• br EphB as a therapeutic target in

  2021-02-20

  

  EphB4 as a therapeutic target in cancer Eph receptors and ephrins are promising new therapeutic targets in cancer. Various strategies have been employed to evaluate the interference of tumor-promoting effects or the enhancement of tumor suppressive effects. The inhibition of the Eph-ephrin system

• br Materials and methods br

  2021-02-20

  

  Materials and methods Results Discussion The EP4 FAUC-365 synthesis for PGE2 is similar to the EP1, EP2 and EP3 receptors in that they all have seven transmembrane segments and are coupled to Gα subunits of heterotrimeric G proteins, with a different Gα subunit for each receptor (Sugimoto

• br Acknowledgments br Introduction Hypertensive retinopathy

  2021-02-20

  

  Acknowledgments Introduction Hypertensive retinopathy is a disease of the retinal microvasculature associated with elevated blood pressure (Fraser-Bell et al., 2017). Narrowing of retinal arterioles occurs in the early stage of the disease, and with persistent hypertension further vascular pat

• br Materials and methods br Results and discussion br Conclu

  2021-02-20

  

  Materials and methods Results and discussion Conclusions Data about the ability of non-conventional ligands to operate class-A GPCRs have been accumulating. Specifically, increasing evidence indicates that oxysterols, oxidized derivatives of cholesterol, are involved in many activities that

• br Results and discussion br Conclusion Based on the structu

  2021-02-19

  

  Results and discussion Conclusion Based on the structure of ThDP, in this study, a series of novel ThDP analogs 6a-6g and 8a-8g were designed by optimizing triazole-benzene linker and modifying the substituent group of triazole ring. Then they were synthesized as potential inhibitors of Cy-PDH

• GLP also showed cardioprotective effects i

  2021-02-19

  

  GLP-1 also showed cardioprotective effects (i.e., infarct size reduction and ejection fraction improvement) in experimental models of myocardial ischemia-reperfusion injury by suppressing caspase-3 activation and preventing apoptosis of cardiomyocytes [[50], [51]]. Of note, such a cardioprotection w

• In the present study the expression of the CYP C

  2021-02-19

  

  In the present study, the VE821 of the CYP2C11 gene and the levels of its protein and activity were decreased in rats with liver insufficiency and in rats after induced dysfunction of the serotonergic system during normal liver function. Moreover, serotonergic system dysfunction during liver insuff

• CH 223191 The mechanism by which OC use leads to impaired

  2021-02-19

  

  The mechanism by which OC use leads to impaired glucose tolerance is yet to be fully clarified. Decreased insulin sensitivity appears to be mainly accounted for by estrogenic component and this effect may be modified by progestogenic component [14], [15]. Estrogenic effect on glucose tolerance has b

• Furan analogs and N methylpyrrole analogs had completely

  2021-02-19

  

  Furan analogs and N-methylpyrrole analogs had completely different SARs. For example, replacement of the furan-2-sulfonyl moiety of 6 with the furan-3-sulfonyl moiety resulted in 8 with a decreased EP1 nox4 affinity and an increased antagonist activity, while the corresponding chemical modification

• Nitrid oxide NO and its potential endogenous

  2021-02-18

  

  Nitrid oxide (NO) and its potential endogenous production as an endothelium-derived factor was the first gaseous molecule accepted to be a signaling mediator in the organism [4,5]. NO plays a key role in physiological regulation of the diacerein receptor and exerts physiological functions in the ne

• Since the number of peptides hydrolized

  2021-02-18

  

  Since the number of peptides hydrolized by PEP is quite large, it is not easy to relate the increase of enzymatic activity with the altered changes of a concrete peptide. However, it is noticeable that imbalances of several natural substrates of PEP [6], such as angiotensins, bradykinin, vasopressin

• br DDR mediated signaling DDRs initiate signaling

  2021-02-18

  

  DDR-mediated signaling DDRs initiate signaling pathways in a context and cell type-dependent manner. For instance, DDR1 was reported to activate ERK in vascular smooth muscle Mepivacaine HCl (Lu et al., 2011), to inhibit ERK in mesangial cells (Curat and Vogel, 2002), and to have no effect on ER

• br Experimental Procedures br Author Contributions br

  2021-02-18

  

  Experimental Procedures Author Contributions Acknowledgments We acknowledge Géraldine Le Goff and Mathieu Canales for blood sampling, Cécile Gameiro and Jean-Pierre Aubry for flow cytometry technical assistance, Giuseppe Pantaleo for support, and Britta Engelhardt, Gisella Puga-Young, Nicol

• Ubiquitin activating enzyme activates ubiquitin

  2021-02-18

  

  Ubiquitin-activating enzyme activates ubiquitin by a three-step process with ATP as a cofactor (Chen et al., 2011, Haas and Rose, 1982, Haas et al., 1982). We demonstrated that ATP is required for mRFP-Ub–E1 formation under non-reducing conditions (Fig. 2A). A time course of radioactive ATP producti

• br Funding This work was supported by

  2021-02-18

  

  Funding This work was supported by the grants from MSD, Terumo Life Science Foundation, Takeda Science Foundation, and Japan Diabetes Foundation. Disclosures Acknowledgments The authors thank C. Morimoto (Juntendo University, Tokyo, Japan) and K. Takeda (Immunology Frontier Research Center

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