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Docking studies were performed on
2025-02-26
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-83
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In this report the natural compound deguelin potently and
2025-02-26
In this report, the natural compound deguelin potently and dose-dependently suppressed Aurora B kinase activity in vitro, indicating that this compound is an effective Aurora B inhibitor. The docking study indicated that deguelin was docked into the ATP-binding pocket of Aurora B and formed hydropho
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After infection with Salmonella those bacteria
2025-02-26
After infection with Salmonella those bacteria that are not targeted by autophagy of the complete Salmonella-containing phagosome (see above) but are living freely in the cytosol can be eliminated by xenophagy, that is direct targeting of the ‘naked’ bacteria to the autophagic pathway. The type III
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In this study we found that ACL
2025-02-26
In this study, we found that ACL silencing is sufficient to impair myoblast differentiation and that this effect is accompanied by a decrease in MYOD early in the myogenic process and by a subsequent decline in fast MyHC protein 2-Chlorotrityl Chloride Resin at a later stage of differentiation (Fig
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We wanted to investigate the influence of substituents
2025-02-26
We wanted to investigate the influence of substituents on the pyrazole ring on the activity, but only a few substituted pyrazole-3-carboxylic acids/esters were commercially available in useful amounts at a reasonable price, for example, 4- and 5-nitro-pyrazole-3-carboxylic acid. The preparation of 4
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Crystal structures were obtained of sulfonamide and
2025-02-26
Crystal structures were obtained of sulfonamide 18 and amide 19 as a derivative of amide 36 (Fig. 7A and B). The precise rotameric orientation of amide 36 was of significant interest to understand the compound's interaction with the protein. As it would be difficult to assign the rotomer of 36, the
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Recently competitive inhibitors of arginase have been
2025-02-26
Recently, competitive inhibitors of arginase have been developed which have greater specificity for the enzyme. Initial development of these compounds involved determination of the crystal structure of arginase. Christianson and colleagues found that a binuclear manganese cluster was required for ca
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br Introduction Humans have consumed mushrooms for centuries
2025-02-25
Introduction Humans have consumed mushrooms for centuries because of their high nutrient content and low lipid content, as well as their excellent flavor and texture [1]. Edible mushrooms possess notable medicinal properties and bioactivities, including antitumor, antiviral, antidiabetic, and ant
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Perforation of the surface membrane however is
2025-02-25
Perforation of the surface membrane, however, is not the only mechanism of calcium dysregulation by Aβ at the presynaptic terminals. When in excess, both monomers and oligomers modulate biophysical properties of voltage-activated calcium MPEP Hydrochloride as well as calcium release from the endopl
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bapta In order to postulate its binding mode
2025-02-25
In order to postulate its binding mode in APN, bapta 13v was docked into the active site of APN (PDB code: 2DQM) using Sybyl_X 1.3. As illustrated in Fig. 5A, the catalytic zinc ion of APN was chelated by the hydroxamate moiety of 13v, and the S1, S1′ and S2′ pockets of APN were occupied by the leu
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br Conclusion br Acknowledgement This study was supported
2025-02-25
Conclusion Acknowledgement This study was supported by NIH/NINDSR01 NS036812-16. Introduction Lipoxygenases (LOXs) are a heterogeneous family of enzymes that catalyze the peroxidation of polyunsaturated fatty acids (PUFAs). By oxidizing free PUFAs, they were shown to contribute to the gene
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br Current therapies for metabolic diseases Inborn errors
2025-02-25
Current therapies for metabolic diseases Inborn errors of metabolism caused by deficiency of particular enzymes due to loss of function mutations or deletions have been treated by decreasing the intake of the enzymatic substrate, supplementation with an essential cofactor or vitamin, increasing m
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br Dihydrotestosterone in adult fish and frogs br New
2025-02-25
Dihydrotestosterone in adult fish and frogs New perspectives and next directions Similar to other androgens, DHT can modulate reproductive endpoints in both fish and amphibians. However, predicting the effects of DHT can be challenging, as reproductive homeostasis is dependent upon the balance
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Through activation of the CD GOPC pathway attenuated vaccina
2025-02-24
Through activation of the CD46–GOPC pathway, attenuated/vaccinal MeVs rapidly induce a transient phase of autophagy which then diminishes with no signs of negative regulation and precedes a second autophagy phase related to viral protein synthesis [115]. In sharp contrast, virulent MeVs do not inter
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Many reports have well documented that
2025-02-24
Many reports have well documented that signaling pathways play a pivotal role in controlling longevity. The most studied of these pathways is the IGF-1 pathway [11,12]. A disruption of this pathway has been found to extend longevity in different groups of species starting from Caenorhabditis elegans