• In summary this study shows that compound d

  2021-10-11

  

  In summary, this study shows that compound 4d has strong clinical potential as an efficient GLP-1/GCGR agonist exhibits weight-lowering, lipid-regulation and diabetes-protective effects and plays an important role in the prevention and therapy of diet induced obesity and dyslipidemia. The present st

• In the light of the above mentioned

  2021-10-11

  

  In the light of the above-mentioned considerations, it is interesting to note that the FPR-related research with regards to bias agonism did not prosper during considerably during the last decade (possible exceptions are [[8], [9], [10], [11]]. However, with new insights in receptor chemistry and fu

• br ABT aR aR methyl hexahydropyrrolo

  2021-10-11

  

  ABT-288 (2-[4'-((3aR,6aR)-5-methyl-hexahydropyrrolo[3,4-b]pyrrol-1-yl)-biphenyl-4-yl]2H-pyridazine-3-one) is a selective H3R antagonist/inverse agonist developed by Abbott. Structurally, it is a compound with molecular weight (MW) 372.46 g/mol, three H-bond acceptors (HBA), and Moriguchi LogP (MLo

• br Tissue Specific Roles for HIF

  2021-10-11

  

  Tissue-Specific Roles for HIF/PHD Isoforms Hypoxia signaling pathways are active in almost all mammalian cells, including immune 5 03 synthesis and tissues such as the epithelium and endothelium. This is of crucial importance when considering the influence of environmental hypoxia in inflammatory

• Glucagon (19-29), human mg Over the last few years experimen

  2021-10-11

  

  Over the last few years, experimental evidence for the involvement of Epac1 in cancer progression is beginning to emerge (Almahariq et al., 2015, Banerjee and Cheng, 2015, Parnell et al., 2015, Parnell et al., 2015, Schmidt et al., 2013). For example in melanoma cells, silencing of Epac1 attenuates

• Concerning the molecular mechanisms underlying transcription

  2021-10-11

  

  Concerning the molecular mechanisms underlying transcriptional regulation of the GSTP1-1 gene expression we and others have characterized structural and functional properties of the human GSTP1-1 promoter. GSTP1-1 gene promoter activity is driven by a TATA-box [16] as well as Spl [16], [17], AP-1 [1

• br STAR Methods br Acknowledgments This work was

  2021-10-11

  

  STAR★Methods Acknowledgments This work was supported by the American Diabetes Association (grant 1-12-BS-161 to J.D.P.), an NIH predoctoral T32 in Autoimmunity and Immunopathology grant (AI089443-05 to D.M.P.), the NIH (grant DK099550 to H.M.T.), the American Association for Cancer Research (S

• Phos-tag Biotin BTL-104 The intracellular signaling that me

  2021-10-11

  

  The intracellular signaling that mediates the adipogenesis induced by GPR120 still remains largely unknown. In the present study we showed that TUG-891 induced the activation of [Ca2+]i and ERK1/2 signaling in 3T3-L1 cells. Moreover, incubation of TUG-891 combined with BAPTA-AM or U0126 abolished TU

• Vicriviroc Malate In humans the effect of

  2021-10-11

  

  In humans, the effect of GnRH and hCG on trophoblast invasion was found to be mediated through extracellular matrix remodeling by facilitating the activity of MMP2 and MMP9 [13], [18], [44]. Both Vicriviroc Malate are collagenases that degrade extracellular matrix. In canines, this has not yet been

• Melittin GnRH ant have been designed to obtain pharmacologic

  2021-10-11

  

  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

• An alternative approach to improving pharmacokinetic profile

  2021-10-11

  

  An alternative approach to improving pharmacokinetic profile while retaining high GlyT1 potency was also pursued. Libraries were prepared in which potency enhancing piperidine C4 substituents were combined with clearance lowering truncated alkyl sulfonamides. The result was the discovery of (). Unl

• Two pathways have emerged to

  2021-10-11

  

  Two pathways have emerged to explain the beneficial metabolic effect of Roux-en-Y bypass [Fig. 3]. Firstly, the rapid delivery of nutrients to the distal small intestine and bowel might up-regulate secretion of a physiological stimulus that improves glucose homeostasis. As such, GLP-1 represents an

• The molecular nature of these putative Ca

  2021-10-11

  

  The molecular nature of these putative Ca2+ ascorbic acid receptor is at present unknown. Apart from the NSVDC channel, which is permeable to Ca2+ [27], [15] functional Ca2+ channels have been identified in patch clamp experiments [28]. These channels, which were characterized as B-channels, seem t

• br Conclusions GPCRs are versatile signaling molecules regul

  2021-10-09

  

  Conclusions GPCRs are versatile signaling molecules regulating almost all physiological processes, including energy homeostasis and glucose homeostasis.105, 106 They also prove to be important therapeutic targets. Drugs targeting GPCRs account for 30% of current pharmaceutical sales. GPR40 is a m

• This study introduces a mouse model

  2021-10-09

  

  This study introduces a mouse model carrying the point mutation R258W in Ffar1, which abolishes the stimulation of insulin secretion in response to long chain fatty acids. The minimal genetic alteration mirrors the human situation and has the advantage over conventional knockout/congenic mouse model

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