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ACE inhibition is often thought to play a central role
2024-06-26

ACE inhibition is often thought to play a central role in the mechanisms of blood pressure reduction in vivo, and most ACE inhibitory (ACEi) peptides were characterized based on in vitro ACE inhibition. A relationship between in vitro ACE inhibition and antihypertensive activity, however, is not app
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Docking studies were performed on the selected
2024-06-26

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
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In addition to pH regulation by ion counter fluxes
2024-06-26

In addition to pH regulation by ion (counter-) fluxes, acidification is regulated by the abundance of V-ATPase on organelles, by the pumping activity of the complex and by proton leakage. In yeast, the V-ATPase VO subunit a is the only subunit expressed in two isoforms termed Stv1p and Vph1p. V-ATPa
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APJ receptor expression is altered in various
2024-06-26

APJ receptor expression is altered in various cardiovascular diseases, and both increases as well as decreases in APJ receptor expression have been reported. A decrease in mRNA and protein levels of APJ receptors was observed in patients with ischemic heart disease or idiopathic dilated cardiomyopat
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To investigate if WP increased CAT
2024-06-26

To investigate if WP increased CAT activity in cells, C2C12 muscle Penicillin G Sodium were treated with 0.1 to 0.4 mg/mL of WP (80.05% protein) for 24 h and then stressed with 0.75 mM H2O2 for 1 h (Xu et al., 2011). The CAT activity was significantly enhanced from 15.1 ± 0.7 to 23.7 ± 1.3 U/mg of
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The PDZ domains of DLG interact with
2024-06-26

The PDZ domains of DLG interact with tumor suppressor proteins, APC and PTEN, as well as with several viral oncoproteins such as the E6 protein present in oncogenic human papillomavirus (reviewed in [177]). It has been reported that overexpression of DLG in fibroblasts impairs the events in the G0/G
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br The lipoxygenase pathway in
2024-06-25

The 12/15-lipoxygenase pathway in vascular physiology and pathology The mammalian 12- and 15-LOXs have high substrate specificity oxidizing predominantly ω−6 (arachidonic and linoleic acids) but also the ω−3 (docosahexanoic) pdk 1 [86], [87], [88]. Different LOXs oxidize fatty acids both in the
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The fat body is one of the
2024-06-25

The fat body is one of the largest tissues of Bombyx mori, with components including fat, glycogen, protein and vitamins. The fat body exhibits important physiological functions, not only storing a large number of nutrients but also serving as an important site of biosynthesis and metabolism (Arrese
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In conclusion we have shown that mGlu receptors negatively r
2024-06-25

In conclusion, we have shown that mGlu7 receptors negatively regulate α1-adrenergic receptor signalling in heterologous expression systems, chemokine receptor antagonist tissue and living animals. This interaction might represent a protective mechanism aimed at restraining an excessive activation of
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br Conflicts of interest br Newly Identified Mechanisms of
2024-06-25

Conflicts of interest Newly Identified Mechanisms of APN Resistance Hold Therapeutic Potential APN, APN Receptors, and APN Cardiovascular Protection APN Resistance in Cardiovascular Disease The Molecular Mechanisms of APN Resistance Concluding Remarks and Future Directions Finally,
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Since forskolin is known to
2024-06-25

Since forskolin is known to act directly at the catalytic site of adenylate cyclases near the ATP binding (Tesmer et al., 1997), the synergistic and/or permissive effect of gonadotropins on FSK activity must occur at the level of AC itself or very near, at the level of one of its direct partner. The
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Regarding A Rs and A ARs basal conditions generate
2024-06-25

Regarding A1Rs and A2ARs, basal conditions generate a low tone of endogenous adenosine and cause A1R activation, in contrast to situations of increased adenosine where A2AR activation becomes dominant. When adenosine concentrations rise, e.g. during hypoxia, also time appears likely important in reg
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Derivatives of M that possess either an alkyne or an
2024-06-25

Derivatives of (+)-M100907 that possess either an alkyne or an azide have been synthesized. The most active enantiomer was obtained by resolution of a relatively early intermediate in the synthesis. The ability of these PLX-4720 to maintain 5-HTR antagonist properties as (+)-M100907 was demonstrate
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We conducted the largest drug
2024-06-25

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
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CHK has been reported to
2024-06-25

CHK1 has been reported to be the kinase responsible for H3.3S31 phosphorylation in human ALT cancer Oxybutynin . However, in our study, knockdown of CHK1 in HEK293F (Figs. S1c and S6) or HeLa S3 (data not shown) cells did not result in a significant decrease in H3.3S31ph, which is in agreement with
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