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Previously we have shown that rapid action of E
2022-03-03
Previously, we have shown that rapid action of E2in vitro is mediated through two E2 membrane receptors, GPR30 (GPER1) and the STX-sensitive membrane receptors (Noel et al., 2008; Kenealy et al., 2011a, Kenealy et al., 2011b). This is significantly different from receptors implicated in the positive
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In parallel we were also
2022-03-03
In parallel, we were also preparing and evaluating other piperidine bioisosteres and modifications to – to further access additional novel intellectual property (IP) space. Modeling work suggested that 4-position homologated piperidines, as well as 3-position homologated azetidines overlapped favora
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br Introduction Given the growing acceptance of ergothionein
2022-03-03
Introduction Given the growing acceptance of ergothioneine (ET) as a biologically important agent with potential therapeutic applications [[1], [2], [3], [4]] it is increasingly important to clearly establish the role of the organic cation transporter (novel) type 1 (OCTN1). OCTN1 was discovered
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To this end we evaluated novel D
2022-03-03
To this end, we evaluated novel D22 analogs for selectivity to inhibit substrate transport in OCT2, OCT3, and PMAT heterologous cell ABT systems, and in mouse hippocampal and striatal preparations. Chosen analogs were based upon availability of essential chemical precursors (e.g. 6-substituted-2-me
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br Characterization and regional localization of Glu transpo
2022-03-03
Characterization and regional localization of Glu transporters Molecular studies led to the description of five subtypes of plasma membrane Glu transporters termed in accordance to their human or rodent origin (Kanai and Hediger, 1992, Pines et al., 1992, Storck et al., 1992). In humans, these tr
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br Conflicts of interest br Acknowledgments This work
2022-03-02
Conflicts of interest Acknowledgments This work was supported by the following funds: National Natural Science Foundation of China (81502222); Natural Science Foundation of Hubei Province (2013CFB370); Training program for Wuhan young and middle-aged medical backbone personnel (2017–51). In
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br Conclusion Our experiments have confirmed the effects of
2022-03-02
Conclusion Our experiments have confirmed the effects of fasting, DIO, and E2 on the expression of Ghsr, Npy, and Agrp in the ARC (Briggs et al., 2013, Briggs et al., 2010, Brown and Clegg, 2010, Coppola et al., 2007, Palou et al., 2009, Roepke et al., 2008, Verhulst et al., 2012). However, gene
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Among sensitizers tested in the previous study six test
2022-03-02
Among 22 sensitizers tested in the previous study, six test chemicals were pre- or pro-haptens (Nepal et al., 2018a). Among 6 chemicals, hydroquinone and 2-aminophenol, strong sensitizers, were falsely classified as non-sensitizers due to the lack of metabolic activation (Nepal et al., 2018a). Liter
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br Results and discussion The synthesis
2022-03-02
Results and discussion The synthesis of core aldehyde building block 2 commenced with known aldehyde 5. The Horner–Wadsworth-Emmons olefination of the latter (using commercially available 6) gave cinnamate ester 7. Facile hydrogenation of the double bond in 7 was achieved over Raney nickel withou
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Canonical and non canonical Wnt signaling pathways
2022-03-02
Canonical and non-canonical Wnt signaling pathways play essential roles in various cellular activities, including cell fate determination, proliferation, migration and gene expression [57]. The canonical Wnt pathway (β-catenin dependent pathway), is activated by the binding of Wnt ligands, leading t
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br STAR Methods br Acknowledgments Anthony Koleske is
2022-03-01
STAR★Methods Acknowledgments Anthony Koleske is thanked for helpful discussions and for providing p190RhoGAP-A cDNA. Anatoly Kiyatkin and Mark Lemmon are thanked for use of the BioTek Synergy 2 plate reader for the MANT assays. Leena Kuruvilla is thanked for assistance with the thermal shift a
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INTRODUCTION Scar formation and tissue regeneration are oppo
2022-03-01
INTRODUCTION Scar formation and tissue regeneration are opposite results of the wound healing process. Although fibrosis is more common after skin injury, full skin regeneration results in complete replacement of adnexa and function. Examples of tissue regeneration in mammalian systems include annu
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Compounds and were tested for pharmacodynamic effects in
2022-03-01
Compounds , and were tested for pharmacodynamic effects in a mouse oral glucose tolerance test (oGTT) in wild-type and GPR120 deficient mice, and each compound demonstrated GPR120 mechanism-based effects. Data for compound is shown in , indicating mechanism-based reduction in glucose excursion a
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Attempting to further elucidate the role of glucagon and act
2022-02-28
Attempting to further elucidate the role of chemical d and activation of the Gcgr without the influence of GLP-1, we used DT-Gcg mice with acute knockdown of all proglucagon products. This mouse model has previously been shown previously to have a normal total islet area as well as β cell area comp
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As mentioned earlier two different isoforms of
2022-02-28
As mentioned earlier two different isoforms of TFE3 [16] have been reported viz. the full length (TFE3L) and smaller (TFE3S) without exon 1&2. TFE3S lacks an N-terminal acidic activation domain which is present in TFE3L hence is a dominant negative form of TFE3L [51]. This dominant negative feature
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