• Herein we describe the design and optimization of

  2022-06-24

  

  Herein, we describe the design and optimization of fused-ring phenyl propanoic acids as novel GPR40 agonists, leading to the discovery of compound 40a which exhibits excellent pharmacokinetic properties, improved hepatobiliary transporter inhibition, and significant glucose-lowering efficacy during

• In the Joint United Nations Program

  2022-06-24

  

  In 2015, the Joint United Nations Program on HIV/AIDS (UNAIDS) proposed that by 2020, 90% of people living with HIV should be aware of their HIV status, as the first part of 90-90-90 strategy to end AIDS epidemic. Early detection of HIV allows initiating care for proper treatment, which impacts in m

• Bile acids synthesized in the liver are secreted into the

  2022-06-23

  

  Bile acids synthesized in the liver are secreted into the intestinal tract to facilitate the digestion and Fluoxymesterone of nutrients. Most bile acids are reabsorbed by the ileum and are transported back to the liver via the portal blood circulation. Recently, bile acids have also been considered

• br Materials and methods br Results

  2022-06-23

  

  Materials and methods Results Discussion The innate immune system plays an important role in protecting against IAV infections. However, the virus has the ability of escaping the innate immune system. Activating or enhancing an innate immune response before or during a viral infection will

• trp channels br Concluding Remarks and Future

  2022-06-23

  

  Concluding Remarks and Future Perspectives Our understanding of substrate targeting mechanisms utilized by kinases has grown tremendously in the past few years, but challenges still remain in relating these mechanisms to the organization of complex signaling networks. Substrate prediction based o

• Activity of compound in rat brain

  2022-06-23

  

  Activity of compound 10 in rat Vacuolin-1 tissue highlights the potential to use this new class of allosteric sGC inhibitors to study the role of the NO—sGC—cGMP signalling pathway in the brain. Reducing amounts of cGMP in cells would have implications in downstream signalling proteins, such as cGMP

• As more genes were identified

  2022-06-23

  

  As more genes were identified to cause IRDs, a relatively large proportion were found to either cause multiple phenotypes or multiple inheritance patterns. Out of the 112 autosomal genes that are listed in RETNET (as of July 22, 2016) that are known to cause non-syndromic IRDs (RP, LCA, and CRD), 16

• br Discovery of GPR A The murine niacin

  2022-06-23

  

  Discovery of GPR109A The murine niacin receptor, protein upregulated in macrophages by interferon-γ (PUMA-G), was identified as a G-protein-coupled receptor (GPCR) expressed in adipocytes and spleen [22], [23]. This finding suggested a role of this receptor in macrophage function [24]. In 2003, t

• br Disclosure statement br Acknowledgements We thank

  2022-06-23

  

  Disclosure statement Acknowledgements We thank Dr. Rona Carroll for her contribution to the preparation of the manuscript and Dr. Iosif Pediaditakis for his contribution to the preparation of the figures. This work was supported by NIHR01 HD019938 to U.B.K. Introduction The mammalian hypot

• br Results and discussion br Conclusion In

  2022-06-23

  

  Results and discussion Conclusion In this study the first binding assays based on a nonlabelled reporter ligand addressing GlyT1 are described. Following the concept of MS Binding Assays recently introduced in our group, binding of the well-known GlyT1 inhibitor Org24598 employed as reporter l

• Excessive extracellular glutamate may induce excitotoxic neu

  2022-06-23

  

  Excessive extracellular glutamate may induce excitotoxic neuronal damage in disorders of the CNS (Schwartz et al., 2003). EAATs are considered to contribute to prevention of excitotoxicity by glutamate uptake. Our data revealed that expression levels of membrane EAAT proteins in astrocytes are much

• Both anxiety like behavior and sucrose preference intake

  2022-06-23

  

  Both anxiety-like behavior and sucrose preference/intake were reduced in GPR40/FFAR1 KO male mice, while social behavior was normal in KO mice. These findings indicate that brain GPR40/FFAR1 is involved in the modulation of anxiety- and depression-like behavior in rodents. Previous studies have demo

• As cardiovascular disease accounts for the majority

  2022-06-23

  

  As cardiovascular disease accounts for the majority of deaths in subjects with T2D, it is imperative that we better characterize the cardiovascular risks and benefits of the various therapies we prescribe to these individuals to control their glycemia. Indeed, the potential to identify subsets of di

• Our own search towards aryl imidazole

  2022-06-22

  

  Our own search towards aryl-imidazole derived GSMs led to the discovery of the benzimidazole derivative (). It is one of the most potent GSMs to date, suffering however from sub-optimal drug-like properties. More recently, we have described the design and synthesis of bicyclic triazolo-derivatives,

• Acute lung injury is present in sepsis and SIRS and

  2022-06-22

  

  Acute lung injury is present in sepsis and SIRS and is associated with increased pulmonary levels of proinflammatory cytokines and neutrophil extravasation into the alveolar space [19], [24]. Hauser et al. [25] observed that fragmented mitochondria induced pulmonary inflammation via neutrophil activ

15943 records 425/1063 page Previous Next First page 上5页 421422423424425 下5页 Last page