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Some of the earliest LOX inhibitors were redox inhibitors
2025-02-11
Some of the earliest 12-LOX inhibitors were redox inhibitors, including nordihydroguaiaretic GLP-2 (rat) (NDGA), BW 755C, and baicalein 48, 49, 50. Redox inhibitors block the oxidation of the nonheme iron at the cataylytic site, preventing its conversion from the inactive (Fe2+) to the active (Fe3+
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The specific mechanisms underlying glutamine
2025-02-11
The specific mechanisms underlying glutamine dependency are still being explored, and current research indicates that the mechanisms likely vary between breast cancer subtypes. In HER2-positive breast cancer, increased levels of the transcriptional activator PGC-1α lead to expression of genes that m
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Moreover mice exposed to high cholesterol diet have mildly a
2025-02-11
Moreover, mice exposed to high-cholesterol diet have mildly activated astrocytes, increased expression of ApoE and aquaporin-4 in the hippocampus, and altered levels of proteins associated with Aβ metabolism (Chen et al., 2016), which is related to a higher demand for cholesterol transport and the n
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br Hypoadiponectinemia in metabolic syndrome APN belongs str
2025-02-10
Hypoadiponectinemia in metabolic syndrome APN belongs structurally to the complement 1q family and is found at high concentrations (>0.01% of total protein) in the serum of healthy individuals [6]. Given the abundance of APN in plasma, it is assumed that alterations in plasma levels of APN might
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Derivatives of M that possess either an alkyne or
2025-02-10
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 WY-14643 to maintain 5-HTR antagonist properties as (+)-M100907 was demonstrate
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Polydatin Synthesis pharmacological evaluation for the bindi
2025-02-10
Synthesis, pharmacological evaluation for the binding at hA, hA and hA ARs, and efficacy at hA subtype of the synthesized compounds, together with the assessment of their theoretical ADME properties were the guidelines in this preliminary drug discovery investigation. The synthetic pathways which y
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The theoretical calculations of ADME parameters molecular we
2025-02-10
The theoretical calculations of ADME parameters (molecular weight (MW), log P, topological polar surface are (tPSA), number of hydrogen donors (nON) and acceptors (nOHNH), and volume) and DLS are presented in along with the violations of Lipinski’s rule. According to these data, all compounds (–) c
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During years research efforts at
2025-02-10
During 2002–2004years research efforts at Los Alamos National Laboratory (LANL) focused on constructing a quantum computer based on regular arrays build from neutral radical molecules possessing one single unpaired 5,7-dihydroxychromone spin. The idea was built on the ability to manipulate individua
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In vitro studies with soman inhibited non aged AChE revealed
2025-02-10
In vitro studies with soman-inhibited, non-aged AChE revealed a species dependent reactivating potency of HI-6 and MMB-4. With guinea pig AChE second order reactivation rate constants of 0.051 and 0.038mM−1min−1 were determined for HI-6 and MMB-4, respectively (Luo et al., 2007). Corresponding value
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The inhibition of the exacerbated
2025-02-10
The inhibition of the exacerbated inflammatory response that follows injury may be an alternative approach to induce a more efficient repair [17,83]. In line with that, 5-LO is one of the most consolidated targets for dampening inflammation, mainly through the therapeutic effects of 5-LO inhibitors
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Despite the growing knowledge surrounding the link between A
2025-02-10
Despite the growing knowledge surrounding the link between ATX and cholestatic pruritus in PBC, it remains unclear if the role of the ATX-LPA signaling axis includes lymphocytes homing in the liver of PBC, and if the resulting inflammation is associated with PBC pruritus (Fig. 3). PBC is characteriz
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primaquine phosphate In conclusions MPE effects in causing l
2025-02-10
In conclusions, MPE effects in causing lesser increase in vaginal fluid pH could partly restore the vaginal acidity in sex-steroid deficient state. MPE could exert its effect via enhancing both H+ generation as well as H+extrusion into the vaginal lumen. Although gallic primaquine phosphate is the
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Lysosome exocytosis inhibitor The R pycnus arginase was iden
2025-02-10
The R. pycnus arginase was 65% identical to the published B. caldovelox arginase sequence (AAB06939). Furthermore, the R. pycnus arginase gene was 62%, 45%, 36% and 22% identical to the published arginase sequences from Bacillus thuringiensis (AJI37018), Thermus thermophiles (WP_038039155), Human ar
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Researchers demonstrated that mitochondria are the main prod
2025-02-10
Researchers demonstrated that mitochondria are the main producers of ROS and are the most sensitive to the effects of ROS. Mitochondria-mediated apoptosis may not be limited to the role of cytochrome c in the activation of caspase-3 and ROS may provide an alternate mitochondrial signaling pathway (H
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br Introduction O Dowd et
2025-02-10
Introduction O’Dowd et al. identified a gene very similar to angiotensin type-1 receptor in 1993 (O’Dowd et al., 1993). The specific selective ligand of this receptor called APJ receptor was determined by Tatemoto et al. in 1998 as apelin (Tatemoto et al., 1998). The high expression of apelin and
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