• Although GLP has greater insulin releasing effects at pharma

  2022-04-18

  

  Although GLP-1 has greater insulin-releasing effects at pharmacological concentrations [10], it is apparent that the higher circulating concentrations of GIP combined with more pronounced increase in secretion following feeding make GIP the major physiological incretin [7], [11]. The peptide exerts

• br Methods br Results br Discussion The

  2022-04-18

  

  Methods Results Discussion The measurement of intraocular pressure was made with a commercially available rebound tonometer, the Tonovet®. In our studies, Tonovet® underestimated the intraocular pressure in both animal models, being this effect more pronounced in the rat. To study the effe

• CC-10004 Bile acids BAs are detergent like amphipathic molec

  2022-04-18

  

  Bile acids (BAs) are detergent-like amphipathic molecules synthesized from cholesterol in the liver, stored in the gallbladder, and released into the intestine after food intake in order to facilitate the CC-10004 of dietary lipids and liposoluble vitamins. BAs travel along the intestine and once in

• OCA has recently been approved for the

  2022-04-18

  

  OCA has recently been approved for the treatment of patients with PBC and is under study for diseases such as NASH, PSC and biliary atresia [30], [49]. Up to now, the beneficial effects of OCA have been related to its anti-cholestatic, anti-inflammatory and anti-fibrotic properties. We have here rep

• br Discussion and concluding remarks FPR is considered to be

  2022-04-18

  

  Discussion and concluding remarks FPR1 is considered to be a promising drug target for treating inflammatory and immunological diseases. Thus, natural compounds that could block and/or regulate FPR1 activity may be an important source of novel therapeutics for modulating inflammatory processes. H

• Hardy et al had demonstrated the role of GPR in

  2022-04-18

  

  Hardy et al. had demonstrated the role of GPR40 in mediating the proliferative effect of the FFA oleate's in breast cancer cells, and found that such effect can be reversed by silencing of GPR40 [14]. Similarly we have observed that inhibition of GPR40 function by its antagonist GW1100 inhibited cel

• ATN Ac PHSCN NH is a small peptide antagonist

  2022-04-18

  

  ATN-161 (Ac-PHSCN-NH2) is a small peptide antagonist of integrin α5β1, a recently developed anticancer drug that interacts with the N-terminus of the β1 region of integrin α5β1 to lock integrin α5β1 in its non-activated conformation (Wang et al., 2016). The drug has been tested in Phase 2 clinical t

• Histamine H and H receptors are considered as low affinity

  2022-04-16

  

  Histamine H1 and H2 receptors are considered as low affinity receptors (pKi of 4.2 and 4.3 respectively), whereas histamine H3 and H4 receptors as a high affinity receptors (pKi of 8 and 8.2 respectively) (Schreeb et al., 2013). Therefore it might well be that other histamine receptors might be invo

• In this study we also

  2022-04-16

  

  In this study, we also profiled the expression of the transporters in wild-type RBL-2H3 cells, RBL-2H3 Sc98 cells, and rat peritoneal mast cells. OCT1 and PMAT were expressed at high levels in both RBL-2H3 Sc98 and RBL-2H3 cells. However, OCT2 and OCT3 were weakly or least detected in RBL-2H3 Sc98 c

• In various models histamine has been shown to induce chemota

  2022-04-16

  

  In various models, histamine has been shown to induce chemotaxis. This was first appreciated over 40 years’ ago in studies with eosinophils (Clark et al., 1977). At that time, only histamine H1 and histamine H2 receptors were recognized and studies with ligands to these receptors indicated that neit

• br Main Text Metabolism drives diverse biological processes

  2022-04-16

  

  Main Text Metabolism drives diverse biological processes including differentiation, proliferation, and effector function in diverse cell types. In particular, the process of mounting an innate immune response to pathogens entails rapid sensing of a wide range of patterns displayed by invading mic

• br Mechanisms of HDAC inhibition dependent cardioprotection

  2022-04-16

  

  Mechanisms of HDAC inhibition-dependent cardioprotection Multiple preclinical studies have demonstrated potent cardioprotective benefits of HDAC inhibition in murine models of myocardial stress, including I/R [19,25,29,30]. TSA reduces myocardial infarct size by up to 50% [19,25]. In addition, tr

• Previous studies have established that phosphorylation

  2022-04-16

  

  Previous studies have established that phosphorylation of GC-B is required for activation of GC-B. Conversion of all six chemically determined serine and threonine phosphorylation sites in GC-B to alanines produced a properly folded enzyme that retained GC activity under synthetic detergent activati

• Several compounds have been described in the literature

  2022-04-16

  

  Several compounds have been described in the literature as inhibitors of the sGC. Among them, methylene blue and LY83583 () are not direct sGC inhibitors, but rather block cGMP formation by generating superoxide anion radicals that deactivate NO. Despite their extensive use in plethora of research s

• Introduction Although G protein coupled receptor GPR

  2022-04-16

  

  Introduction Although G-protein-coupled receptor 55 (GPR55) was considered a cannabinoid receptor, it differs phylogenetically from cannabinoid type 1 (CB1) and type 2 (CB2) receptors as it lacks the classic cannabinoid-binding pocket (Baker et al., 2006). GPR55 is sensitive to an array of cannabin

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