• Mice lacking S nitrosoglutathione reductase

  2022-05-21

  

  Mice lacking S-nitrosoglutathione reductase (GSNOR), a denitrosylase that regulates S-nitrosylation, have increased levels of S-nitrosoglutathione (GSNO) and exhibit nitrosative stress. GSNO is in equilibrium with protein S-nitrosylation in cells, and GSNOR controls the cellular concentration of pro

• Based on these findings we set out to identify

  2022-05-21

  

  Based on these findings, we set out to identify GPR109A agonists capable of biasing the receptor's signaling towards the functional anti-lipolytic and presumed therapeutic response, and away from the flushing side-effect pathways. Indeed, using recombinantly expressed GPR109A, two classes of compoun

• molarity conversion CD binding to gp causes

  2022-05-21

  

  CD4 binding to gp120 causes a large scale conformational change of gp120 which involves the gp120 core structure and the transitions of inner-domain layers (layer 1, 2 and 3), but also involves the movement of the major loops (V1, V2 and V3) [16], [17], [18], [19]. For instance, the V2-loop joins th

• CD binding to gp causes

  2022-05-21

  

  CD4 binding to gp120 causes a large scale conformational change of gp120 which involves the gp120 core structure and the transitions of inner-domain layers (layer 1, 2 and 3), but also involves the movement of the major loops (V1, V2 and V3) [16], [17], [18], [19]. For instance, the V2-loop joins th

• GnRH ant have been designed to obtain pharmacological compou

  2022-05-21

  

  GnRH-ant have been designed to obtain pharmacological compounds to block the pituitary–gonadal axis without the undesirable flare effect exerted by GnRH itself or by the GnRH-a (see Section 2.2). GnRH-ant competitively block the binding of GnRH to GnRHRs (Schally, 1999; Tan & Bukulmez, 2011); they p

• br Materials and methods br Results In

  2022-05-21

  

  Materials and methods Results In this study we re-examined the kinetics of ET transport and tested the ability of various suggested substrates of OCNT1 to inhibit ET uptake. Using a native ET transporter expressed in the human HeLa cell line ET was found to be taken up with a Km of 51 μM and V

• Human Glucocorticoid Receptor hGR was first cloned in

  2022-05-21

  

  Human Glucocorticoid Receptor (hGR) was first cloned in 1985 (Hollenburg et al., 1985). It is a modular protein comprised of an N-terminal trans-activating domain (NTD), a C-terminal ligand-binding domain (LBD) and a central DNA- binding domain (DBD). The DBD is highly conserved and has two zinc fin

• Similarly both neofunctionalization and subfunctionalization

  2022-05-21

  

  Similarly, both neofunctionalization and subfunctionalization likely occurred for the duplicated proglucagon genes. The change in function of GLP-1 would be a neofunctionalization, however in this case it acquired a redundant function – a function that largely overlaps with glucagon effects in the l

• For many plasma membrane receptors including

  2022-05-21

  

  For many plasma membrane receptors including GPCRs, their density on the cell-surface is finely controlled by various transcriptional, post-transcriptional and post-translational mechanisms, and is often a determinant of overall receptor function in a cell. To date, the transcriptional regulation an

• More recently NMR techniques have been used to monitor K

  2022-05-21

  

  More recently, NMR techniques have been used to monitor K+ () fluxes in isolated rat hearts. These reveal an increased rate of passive efflux of from Langendorff-perfused hearts at 20°C compared to 36°C or 10°C (Gruwel, Kuzio, Xiang, Deslauriers, & Kupriyanov, 1998). Similar experiments assessed th

• br Summary The presented results of the analysis of

  2022-05-21

  

  Summary The presented results of the analysis of the unfolding of G-quadruplex and i-motif, which may appear within the telomeric DNA region, led to several important conclusions. Namely, determination of the work necessary to unfold of these structures, in biased molecular dynamics involving ste

• br The bile acid farnesoid X receptor FXR The

  2022-05-21

  

  The “bile acid” farnesoid X receptor (FXR) The Farnesoid X Receptor (FXR) is a ligand-activated nuclear receptor belonging to the Nuclear Receptor superfamily of transcription factors exploiting various crucial functions in mammalian physiology, including reproduction, development and metabolism

• We also wonder what function s both

  2022-05-20

  

  We also wonder what function(s) both FPPS1 and FPPS2 genes had in leaf. As some research indicated that the alpha-farnesene was also detected in ripe leaf of crabapple (Malus sp.) (Wu et al., 2012), one or both of them may be related to the synthesis of alpha-farnesene in leaf. To our knowledge, th

• Fatty acid amide hydrolase FAAH is a

  2022-05-20

  

  Fatty GSK2194069 amide hydrolase (FAAH) is a membrane-bound enzyme which releases arachidonic acid and ethanolamine by breaking amide bond of AEA. It also controls the cellular uptake of AEA, by creating and maintaining an inward concentration gradient leading to AEA-facilitated diffusion via a spec

• br Acknowledgments I thank Takeshi

  2022-05-20

  

  Acknowledgments I thank Takeshi Sakaba for critical reading of the manuscript and helpful comments. This work was supported by JSPS/MEXT KAKENHI Grant Numbers 17K19466, 17H03548. Introduction The oral route of drug application is the main route in pharmacology since it is easy to handle and o

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