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Molecular docking simulations were carried out
2024-10-11
Molecular docking simulations were carried out for ligands – in the ACE crystal structure (1O86) and DPP4 crystal structure (2G5P). Comparison of the binding mode of – () with enalaprilat (a) in ACE shows that the phenethyl group (–, enalaprilat) occupies the S1 pocket and the adjacent carboxylic ni
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Whereas more research is needed to identify the precise
2024-10-11
Whereas more research is needed to identify the precise mechanism by which FIN exerts its antidyskinetic effect, the calcein am that it can negatively modulate dopaminergic transmission is also supported by our previous findings. Indeed, we have previously shown that FIN completely reversed the beh
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rolipram Song et al reported series of
2024-10-11
Song et al. reported series of 1,2,3-triazolylsalicylamide derivatives and screened over kinase panel and found compound 31 as most potent which inhibited Aurora-A, specifically with IC50 of 0.37 μM. Compound 31 was about 10-fold more active for Aurora-A than for Aurora-B (IC50 = 3.58 μM reported se
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Because the V ATPase inhibitors that have
2024-10-11
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
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In Rainey et al published the results of a targeted
2024-10-10
In 2008, Rainey et al. published the results of a targeted compound library screen for potential inhibitors of the ATM kinase. In this study, the compound CP466722 was identified as a highly selective and rapidly reversible ATM inhibitor, which did not inhibit PI3K or related PIKK family members. Mo
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Previous studies have indicated that maximal
2024-10-10
Previous studies have indicated that maximal IL-8 protein hmg-coa reductase requires NF-κB activation as well as the activation of the MAP kinases ERK, JNK, and p38 (Li et al., 2002). In our study, NF-κB inhibitor can reduce the up-regulated IL-8 production by PRRSV infection, indicating that PRRSV
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However one should keep in mind that these results
2024-10-10
However, one should keep in mind that these results may not reflect exactly in vivo antioxidant activity. Many other issues such as absorption, metabolism and physicochemical properties of different antioxidants must also be considered (Prior et al., 2007, Wu et al., 2004). Some research groups are
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The primary structure of the A
2024-10-10
The primary structure of the Aβ peptide can be divided into four regions based on hydrophobicity. The N-terminal residues 1–16 comprise the first hydrophilic region, which also contains the metal binding site. More specifically, side chain carboxylate of D1 and the side chain nitrogens of H6, H13 an
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PGC mediated mitochondrial biogenesis in brown fat
2024-10-10
PGC-1α-mediated mitochondrial biogenesis in brown fat and endothelial Torin1 sale is in part regulated by eNOS and NO [28], [29]. Recent studies indicate that H2S not only augments NO bioavailability and signaling [11], [17], but provides protection against cardiac injury in an eNOS-dependent manne
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Pentamidine br Conflicts of interest br Newly Identified Mec
2024-10-10
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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A highly attenuated B pertussis strain named BPZE has
2024-10-10
A highly attenuated B. pertussis strain, named BPZE1, has recently been described [10]. It produces enzymatically inactive pertussis toxin (PT), no dermonecrotic toxin and only trace amounts of tracheal cytotoxin. Markedly reduced lung pathology was observed in mice intranasally (i.n.) infected with
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br Conflict of interest br Acknowledgements The authors woul
2024-10-10
Conflict of interest Acknowledgements The authors would like to thank Mrs. Amparo Pacheco from CMPL, PUC, for her technical and secretarial assistance. This work was supported by the Fondo Nacional de Desarrollo Científico y Tecnológico (FONDECYT 1150344, 1050377, 11150083), and the Direccioń
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Our initial approach to identify hits was two pronged
2024-10-09
Our initial approach to identify hits was two-pronged and included a high-throughput screening (HTS) campaign of the OSI MDL800 synthesis library as well as a virtual screening (VS) campaign, utilizing a publically available crystal structure of ACK1 (PDB code: ). A tolerance for protein flexibilit
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br Materials and methods br Results
2024-10-09
Materials and methods Results Discussions Our results indicated that autophagy was suppressed in GECs under HAGG treatment, through Akt/mTOR-dependent pathways. Previous reports provided clues for the linkages between ICs and endothelial cell autophagy. Fujii and colleagues reported that se
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rho kinase inhibitor The combination of Aurora kinase
2024-10-09
The combination of Aurora kinase inhibitors with standard chemotherapeutics or radiotherapeutics are currently in progress, such as AZD1152 plus radiotherapy in various solid cancer models. In addition, Azzariti et al. found that AZD1152-HQPA enhanced oxaliplatin and gemcitabine effectiveness in the
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