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MAPs require divalent transition metal
2024-12-25
MAPs require divalent transition metal ions as cofactors for activity [21]. Previous studies on MAPs from different organisms indicate cobalt ions to be the most preferred divalent metal activator [22]. However, MAPs also exhibit activity with other divalent cations like Mn(II), Ca(II), Ni(II) or Fe
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Recent genome wide association studies have indicated SORL a
2024-12-25
Recent genome-wide association studies have indicated SORL1 as a risk factor for AD (Meng et al., 2007, Rogaeva et al., 2007, Wen et al., 2013). SORL1, is expressed in neurons (Yin et al., 2015) and also regulates APP traffic from the cell membrane to the Golgi apparatus. A reduction in its expressi
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Further evidence for action mechanism was
2024-12-25
Further evidence for action mechanism was provided by assays using [3H]nisoxetine, a selective NET inhibitor used as standard radioligand for competitive binding experiments. The results showed dose-dependent blocking of [3H]nisoxetine binding by both xylazine and dexmedetomidine. Nisoxetine binds t
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Given the profound expression of HT A and HT
2024-12-25
Given the profound WEHI-539 hydrochloride of 5-HT1A and 5-HT2A in the hippocampal CA1 region, and their potential to complex with mGluRs, the objective of this study was to examine if sleep deprivation alters the expression of 5-HT1A and 5-HT2A receptors and determine whether potential changes are r
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Does dietary caffeine interfere with antinociception by othe
2024-12-25
(8) Does dietary caffeine interfere with antinociception by other modalities that alter pain (TENS, exercise, joint mobilization, water immersion therapy)? Caffeine and/or A1R antagonists inhibit antinociception by each of these modalities in preclinical studies, such that there is potential for int
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where is the breaking force
2024-12-25
where is the breaking force. In the following, the details of the simulation are presented and subsequently, the results are discussed. The initial atomic structure is extracted from the crystal structure of single AF (PDB identification 3G37) which consist 12 monomers. As aforementioned 4 monomer
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Toxicity is the main reason for the
2024-12-25
Toxicity is the main reason for the failure at all stages of the new drug development process. The major part of safety-related attrition occurs at preclinical phases while predicting preclinical safety liabilities earlier in the drug development process. This strategy enables the design and/or sele
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It has been recognized for decades that
2024-12-25
It has been recognized for decades that neurons in the mammalian central nervous system may release both a fast-acting, typically amino acid derived neurotransmitter such as glutamate or GABA, and a second peptidergic neuromodulatory molecule such as neuropeptide Y, substance P, or cholecystokinin.
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In an effort to determine if one ARI was
2024-12-25
In an effort to determine if one 5ARI was more effective than the other, the Enlarged Prostate International Comparator Study (EPICS) [17] compared treatment with finasteride and dutasteride in 1630 men over the age of 50 and concluded that after one year of treatment, both groups had statistically
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Since the localization of LO
2024-12-25
Since the localization of 5-LO depends on phosphorylation, we also analyzed the phosphorylation profile of 5-LO-WT and all isoforms by Western blot using specific po1 against the phosphorylation sites S271 and S523. Whereas phosphorylation at S271 activates the 5-LO, inhibits nuclear export and lea
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A rational approach for the
2024-12-25
A rational approach for the design of new steroid compounds as possible competitive inhibitors of CYP17 include chemical modification at C17 of the enzyme's natural substrates, pregnenolone (1) and progesterone (2), introducing groups with moderate to strong dipole properties at C20, such as oxime a
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In this paper we describe the formation of a
2024-12-25
In this paper, we describe the formation of a structure-based pharmacophore which lead to the discovery of several hydrophobic, yet non-lipid inhibitors of ATX. These compounds docked within the same volume occupied by the initial non-lipid inhibitors of ATX used to build the pharmacophore. Violatio
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We conducted the largest drug screen to
2024-12-25
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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br Materials and methods br Results
2024-12-25
Materials and methods Results and discussion In our previous studies (Matarneh et al., 2017), mitochondria were mechanically disrupted and separated into supernatant and pellet fractions by centrifugation. The causative agent for enhnced glycolytic flux was shown to be a protein that resides i
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Production of reactive oxygen species ROS during
2024-12-24
Production of reactive oxygen species (ROS) during RSV infection is one the important ways that neutrophils can injure the lungs [2], [24], [25]. Lipoxygenases are considered as an important source of producing ROS inside the cl 2 [26]. Several studies have indicated that the 12/15-LOX is a pro-inf
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