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A compound structurally similar to PF has been
2022-02-09
A FRAX486 structurally similar to PF-03654746 has been developed by Pfizer (PF-03654764), with a minor change in the substituent attached to the cyclobutanecarboxamide moiety (Wager et al., 2011). This compound, with the chemical name trans-3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)phenyl]-N-(2-
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br Discussion br Conflict of interest br Acknowledgements We
2022-02-09
Discussion Conflict of interest Acknowledgements We thank Rosetta Barkley for expert technical assistance. We thank Robin Maser, James Calvet, Darren Wallace, and Jovanka Koo for many helpful discussions and expert technical advice. This work was supported by National Institutes of Health,
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The relaxant response to carperitide was
2022-02-09
The relaxant response to carperitide was influenced neither by the removal of the endothelium nor by treatment with the nitric oxide synthase inhibitor or nitric oxide scavenger. This result was to be expected as previous studies showing that the vasodilator action of atrial natriuretic peptide is e
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br Role of dynamin in NPRA endocytosis In recent
2022-02-09
Role of dynamin in NPRA endocytosis In recent studies using 125I-ANP binding assay and confocal microscopy, we have examined the role of dynamin in the internalization and trafficking of NPRA in a stably transfected HEK-293 β-Glycerophosphate sodium salt hydrate [69]. Our findings indicated that
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br Mechanism of action of herbs
2022-02-09
Mechanism of action of herbs and their active constituents used in hair loss treatment The hair growth cycle consists of 4 stages known as the anagen (active growth phase; takes 2–7years), catagen (involuting or regressing phase; takes approx. 2weeks), telogen (short resting phase; takes approx.
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Third we performed correlation analysis between
2022-02-09
Third, we performed correlation analysis between the results obtained using DMR agonist assay in HT-29 and Tango assay in the engineered U2OS cells. First, we compared their relative efficacy, the maximal responses after normalized to the maximal responses of zaprinast obtained using both DMR and Ta
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br Genetic rescue of GluR A dependent spatial working memory
2022-02-08
Genetic rescue of GluR-A-dependent spatial working memory Spatial working memory performance in GluR-A−/− mice can be restored by the forebrain-specific praziquantel biltricide of GluR-A subunits labeled with green-fluorescent protein (GFP) on an otherwise GluR-A knockout background (Schmitt et
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The biological actions of ghrelin are mainly due to
2022-02-08
The biological actions of ghrelin are mainly due to its interaction with GHSR-1a (Howard et al., 1996). The pharmacological properties of D-Lys3-GHRP-6, a selective antagonist of GHSR-1a, have been extensively studied (Beck et al., 2004, Benso et al., 2007, Sibilia et al., 2006). To study the recept
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Clinical trials of all GSIs have ended prematurely raising t
2022-02-08
Clinical trials of all GSIs have ended prematurely, raising the question on our understanding of their target, the γ-secretase/presenilin. Development of compounds to target γ-secretase and reduce Aβ production is complicated by the fact that γ-secretase/presenilin has critical biological function,
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Caffeine br Secretase modulators a loss
2022-02-08
γ-Secretase modulators: a loss of pharmacology? A lack of translation from in vitro to in vivo pharmacology is an unresolved issue among most GSMs. R-flurbiprofen was tested in clinical trials, however, it did not achieve statistical significance on either of its primary endpoints – cognition or
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The PK and the tissue distribution
2022-02-08
The PK and the tissue distribution profiles of 15k, 15j, 14d and 2 (Table 8) in male ICR mice were assessed. 15k, 15j, 14d all exhibited prolonged half-lives and improved plasma exposure. 15k achieved the highest concentration (15.45 μg/mL) in plasma among four compounds. The observation that 15j (S
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AVL-292 The cortical actin filaments are arranged in a netwo
2022-02-08
The cortical AVL-292 filaments are arranged in a network abuting the plasma membrane with a thickness of ∼190nm in living cells, that displays highly dynamic behaviors 15, 16, 17. Technical challenges, however, have hampered investigation of the detailed function dynamic interactions between the co
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br STAR Methods br Acknowledgments
2022-02-08
STAR★Methods Acknowledgments We thank the Shanghai Synchrotron Radiation Facility (SSRF) BL18U for help with X-ray data collection. We thank Dr. Thomas F.J. Martin for providing the pcDNA3.1-CAPS-1 plasmid and Dr. Xiaofei Yang for providing the pFHUUIG_shortU6 (l309) plasmid. We thank Dr. Shun
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The combination of HIV antigen and
2022-02-08
The combination of HIV antigen and antibody testing with the fourth generation immunoassays shortens the window Methicillin sodium salt synthesis for HIV by detecting HIV antigen, which appears in the blood before seroconversion [3,5,11,12]. Analysis of the seroconversion panels indicated the Elecs
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CTGF is an established YAP TAZ target gene
2022-02-08
CTGF is an established YAP/TAZ target gene which plays a central role in tissue remodeling. Downregulation of CTGF mediates collagen loss in chronologically-aged human skin whereas persistent activation of CTGF can result in excessive deposition of collagen and fibrotic disorders [63]. The authors f
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