• Over expression of Glo can suppress inflammatory responses M

  2021-10-15

  

  Over-expression of Glo-1 can suppress inflammatory responses. Methylglyoxal mediates vascular inflammation in human endothelial NS 1619 [33], indicating that Glo-1 may attenuate inflammation via eliminating methylglyoxal. Glo-1 knockdown mediated methylglyoxal accumulation provokes collagen expressi

• br Introduction The glucagon receptor

  2021-10-15

  

  Introduction The glucagon receptor (GCGR) is a G-protein-coupled receptor expressed mainly in the liver and kidney. Upon glucagon binding, it activates the stimulatory G protein (Gs) and increases cAMP level, subsequently transducing glucagon signaling involved in glucose, amino acids and lipid m

• Besides the described effects on gross locomotor function im

  2021-10-15

  

  Besides the described effects on gross locomotor function, impairment of visuo-motor coordination and fine-motor skills like resting tremors, bradykinesia and rigidity were also investigated, reflecting on the symptomatology of Parkinson's disease in humans (Inzelberg et al., 2008). Preclinically, t

• Here we used a designer receptors activated

  2021-10-15

  

  Here, we used a designer receptors activated exclusively by designer drugs (DREADD)-based chemogenetic approach in a novel Ghsr-IRES-Cre knock-in mouse line to test whether the activity of MBH GHSR neurons is required for the normal rebound food intake following fasting. We also used the Ghsr-IRES-C

• Ligand selectivity may directly be related to the

  2021-10-14

  

  Ligand selectivity may directly be related to the conformational landscape explored by GPCRs despite that most GPCRs do not require dimerization for ligand recognition (Mary et al., 2012). Monomer FPRs have traditionally been perceived as receptors that can recognize N-formyl peptides and LXA4. This

• ADAM has two alternative splicing forms a

  2021-10-14

  

  ADAM12 has two alternative splicing forms, a membrane-anchored long form (ADAM12-L) and a secreted short form (ADAM12-S). Both the long and short forms have metalloproteinase, disintegrin, cysteine-rich, and epidermal growth factor-like domains and can shed pro-heparin binding-epidermal growth facto

• The ETA receptor has a higher affinity for endothelin than

  2021-10-14

  

  The ETA receptor has a higher affinity for endothelin-1 than the two other agonists, with an affinity order of endothelin-1>endothelin-2>endothelin-3, while the ETB receptor exhibits similar affinities for all three isopeptides (Arai et al., 1990b, Sakurai et al., 1990). Earlier studies of the selec

• Histamine functions as a key neurotransmitter in multiple

  2021-10-14

  

  Histamine functions as a key neurotransmitter in multiple circuits to control various behaviors. In Drosophila photoreceptor, histamine is produced de novo by histidine decarboxylase (Burg et al., 1993); meanwhile, maintaining normal histamine content also depends on the histamine recycling pathway

• OS has a key role in the

  2021-10-14

  

  OS has a key role in the pathogenesis of micro- and macrovascular diabetic complications [3]. There is now convincing evidence that the enzymes that generate ROS and gasotransmitters, such as nitric oxide (NO) and CO, are redox regulated at both the transcription and activity levels, and are also im

• Interestingly in vivo infusion and uptake of Ang II in

  2021-10-14

  

  Interestingly, in vivo infusion and uptake of Ang II in intact mice indicated that multiligand endocytic receptor megalin has at least some role in the uptake of Ang II and the downstream signaling process in proximal tubule acpt (PTCs) in vivo [173]. Earlier in vivo studies showed that PTCs of the

• The vessel wall protein collagen which becomes exposed to

  2021-10-14

  

  The vessel wall protein collagen, which becomes exposed to circulating platelets after vascular injuries, is a very strong platelet agonist. It stimulates all relevant platelet activation steps predominantly via the GPVI/FcRγ-chain receptor complex through an immunoreceptor tyrosine-based activation

• TG-101348 CF patients can suffer from a multitude of hepatob

  2021-10-14

  

  CF patients can suffer from a multitude of hepatobiliary problems including gall stones, hepatitis, steatosis and cirrhosis. Hepatobiliary problems are common in pediatric CF patients with reported prevalence rates up to 25% [12,13]. Cystic fibrosis related liver disease (CFLD) was thought to devel

• LbGlcK and the HsHxKIV d glucose

  2021-10-14

  

  LbGlcK and the HsHxKIV-d-glucose complex (PDB entry 3IDH) [17] were superimposed from individual subunits. The active site regions revealed the key Busulfan binding residues to be present for LbGlcK; also, the superposition showed that HsHxKIV had residues that were absent in LbGlcK, such as K169 a

• The rationale for developing HDACi as anticancer agents was

  2021-10-13

  

  The rationale for developing HDACi as anticancer agents was based on their ability to induce the hyperacetylation of histones and nonhistone proteins, resulting in increased differentiation, apoptosis, and PRT062070 synthesis arrest of cancer cells 1, 2, 3. HDACi have been used in the treatment of

• As comparators compounds and were made

  2021-10-13

  

  As comparators, compounds and were made using the pyrazolopyridine core with the CF triazole attached. The 2-fluorophenyl group was replaced with the methylpyrimidine in compound . The potency of these compounds were very good and compound looks attractive from a physicochemical perspective as it

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