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The PK and the tissue distribution profiles of k
2022-02-24

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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br Interference in coagulation assays Conversely
2022-02-24

Interference in coagulation assays Conversely to heparin, or heparin like Methicillin sodium salt (LMWH, Fondaparinux, Sodium Danaparoid), which are catalytic inhibitors requiring the presence of AT for their activity, as depicted on Fig. 2, DiXaIs are directly targeted to Factor Xa, and are reve
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A biochemical characterisation of this functionally crucial
2022-02-24

A biochemical characterisation of this functionally crucial LSD1-p53 interaction is the focus of this study. Using several complementary assays [29], [30], [31], [32], we find that a well-defined segment of p53-CTD is capable of binding to LSD1 active site, thereby inhibiting the enzymatic activity
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CTGF is an established YAP TAZ target gene
2022-02-24

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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br STAR Methods br Acknowledgments
2022-02-24

STAR★Methods Acknowledgments We thank the TCGA PanCanAtlas Analysis Working Group. This study was supported in part by grants from the NIH (CA175486 and CA209851 to H.L., CA217842 to G.B.M., and CCSG grant CA016672); a grant from the Cancer Prevention and Research Institute of Texas (RP140462
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Continuing studies of endocannabinoid ligands at GPR reveal
2022-02-24

Continuing studies of endocannabinoid ligands at GPR55 reveal that virodhamine (O-arachidonylethanolamine) and AEA can act as a partial agonists at GPR55; at high micromolar concentrations can inhibit β-arrestin recruitment (Sharir et al., 2012). It is likely that there are allosteric as well as ort
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Shikonin Diabetes induced damage results in peripheral nerve
2022-02-23

Diabetes-induced damage results in peripheral nerve pathology that Shikonin correlates with clinical signs and symptoms. Nerve injury that results in structural changes can be measured through clinical neurological assessment, quantitative sensory testing, nerve conduction studies, and peripheral ne
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br Dysregulation of glutamate transporter expression and fun
2022-02-23

Dysregulation of glutamate transporter expression and function Aberrant glutamate transporter function and expression are associated with various neurological disorders. Therefore, understanding the underlying mechanisms of EAAT1/2 expression may provide therapeutic targets for treating neurolog
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LXRs are physiological regulators of cholesterol and
2022-02-23

LXRs are physiological regulators of cholesterol and lipid metabolism and influence glucose metabolism. In addition, they have been shown to repress transcription of certain pro-inflammatory genes (Jakobsson et al., 2012; Ogawa et al., 2005; Terasaka et al., 2005). Thus, LXRs can either activate or
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Type II diabetes is characterized by an inability
2022-02-23

Type II diabetes is characterized by an inability to maintain glucose homeostasis due to insulin desensitization and/or insufficient insulin secretion. GPR40, also known as free fatty herpes simplex virus 2 receptor 1 (FFAR1), is a member of the G-protein-coupled lipid-activated family of receptors
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In the current study we report the
2022-02-23

In the current study, we report the properties of P. anserina mutants carrying mutations in a gene encoding the bi-functional enzyme 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase (PFK-2/FBPase-2). This enzyme catalyzes two opposite reactions (Pilkis et al., 1995, Rider et al., 2004): synthesi
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br Acknowledgments We apologize for the omission
2022-02-23

Acknowledgments We apologize for the omission of primary citations owing to space limitations. This work was supported by grants from National Natural Science Foundation of China (81772801 and 81472455 to C.D.), the Key Program of Zhejiang Provincial Natural Science Foundation (LZ17H160002 to C.D
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br Materials and methods br Results br Discussion ERK signal
2022-02-23

Materials and methods Results Discussion ERK5 signaling and its regulation has gained focus in recent years specially in the subject of cardiovascular biology, where this kinase plays a key role in angiogenesis and maintenance of blood vessel integrity [18,20,34,35]. The signaling pathways
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The third group also included
2022-02-23

The third group also included samples belonging to subjects with undetectable viraemia, for which the negative or persistence of the indeterminate WB result in subsequent samples indicated a non-HIV infection. In this subgroup, the VITROS HIV Combo test (as well as the other two tests) was negative
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Thus far it is reported
2022-02-23

Thus far, it is reported that the histone methyltransferase activity of SUV39H1 is regulated through some posttranslational modifications. For example, deacetylation of SUV39H1 at Lys-266 by SIRT1 deacetylase increases SUV39H1 activity [31], and methylation of SUV39H1 at Lys-105 and Lys-123 by SET7
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