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Most of the identified aldose reductase
2024-08-23
Most of the identified aldose reductase inhibitors possess undesirable effects like poor pharmacokinetic properties, hypersensitivity and Steven-Johnson Syndrome [1]. However, the main side effect is the lack of selectivity relative to aldehyde reductase (ALR1, EC 1.1.1.2). ALR1 plays the important
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Our results add to previously published data on
2024-08-23
Our results add to previously published data on the contribution of ALDH3A1 to the optical properties of the cornea. Specifically, the study by Nees et al. (2002) was among the first to examine whether ALDH3A1 serves as a structural component in the cornea and similarly to lens crystallins. Their ex
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These results from the present study are summarized
2024-08-23
These results from the present study are summarized in Table 1. Eight drugs (doxorubicin, epirubicin, daunorubicin, idarubicin, irinotecan, imatinib, sunitinib and gefitinib) inhibited 5-HT-induced 5-HT3A and 5-HT3AB currents; three (irinotecan, topotecan and mitoxantrone) showed different responses
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The total IgG concentration decreased from
2024-08-22
The total IgG concentration decreased from a mean of 997 mg/100 ml before treatment to a mean of 696 after treatment in the MuSK+MG patients, and from a mean of 1736 mg/100 ml to a mean of 802 mg/100 ml in the AChR+MG patients (normal values 723–1685 mg/100 ml). This decrement was also statistically
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Osteocytes the most abundant cells in an adult skeleton
2024-08-22
Osteocytes, the most abundant cells in an adult skeleton, are essentially mature osteoblasts that are surrounded by the products they secreted (Noble and Reeve, 2000). Osteocytes serve as mechanosensors that direct bone remodeling and that regulate the activities of osteoblasts and osteoclasts (Bone
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Molecular docking simulations were carried out for ligands i
2024-08-22
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 Si
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A promising target that is involved in
2024-08-22
A promising target that is involved in the biosynthesis of the precursor LTA4 is the 5-LO-activating protein (FLAP), which in vivo is seemingly indispensable for LT formation [8], [9]. FLAP, a member of the MAPEG family (membrane-associated proteins in eicosanoid and glutathione metabolism), is an i
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Finasteride has been shown to be a mechanism based inhibitor
2024-08-22
Finasteride has been shown to be a mechanism-based inhibitor of 5AR-2 [9]. Finasteride acts as an alternate substrate for 5AR-2 and is initially bound in an extremely stable enzyme-bound NADP-dihydrofinasteride adduct which is ultimately processed to dihydrofinasteride. The NADP-dihydrofinasteride a
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At present the role of autophagy in
2024-08-22
At present, the role of autophagy in neurons remains controversial. Autophagy has homeostatic and waste-recycling functions and plays a protective role in neurodegeneration diseases. Moreover, it has been thought as a programmed cell death participating in the occurrence and development of various d
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Matthew et al synthesized and carried out SAR
2024-08-22
Matthew et al. synthesized and carried out SAR studies of imidazo-[1,2-a]-pyrazine as Aurora kinase inhibitors with enhanced kinase selectivity and found that Amfenac Sodium Monohydrate receptor 39 showed optimal potency on Aurora-A and Aurora-B with IC50 value of 4 nM and 13 nM while on phosphoryla
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The co crystal structure of blebbistatin bound to myosin II
2024-08-22
The co-crystal structure of ()-blebbistatin ()- bound to myosin II (PDB: ) was used to scout for possible favorable interactions with the residues lining the binding pocket. Looking at A, we hypothesized that -oriented hydrophilic moieties (e.g. hydroxymethyl) on C of the blebbistatin scaffold migh
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In our bioinformatics analysis of proteins with increased
2024-08-22
In our bioinformatics analysis of proteins with increased SUMOylation upon treatment with MMC and HU, we found clusters of co-regulated proteins that are known to function together in the RS response. In addition to the ATR activation proteins, BRCA1 and BARD1, we also found Fanconi anemia proteins
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nisoldipine australia Plant tissues were thought to be natur
2024-08-22
Plant tissues were thought to be natural sources containing different types of antioxidant compounds (tocopherols, ascorbic acid, carotenoids, and phenolic compounds). As a general classification, antioxidants were grouped as vitamins (ascorbic acid, tocopherols), carotenoids (condensed tannins, xan
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Consistent with the in vitro results memantine ameliorated A
2024-08-21
Consistent with the in vitro results, memantine ameliorated Aβ-induced cytotoxicity in rat primary cortical cultures. Studies reported that memantine protected neurons against the damage caused by aggregated Aβ40 or Aβ42 oligomers in vivo[26], [27]. These results suggest that, in addition to its neu
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We have recently begun to demonstrate this concept
2024-08-21
We have recently begun to demonstrate this concept by reporting a novel class of β-hairpin peptidomimetics, built on a piperidine-pyrrolidine semi-rigid β-turn inducer [12] and bearing two recognition pentapeptide sequences, designed on oligomeric and fibril structures of Aβ1-42 (compound 1, Fig. 1)
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