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To gain insights for further
2021-12-02

To gain insights for further improvement of the agonistic activity, we compared the structural features of the -carbamate piperidine moiety in with that of the spirocyclic moiety in –. Obviously, the substituent corresponding to an isopropyl group on the -carbamate in was lacking in the spirocycli
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Previously we have shown that rapid
2021-12-02

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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The aim of this study is to
2021-12-02

The aim of this study is to explore new Glo-I inhibitors using the structure-based pharmacophore approach. Eighteen Glo-I co-crystallized structures have been explored to investigate their pharmacophoric features. Ninety two pharmacophoric models were generated. QSAR analysis followed by Ligand Prof
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br Acknowledgements Supported by the grant from
2021-12-01

Acknowledgements Supported by the grant from National Natural Science Funds of China (81371262). I would like to express my heartfelt gratitude to Professor Yonghua Zhu, who help language editing. Introduction Glucocorticoids are steroid hormones secreted from the adrenal glands in response t
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br Pathological consequences of disruption in the GABA T cur
2021-12-01

Pathological consequences of disruption in the GABA/T current equilibrium This issue has been particularly investigated in the context of absence seizures. These seizures are non-convulsive epileptic attacks present in many generalized genetic epilepsies that are characterized by a sudden and rel
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Acquiring resistance to the FGFR inhibitor
2021-12-01

Acquiring resistance to the FGFR inhibitor may determine treatment outcomes in patients with GC dependent on FGFR2 amplification, and we investigated the mechanism of AZD4547 resistance in FGFR2-amplified GC cells. We established a FGFR2-amplified GC cell line resistant to the selective FGFR inhibit
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br Conflicts of interest br Significance p is
2021-12-01

Conflicts of interest Significance p53 is required for the induction of cell senescence to limit the proliferation of polyploid cells. We found that Hippo signal deficiency or Yap activation in mouse livers result in polyploid formation and polyploid cell growth. The combined loss of Hippo sig
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br STAR Methods br Acknowledgments We thank the
2021-12-01

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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Considering that TGF plays a pivotal role in inflammation re
2021-12-01

Considering that TGF-β1 plays a pivotal role in inflammation, renal fibrosis, cell growth, differentiation, and apoptosis, it has been viewed as a vital mediator in kidney disease [49,50]. Studies have demonstrated that TGF-β1 is upregulated in both human and experimental kidney diseases [51,52]. TG
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Materials and methods br Results br
2021-12-01

Materials and methods Results Discussion Since LF is a protease, rapid and direct purification is critical for production of functional rLF. Although previous investigators improved the rLF quality by simplifying purification steps, avoiding formation of inclusion body, decreasing degradation
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NG,NG-dimethyl-L-Arginine hydrochloride br Materials and met
2021-12-01

Materials and methods Results Discussion Recently, we characterized the interaction of the PH domains of various Lbc family RhoGEFs with the activated small GTPase, RhoA, and demonstrated that this could serve as a positive feedback mechanism for robust activation of RhoA (Medina et al., 20
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To investigate the simultaneous effects of possible confound
2021-12-01

To investigate the simultaneous effects of possible confounding factors in the urinary 1-OHP excretion, multivariate regression analysis was performed (Table 3). Based on stepwise regression analysis, four independent variables (age, CYP1A1⁎4, GSTM1 and GSTP1 polymorphisms) entered into the final mo
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Several previous reports have demonstrated that epithelial
2021-12-01

Several previous reports have demonstrated that epithelial cell migration is important in promoting mucosal repair after damage caused by DSS and nonsteroidal anti-inflammatory drugs [33], [34], [35]. Cell migration is coordinated by many factors, including fibronectin and its receptor integrin α5,
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Cathepsin K Activity Fluorometric Assay Kit Compounds and w
2021-12-01

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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PI3K Akt mTOR Compound Library br Materials and methods br R
2021-12-01

Materials and methods Results Discussion and conclusions Our data demonstrate that native and 2-OMe-LPC analogues are GPR119 ligands and activate insulin secretion from βTC-3 pancreatic cells. LPC 18:1 was the first proposed endogenous ligand for GPR119 [1], however natural LPC has limited
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