• Sometime ago we have described diamino triazines as histamin

  2021-09-30

  

  Sometime ago we have described diamino-1,3,5-triazines as histamine H4R ligands,12, 13 and aryl derivatives of the 1,3,5-triazine, which attenuated inflammatory and nociceptive response in vivo in the rodent models of inflammation induced by bace inhibitors and zymosan. In this work we describe new

• br Material and methods br Results br Discussion HBV

  2021-09-30

  

  Material and methods Results Discussion HBV develops several strategies to suppress antiviral immune responses. Here, we used a bifunctional siRNA molecule to silence HBx and activate RIG-I, which induced HBV inhibition partly mediated by RIG-I in HBV-carrier mice. Furthermore, this 3p-siHB

• Although it is currently unknown why the

  2021-09-30

  

  Although it is currently unknown why the longer splice variant found in the human has not been found in any other species, similar results have been reported for other receptors, including the Anidulafungin receptor splice variant ERbeta2 identified in human and primate, but not other species (Sier

• More recently several groups have characterized a

  2021-09-30

  

  More recently, several groups have characterized a role for GPR120 signaling via omega-3 fatty acids in amelioration of alcoholic hepatic injury and non-alcoholic fatty liver disease (NAFLD) [18], [19]. Nakamoto et al. demonstrated protective effects of the omega-3 fatty Glycopyrrolate docosahexaeno

• Previous studies have demonstrated that cannabinoid potentia

  2021-09-30

  

  Previous studies have demonstrated that cannabinoid potentiation of GlyR α3 subunits contributes to cannabinoid-induced analgesia. For instance, Dehydroxylcannabidiol (DH-CBD), a chemically modified cannabinoid, can alleviate acute pain and chronic inflammatory pain by targeting spinal α3 GlyRs (Xio

• In this study we present

  2021-09-30

  

  In this study, we present the synthesis and structure–activity studies of a structurally distinct series possessing high potency and selectivity in HEK cell lines together with a potentially promising overall biopharmacological profile. Focusing on creating sufficient structural dissimilarity with g

• The dopamine substrate currents IDA IControl were determined

  2021-09-30

  

  The dopamine substrate currents (IDA – IControl) were determined at different holding potentials (IV curves) in transfected HT22 cells (Fig. 5A). The plot for HT22 cells transfected with DAT exhibited the typical behavior of dopamine transporter currents (Ingram et al., 2002; Sonders et al., 1997),

• br Materials and methods br Results br

  2021-09-30

  

  Materials and methods Results Discussion The previous studies have reported that positive GLUT1 expression had a predictive value for prognosis of lung cancer patients (Younes et al. 1997a; Meijer et al., 2012; Sasaki et al., 2012). Our conclusion was accordant with these studies. Recently,

• br Results and discussion br Conclusion In summary we design

  2021-09-29

  

  Results and discussion Conclusion In summary, we designed and discovered a series of novel GPR40 agonists containing 3,5-dimethylisoxazole with improved tPSA and ideal cLog P. Most of these compounds were confirmed as excellent GPR40 agonists in vitro. Especially, compound 11k exhibited robust

• Through the analysis of various

  2021-09-29

  

  Through the analysis of various synthetic GPR40 agonists as reported in literature, we found that a number of these compounds contained a phenylpropanoic methoxsalen motif which was inspired from naturally occurring medium to long chain fatty acids. For instance, in the early period of discovering T

• Several transgenic and knockout congenic mouse models

  2021-09-29

  

  Several transgenic and knockout/congenic mouse models have been generated in order to assess the role of FFAR1 for proper insulin secretion and maintenance of glucose homeostasis. The results obtained with three different receptor knockout mouse models were not consistent. The protection against hig

• The RAS RAF MEK ERK pathway also known as

  2021-09-29

  

  The RAS/RAF/MEK/ERK pathway (also known as the MAPK/ERK pathway) is one of the most important signaling pathways in PDAC. Activation of the MAPK/ERK pathway promotes PDAC growth and apoptosis resistance in response to gemcitabine [43,44]. We previously demonstrated that inhibition of GPX4 can overco

• Batimastat br Results br Discussion Impaired BBB functions e

  2021-09-29

  

  Results Discussion Impaired BBB functions evoke vasogenic edema, which elevates intracranial pressure and leads to a life-threatening condition (Sperk, 1994, Unterberg et al., 2004, Simard et al., 2007). In addition, vasogenic edema formation results in the worsen consequence contributing to p

• There are many histone H

  2021-09-29

  

  There are many histone H3K9 demethylases, including JMJD1 A, JMJD2 A, JMJD2B, and JMJD2C (Kooistra and Helin, 2012). Considering that EPO CHIR-99021 is regulated by hypoxia, we further analyzed several hypoxia-induced H3K9 demethylases, such as JMJD1 A, JMJD2B and JMJD2C (Beyer et al., 2018; Pollard

• br Materials and methods br Results Estimations of OMP

  2021-09-29

  

  Materials and methods Results Estimations of OMP generated by the proposed mechanism (Fig. 1) were first performed for the range of 0.001–2 mM of Tubacin concentration in the cytosol. It was assumed that only 5% of all VDACs in MOM form the ANT-VDAC1-HKI contact sites, and that the fraction o

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