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br Reaction mechanism The dissimilarity between monofunction
2021-09-16
Reaction mechanism The dissimilarity between monofunctional and bifunctional glycosylases is that the monofunctional glycosylases removes the substrate base, leaving an intact AP site while the bifunctional glycosylases have an additional lyase activity. This intrinsic lyase activity is present i
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The amino hydroxy methyl isoxazolepropionic acid AMPA
2021-09-16
The α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic kras-pdeδ inhibitor (AMPA) receptors are related ionotropic glutamate receptors (iGluRs) that mediate fast excitatory neurotransmission, and are also typically heteromeric ion channels, composed of GluA2 subunits in conjugation with GluA1, GluA3,
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br Endogenous lipids as SLC transporter modulators
2021-09-16
Endogenous lipids as SLC6 transporter modulators Lipids constitute part of the environment in which membrane-embedded transporters operate [62]. Endogenous lipids can act as inhibitory ligands [63] or functionally important components of the membrane that impart changes in transporter structure [
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In conclusion we have designed and characterized a novel ser
2021-09-16
In conclusion, we have designed and characterized a novel series of EAAT-blockers, exemplified by (-[4-(2-bromo-4,5-difluorophenoxy)phenyl]--asparagine)—a potent, selective, competitive non-substrate inhibitor of EAAT-2. As one of the most potent and selective EAAT-2 inhibitors identified to date,
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br Vesicular glutamate transporters VGLUTs
2021-09-16
Vesicular glutamate transporters (VGLUTs) Conclusions Due to the molecular cloning of EAAT and VGLUT subtypes, a better understanding of the functional properties of these carriers has been elucidated over the last few years. In the case of the EAATs, specific blockers, such as trans-2,4-PDC,
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SGLT inhibitors have been accepted as
2021-09-16
SGLT-2 inhibitors have been accepted as a new class of antidiabetic agent (Kurosaki and Ogasawara, 2013). They limit renal glucose reabsorption and promote urinary excretion of glucose, thereby reducing plasma glucose levels (de Leeuw and de Boer, 2016, Jojima et al., 2016, Pérez López et al., 2010,
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The main aim of our
2021-09-16
The main aim of our study was to identify whether glucokinase and Irs2 were required for beta cell replication induced by short-term HF diet feeding. Glucokinase plays a critical role in regulating blood glucose levels by catalysing the rate-limiting biochemical reaction of glycolysis [26,27]. In pa
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Cytarabine Apoptosis a form of programmed cell death is a cr
2021-09-16
Apoptosis, a form of programmed cell death, is a critical component in maintaining homeostasis and growth in all tissues and plays a significant role in immunity and cytotoxicity [54,55]. Although GR are expressed in all immune cells, the physiological outcomes of GR activation are highly cell type-
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br Experimental br Acknowledgments This project was
2021-09-16
Experimental Acknowledgments This project was generously supported by Grünenthal GmbH and IECB. We also thank the staff members of the technical platform of IECB and Grünenthal GmbH for their availability and their skills. Introduction Glucocorticoids (GCs) are essential steroid hormones t
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Knowing that our strongest phenotypic differences
2021-09-16
Knowing that our strongest phenotypic differences between the genotypes involved feeding behavior in various contexts, we decided to examine the case of restricted feeding and food anticipatory activity. Animals faced with a restricted schedule of food availability develop a series of anticipatory b
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In early a collaborative effort between the group that pione
2021-09-15
In early 2017, a collaborative effort between the group that pioneered the above described evidence of platinum-induced PUFA chemotherapy resistance and a group that has contributed to much of the known molecular pharmacology of FFA4, revealed that the molecular target of 16:4(n-3), which affords ch
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Compounds were tested for GPR activity in
2021-09-15
Compounds , were tested for GPR40 activity in a functional assay monitoring calcium flux in CHO Cy5 RNA mg transiently transfected with human GPR40 gene. As shown in , compound was found to be a nanomolar GPR40 agonist, while compound was much less potent than . To explore the structure activity
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There are several basic science studies that aim to investig
2021-09-15
There are several basic science studies that aim to investigate potential mechanisms behind the reduced incidence of MI in factor Xa inhibitor treated patients. Perzborn et al. reported that in-vitro addition of rivaroxaban reduced tissue-factor induced platelet aggregation (Perzborn, Heitmeier, & L
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br Introduction Regulation of transcription
2021-09-15
Introduction Regulation of transcription is a critical event of the embryonic development and epigenetic mechanisms such as histone modifications and DNA methylation appear important in mediating temporal changes, and differences among cells/tissues, of temporary stabilized transcriptomes (Mas et
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Taken together the four HRs couple with several
2021-09-15
Taken together, the four HRs couple with several different signaling pathways modulating various G-proteins (Fig. 1). Histamine H1R The H1R, including many other biogenic amine receptors, is one of the GPCR family members (see for a complete list e.g. http://www.gpcr.org/7tm/ or http://tools.gpc
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