• While the specific set of challenges

  2022-02-08

  

  While the specific set of challenges associated with deorphanization and transforming each poorly characterized GPCR into a useful drug target will be unique, much can be learned by considering how these issues have been addressed for other receptors. One group of poorly characterized GPCRs that hav

• In the present study we found that the expression

  2022-02-08

  

  In the present study, we found that the expression of GPR120 in decidua from women of spontaneous abortion was significantly downregulated compared to the decidua from that of normal pregnancy. Moreover, GPR120 deletion (GPR120−/−) or inhibition predisposed mice to LPS or RU486 induced abortion, ind

• Taxifolin br Introduction Over the past two decades the prev

  2022-02-07

  

  Introduction Over the past two decades, the prevalence of obesity and obesity-associated metabolic diseases, such as T2D, insulin resistance, atherosclerosis and stroke, have been dramatically increased globally [1], [2], and obesity has been suggested to be the leading cause of the reduced life

• br Discussion Naloxone and CTAP were able to alter

  2022-02-07

  

  Discussion Naloxone and CTAP were able to alter the febrile response induced by gp120. This effect was particularly evident during the initial hours following gp120 administration (90–210min). We also investigated the potential role of the delta-2 opioid receptor in gp120-induced fever. The delta

• br Materials and methods br

  2022-02-07

  

  Materials and methods Results Discussion Conclusion Pharmacophore modeling was applied to explore new probable Glo-I inhibitors. Ninety two pharmacophoric models were generated representing diverse types of interaction between co-crystallized ligands and corresponding binding site. The g

• Na K ATPase adenosine triphosphate ATP and astrocytic glutam

  2022-02-07

  

  Na+/K+-ATPase, Alosetron receptor and astrocytic glutamate transporters act together to maintain sodium and potassium gradients and the proper activities of EAAT1 and EAAT2 (Rose et al., 2009; Sheean et al., 2013); nevertheless, in present study, Na+/K+-ATPase activity was shown to be increased as

• br Methods br Results br Discussion In

  2022-02-07

  

  Methods Results Discussion In this series of studies we hypothesized that FHH-GHSRm1/Mcwi rats would, relative to their WT counterparts, exhibit a metabolic and behavioral phenotype reminiscent of GHSR−/− mice. Through the use of the GHSR−/− mouse, a great deal about the role of ghrelin sig

• Similarly Somavarapu and Kepp constructed

  2022-02-07

  

  Similarly, Somavarapu and Kepp [29] constructed a PS1 homology model using 4HYG as a template, plus modeling the TM6-TM7 intracellular segment (amino acids 273 to 374). In this study, the authors considered for the first time the mature and immature (not autoproteolyzed) forms of PS1 component, sinc

• atm kinase inhibitor Similarly Somavarapu and Kepp construct

  2022-02-07

  

  Similarly, Somavarapu and Kepp [29] constructed a PS1 homology model using 4HYG as a template, plus modeling the TM6-TM7 intracellular segment (amino acids 273 to 374). In this study, the authors considered for the first time the mature and immature (not autoproteolyzed) forms of PS1 component, sinc

• Gal is a amino acid residue peptide comprising amino acids

  2022-02-07

  

  Gal is a 29-amino GSK1838705A residue peptide, comprising 30 amino acids in humans, isolated from the porcine intestine 30 years ago (Tatemoto et al., 1983). It has been shown to be involved in the regulation of numerous processes, including neuroendocrine control of systems such as the hypothalami

• Through the analysis of various synthetic

  2022-02-07

  

  Through the analysis of various synthetic GPR40 agonists as reported in literature, we found that a number of these compounds contained a phenylpropanoic GW9662 motif which was inspired from naturally occurring medium to long chain fatty acids. For instance, in the early period of discovering TAK-8

• Acknowledgments br Introduction Stress plays a key

  2022-02-05

  

  Acknowledgments Introduction Stress plays a key role in the etiology and/or exacerbation of major depressive disorder characterized by loss of energy, feelings of hopelessness and anhedonia [1]. Ample evidence clearly suggests that endocannabinoids (eCBs) participate in stress-associated neurona

• PRT 4165 br Acknowledgments We would like to thank Coordena

  2022-02-05

  

  Acknowledgments We would like to thank Coordenação de Aperfeiçoamento de Pessoal do Ensino Superior (CAPES) and Conselho Nacional de Desenvolvimento Cientifico e Tecnológico (CNPq) for the grants and scholarships provide to the authors of this work. Introduction Human Immunodeficiency Virus t

• The GSTP promoter region in PCA cells

  2022-02-05

  

  The GSTP1 promoter region in PCA cells without or with reduced GSTP1 mRNA expression had a different histone modification pattern than BPH-1 cells with GSTP1 mRNA expression: the repressive histone modifications H3K9me3/H3K27me2 were distinctly increased and H3K27me3/H3K9me2 were slightly decreased

• Excessive adiposity is also a key pathogenic factor

  2022-02-04

  

  Excessive adiposity is also a key pathogenic factor in the development of CVD. Through reductions in bodyweight, GPR120 agonism is therefore also implicated as a potential therapy for obesity and heart and vessel disease. In addition to weight loss, when compared with their wild-type littermates, GP

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