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Our overall goal is to develop selective compounds for
2022-06-21

Our overall goal is to develop selective compounds for low-affinity/high-capacity transporters inhibitors (i.e. OCT1–3 and PMAT), and provide the field with much needed, specific pharmacological tools to study these transporters. In our initial efforts, we synthesized halogen substituted analogs and
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In prostate cancer PCa glucose
2022-06-21

In prostate cancer (PCa), glucose metabolism plays a major role in progression [14]. Androgens can activate the metabolic regulator AMP-activated kinase (AMPK), promoting oxidative phosphorylation (OXPHOS) [15]. Besides, androgens increase GLUT1 [16], which overproduction has been described in the m
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This GluR A independent mechanism by which the associative s
2022-06-21

This GluR-A-independent mechanism, by which the associative strength of spatial locations can be increased (and/or decreased) gradually over many trials, and which presumably underlies spatial reference memory acquisition during tasks such as the Morris watermaze or the radial maze (Zamanillo et al.
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In general fish has a limited ability
2022-06-21

In general, fish has a limited ability for digestion and metabolism of carbohydrate though carbohydrate is the cheapest dietary energy and carbon source to animals and the best candidate for replacing dietary protein (Enes et al., 2009, Kamalam et al., 2017, Wilson, 1994). Furthermore, the analysis
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br Acknowledgments br The authors would like to
2022-06-21

Acknowledgments The authors would like to acknowledge the technical assistance of J. Lee. This work was supported by the U.S. National Institute of Health grant HL111206 (to R.A.H.) the Italian Ministry for University and Research (MIUR 2010329EKE). Introduction The liver plays a vital role
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Herein in consider of the high similarity between
2022-06-21

Herein, in consider of the high similarity between GR HBP site and AR HBP site, we applied rational drug design strategy to develop AR/GR antagonists based on the chemical structures of antiandrogens and crystal structure of GR. The following bioassay identified Z19 as a dual AR/GR antagonist. Z19 i
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Considerable evidence links sustained GCG administration to
2022-06-21

Considerable evidence links sustained GCG administration to the reduction of food intake, enhancement of energy expenditure and weight loss in rodent and human studies [16], [17], [18]. Moreover, patients presenting with GCG-producing tumors frequently manifest severe weight loss, through mechanisms
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Cx is a phosphoprotein that is predominantly phosphorylated
2022-06-21

Cx43 is a phosphoprotein that is predominantly phosphorylated in the control state. Cx43 can be phosphorylated by a number of kinases and dephosphorylated by protein phosphatases such as PP1 and PP2A [6], [10]. Posttranslational phosphorylation of Cx43 is thought to influence intercellular coupling
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br Materials and methods br Chemical synthesis br Declaratio
2022-06-21

Materials and methods Chemical synthesis Declaration of interest Acknowledgements This research was supported by a grant from the National Institute for General Medicine to K.W.M. (GM 58448) and by the Department of Anesthesia, Critical Care & Pain Medicine at Massachusetts General Hospi
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Similarly spectrophotometric titrations were carried out und
2022-06-21

Similarly, spectrophotometric titrations were carried out under conditions identical to those used for the fluorescence titrations. exhibited a predominant Phosphatase Inhibitor Cocktail 3 (100X in DMSO) band at around 493 nm. The titrations with all G-quadruplex DNAs resulted in a hypochromic eff
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Methods Very briefly PLA polymeric nanoparticles as
2022-06-21

Methods Very briefly: PLA polymeric nanoparticles as well as liposomes were synthesized and loaded with three different FGFR inhibitors. The encapsulation efficiency, average size, PDI, zeta potential, stability and release kinetics were investigated. The most promising formulations were biological
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Macrocycle was synthesized as described in Under SAr conditi
2022-06-21

Macrocycle was synthesized as described in , . Under SAr conditions, 2-chloronicotinonitrile was heated with -butyl 5-aminopentanoate in refluxing ethanol (). The resulting aminopyridine was treated with mesyl chloride and the nitrile was subsequently reduced to afford amine . Chloroaminopyrimidin
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KDM D also known as JARID D or SMCY is
2022-06-20

KDM5D (also known as JARID1D or SMCY) is encoded on the Y chromosome and until now it has been implicated in prostate cancer invasion and metastasis [42], spermatogenesis [43], and sex-specific tissue transplantation rejection [44]. KDM5D acts as a direct epigenetic modulator, and as one of the four
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br Conclusion The present study provides evidence to suggest
2022-06-20

Conclusion The present study provides evidence to suggest that the ingestion of acetate as a way to augment cellular pools of acetyl-CoA and influence histone acetylation, does not replicate the epigenetic effects of the prebiotic B-GOS®. Furthermore, acetate feeding does not influence olanzapine
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The crystal structures of plant class ADH
2022-06-20

The crystal structures of plant class ADH3/GSNOR from Arabidopsis thaliana (AtGSNOR) and Solanum lycopersicum cv. Amateur (SlGSNOR) with bound substrates and cofactors revealed important differences between plant and human enzyme, namely within the substrate-binding pocket. GSNOR are unusually homod
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