• br Introduction The discovery that the

  2021-12-22

  

  Introduction The discovery that the nitric oxide (NO), soluble guanylate cyclase (sGC), and cyclic guanosine monophosphate (cGMP) pathway mediates erection has led to the use of phosphodiesterase type 5 (PDE-5) inhibitors as the gold standard for treating erectile dysfunction (ED) through the inh

• The ketone body receptor HCA is most likely

  2021-12-22

  

  The ketone body receptor HCA2 is most likely not active under normal conditions, since local levels and plasma levels of ketone bodies such as β-HB are too low to activate the receptor. However, overnight fasting or prolonged starvation results in plasma levels of the ketone body in the millimolar r

• GPR co localizes with ghrelin in the duodenum gustducin in

  2021-12-22

  

  GPR120 co-localizes with ghrelin in the duodenum [17], α-gustducin in the small intestine and type II taste bud cells 18, 19, neuropeptide Y centrally in the arcuate nucleus [20] and glucagon-like peptide 1 (GLP-1) in the colon and circumvallate papillae taste bud cells 6, 21, 22. Interestingly GPR1

• It is well known that the

  2021-12-22

  

  It is well known that the expression of GPR109A is regulated under physiological and pathological conditions. We previously found that GPR109A expression in islet beta-cells increased with age and was up-regulated by interferon-γ (Li et al., 2011). GPR109A levels in Min6 and INS-1E islet beta-cells

• br Results and discussion br Conclusion

  2021-12-22

  

  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

• br Results and discussion br

  2021-12-22

  

  Results and discussion Conclusion In conclusion, we designed and synthesized a novel series of thiosemicarbazide-1,2,3-triazole hybrids 10a-o. Further, α-glucosidase inhibitory activity of the synthesized compounds 10a-o was evaluated. The obtained results showed that all the synthesized thios

• br Voltage dependent anion channel

  2021-12-22

  

  Voltage-dependent anion channel VDAC is a ubiquitous protein showing well conserved structural and functional properties in spite of major variations in its sequence (for review see [50]). Most of what we know about VDAC electrophysiological properties (for reviews, see [51], [52]) was initially

• The NVC response in the diseased

  2021-12-22

  

  The NVC response in the diseased or aging pimaricin may be altered, including changes in both the chemical mediators of NVC, ion channel behaviour, and the dynamics of the vascular system. For example, in Alzheimer’s disease the production of NO is shown to be inhibited (Lourenço et al., 2014), hyp

• The active site of PS

  2021-12-22

  

  The active site of PS1 is located at the interior of its TM horseshoe-like fold (29) (Fig. 1). TM2 and TM6 serve as “doors” for substrate entry (30), as also observed in recent molecular dynamics (MD) simulations of the PS1 subunit (31). Recent coarse-grained (CG) and atomic simulations also showed

• Introduction Initially postulated to represent

  2021-12-22

  

  Introduction Initially postulated to represent the main source of ATP production in eukaryotic cells, mitochondria are recently recognized to perform manifold essential functions beyond energy production, impacting most areas of cell biology and medicine [1]. Mitochondrial metabolism is both the ba

• Tetrazole is one of the most commonly used bioisosteres

  2021-12-22

  

  1-Tetrazole is one of the most commonly used bioisosteres for carboxylic acids arising from their similarity in pKa (ca. 4.5–4.9 vs 4.2–4.4, respectively)., Metabolically, tetrazoles may exhibit an advantage over carboxylic acids because they form -glucuronides which are not as chemically reactive

• The precise mechanism by which erastin inhibits SLC A mediat

  2021-12-22

  

  The precise mechanism by which erastin inhibits SLC7A11-mediated cystine import it still unknown. The initially proposed mechanism, by which erastin binds a related transport protein, SLC7A5, and inhibits SLC7A11 in trans [25], was revised soon after, and it was suggested that erastin inhibits SLC7A

• br Materials and methods br Results br Discussion The COMPAS

  2021-12-21

  

  Materials and methods Results Discussion The COMPASS family of histone methyltransferases exhibits HMT activity towards histone 3 lysine 4 residue with KMT2F and KMT2G being the major H3K4 methylases (Shilatifard, 2006). They play an important role in the formation and progression of leukem

• Pyrrolidinedithiocarbamate ammonium Cells undergoing EMT dis

  2021-12-21

  

  Cells undergoing EMT display a downregulation of E-cadherin and dissociation of their junctional complexes that associates cell-cell contacts with the Pyrrolidinedithiocarbamate ammonium cytoskeleton, known as the adherens junction (Berx and van Roy, 2009, Birchmeier and Behrens, 1994). Adherens ju

• Indeed GSTP mRNA appears to be already highly stable

  2021-12-21

  

  Indeed GSTP1-1 mRNA appears to be already highly stable in K562 leukemia Oleamide receptor with a half-live of more then 40h which is even further increasing to 92h after hemin treatment and erythroid differentiation. Previous reports quantified GST mRNA half-lives which depend on the cellular model

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