• Application of the broad acting HTR antagonist methiothepin

  2023-10-19

  

  Application of the broad-acting 5-HTR antagonist methiothepin (Bard et al., 1996, Hoyer et al., 1994, Peroutka, 1990) converted the TBS-induced response of both thalamocortical and intracortical A1 synapses from LTP to LTD, an effect that was mimicked by the selective 5-HT2R antagonist ketanserin (L

• Moreover showed reduction in fibroblast growth factor induce

  2023-10-19

  

  Moreover, showed 73% reduction in fibroblast growth factor–induced neovascularization in a mouse corneal micropocket assay at a dose of 100mg/kg and 50% reduction at 50mg/kg. Both results were highly statistically significant (P showed activity comparable to the clinically approved tyrosine kinase i

• We conducted the largest drug screen

  2023-10-19

  

  We conducted the largest drug screen to date in HPV-positive cancers and identified Aurora kinase inhibitors as effective and understudied drugs in HNSCC and CESC. These drugs cause apoptosis and cell cycle arrest in vitro and decrease tumor size in vivo. This is the first published study to demonst

• Because the V ATPase inhibitors that

  2023-10-19

  

  Because the V-ATPase inhibitors that have been employed in these studies (including bafilomycin and concanamycin), are membrane permeant, they inhibit all the V-ATPases in the cell. This is important since it is possible that intracellular V-ATPases, in addition to those present at the plasma membra

• br Conflict of interest br

  2023-10-19

  

  Conflict of interest Acknowledgements Introduction The mitogen-activated protein kinase (MAPK) pathway is an important intracellular signaling system that regulates diverse cellular functions, such as proliferation, differentiation, and apoptosis [1]. Apoptosis signal-regulating kinase 1 (A

• br COPD As in asthma

  2023-10-19

  

  COPD As in asthma, also in COPD, increased expression of arginase has been reported, and tobacco smoke may increase expression of arginase in human subjects [46, 47]. Increased ADMA levels have also been reported in COPD, and both the increased expression of arginase and ADMA contribute to remode

• br Material and methods br Results br Discussion The

  2023-10-19

  

  Material and methods Results Discussion The present study demonstrates for the first time that Mino selectively induces apoptosis in Jurkat Clofazimine via an H2O2 signaling-dependent mechanism. Structurally, Mino is composed of a C10 and C12 phenol group, C12a hydroxyl group, and C1 and C1

• The androgen receptor gene AR is located on

  2023-10-18

  

  The androgen receptor gene (AR) is located on the X-chromosome and consists of eight exons in humans (Brown et al., 1989; Kuiper et al., 1989). The similar gene structure in mice, monotremes and marsupials indicates AR is highly conserved in mammals (Choong et al., 1998; Faber et al., 1991; He et al

• RNA interference assays have shown that the inhibition

  2023-10-18

  

  RNA interference assays have shown that the inhibition of AMPK expression leads to increases in TNF-α, IL-6 and cyclooxygenase-2 (COX-2) levels after LPS stimulus, whereas the transfection of macrophages with a constitutively active form of AMPKα1 results in decreased LPS-induced TNF-α and IL-6 prod

• br Material and methods br Results br Discussion

  2023-10-18

  

  Material and methods Results Discussion RSV is a major cause of lower respiratory tract infections in infancy and early childhood. Several observations suggest that immunological mechanisms may be the key to understand the severity of RSV bronchiolitis in infancy. Several laboratories have

• br Material and methods br Results br Discussion Although we

  2023-10-18

  

  Material and methods Results Discussion Although we were not able to detect 12/15-LOX mRNA in the lungs of 12/15-LOX knockout mice substantial amounts of 15-HETE could be detected in BALF. In fact, significant synthesis of 15-HETE in 12/15-LOX mice have been already reported [17]. The redun

• Microbe derived ligands can also activate AHR

  2023-10-18

  

  Microbe-derived ligands can also activate AHR. Malassezia, a commensal yeast in human skin, can metabolize tryptophan into several AHR activating compounds including FICZ and ICZ [59]. Lactobacillus converts tryptophan into indole-3-aldehyde (IAld), which can activate AHR and promote IL-22 productio

• As regards feeding the ability to dissipate surplus

  2023-10-18

  

  As regards feeding, the ability to dissipate surplus energy in the form of heat is beneficial for animals if the protein concentration in the food is low, since it allows them then to meet the adequate protein intake requirement without getting fat. Some of the major dietary activators of the AHR ar

• Docking studies were performed on the

  2023-10-18

  

  Docking studies were performed on the selected compounds to explore their binding patterns and to examine SAR in more detail. The co-crystal structure of ATX in complex with PF-8380 (PDB code: ) was selected for the docking studies due to structural similarity of the most potent compound with PF-838

• Cy3 maleimide (non-sulfonated) The synthesis of compounds in

  2023-10-18

  

  The synthesis of compounds in which the ethyl linker has been modified to the carbamate and urea derivatives , and is shown in . Thus the diamine was reacted with glycolic Cy3 maleimide (non-sulfonated) to give the alcohol followed by Mitsunobu reaction with phthalimide to give . Deprotection with h

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