ypt1. The larger TRAPPII and III complexes include regulatory subunits implicated in membrane r
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We have previously established the pharmacokinetic profile a
2021-12-31
We have previously established the pharmacokinetic profile and effective dose of MNF in the rat [43] and demonstrated the effectiveness of MNF as an anticancer drug in AR-A014418 and xenograft models [44]. Moreover, MNF was found to effectively block GPR55 signaling in tumor cells [21]. The compound
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Recently a receptor for nicotinic acid
2021-12-31
Recently, a receptor for nicotinic acid, named GPR109A (also known as HM74a in man or PUMA-G in the mouse) has been identified (Lorenzen et al., 2001, Lorenzen et al., 2002, Soga et al., 2003, Tunaru et al., 2003, Wise et al., 2003). This receptor, a member of the 7 transmembrane G-protein coupled f
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Yes mutations have been linked
2021-12-31
Yes, mutations have been linked to two main types of disorder in humans. Several autosomal dominant mutations, some of which have been characterized and lead to increased PIEZO1 signaling, are associated with dehydrated hereditary stomatocytosis (DHS). DHS is characterized by osmotically-driven dehy
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More recently NMR techniques have
2021-12-31
More recently, NMR techniques have been used to monitor K+ () fluxes in isolated rat hearts. These reveal an increased rate of passive efflux of from Langendorff-perfused hearts at 20°C compared to 36°C or 10°C (Gruwel, Kuzio, Xiang, Deslauriers, & Kupriyanov, 1998). Similar experiments assessed th
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Some clinical reports have suggested that galanin has
2021-12-30
Some clinical reports have suggested that galanin has a role in the neurobiology of mood disorders [[6], [7], [8], [9], [10]]. In behavioral studies, contradictory results have been reported [11,12]. For example, systemic administration of non-selective galanin receptor agonists, such as galmic [13]
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Some previous findings indicate that GALP has
2021-12-30
Some previous findings indicate that GALP has an influence on AVP and OT secretion from the posterior pituitary gland. Cunningham et al. (2004) noted that the expression of GALP mRNA was increased in the neurohypophysis of lactating rats compared to non-lactating rats, whereas GALP mRNA expression i
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Of the cases identified herein three known and novel FGFR
2021-12-30
Of the 52 cases identified herein, three known and 11 novel FGFR fusion partners were identified. Notably, an oligomerization domain, including coiled-coil dimerization domains similar to that seen in echinoderm microtubule associated protein like 4 gene (EML4), which is the most common ALK partner
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The IN gene of the HIV isolate from
2021-12-30
The IN gene of the HIV isolate from Papua (CRF01_AE isolate) contains genetic polymorphisms (Fig. 1A) that encode for variant amino acids in the IN protein, based on the Stanford HIVdb mutation interpretation database (Fig. 1B). These variations slightly changed the three-dimensional structure of IN
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br Histamine H R The cloning of the
2021-12-30
Histamine H4R The cloning of the H3R (Lovenberg et al., 1999) provided a template for the search of other Vincristine receptors, and resulted in the most recent discovery of histamine H4R. This concluded with six independent groups that have reported the cloning of the H4R (Leurs et al., 2009, Li
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br Hedgehog pathway in embryonic development It
2021-12-30
Hedgehog pathway in embryonic development It is now well established that the Hedgehog pathway solves a role as one of the essential signaling mechanisms for the modulation of cellular growth and differentiation during embryogenesis. Operating through time- and position-dependent mechanisms, this
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br Methods br Results and discussion br Conclusions In
2021-12-30
Methods Results and discussion Conclusions In this work, 100-ns MDSs were applied on the WT and on the R155K and D168A single point mutations of the NS3/4A protease in the apo form and in complex with ASV, a current drug in phase III clinical trials. According to the PCA, these two mutation
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Introduction Inorganic arsenic InAs species such as arsenite
2021-12-30
Introduction Inorganic arsenic (InAs) species such as arsenite (AsIII) and arsenate (AsV) are present in groundwater. Arsenic contaminated drinking water is a global public health issue because of its natural prevalence and toxicity. Long exposure to arsenic results in chronic effect in humans, inc
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br Acknowledgements br Introduction Type diabetes is
2021-12-30
Acknowledgements Introduction Type 2 diabetes is a progressive metabolic disorder which is characterised by chronic hyperglycaemia due to relative insulin deficiency, insulin resistance and increased hepatic glucose production [1]. The metabolism of glucose by glycolysis increases the ATP:ADP
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