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br Funding br Introduction l Dihydroxyphenylalanine l
2024-03-05
Funding Introduction l-3,4-Dihydroxyphenylalanine (l-DOPA) is the gold-standard treatment for the motor symptoms of Parkinson's disease (PD); however, its chronic use induces severe motor complications that eventually limit its long-term efficacy (Bastide et al., 2015). The most disabling side
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Finasteride has been shown to be a mechanism
2024-03-05
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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br Breast cancer The interactions between LOX and
2024-03-05
Breast cancer The interactions between 15-LOX and COX enzymes also affect the outcome of breast cancer. Indomethacin, a COX-1 and COX-2 inhibitor, decreased the growth of human breast cancer (BC) cells in nude mice, as well as slowed the rate of lung metastasis formation [41]. The levels of 12-HE
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Introduction Cytochrome P CYP aromatase catalyzes the conver
2024-03-05
Introduction Cytochrome P450 19 (CYP19; aromatase) catalyzes the conversion of androgens to estrogens in a three-reaction sequence, where each step depends on NADPH and O2 [[1], [2], [3]]. The first two steps are accepted to be hydroxylations of the steroid C19 methyl group, whereas the final step
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Plant pathogenic fungi have caused a lot of economic losses
2024-03-05
Plant pathogenic fungi have caused a lot of economic losses to agricultural production worldwide every year. It is necessary to develop an bio-sourced antifungal agent for agricultural use. Many researches have shown that the antifungal activity of quaternized chitosan derivatives is mainly affected
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br Materials and methods br Results br Discussion
2024-03-05
Materials and methods Results Discussion We demonstrate reduced angiogenic activity in NDRG1 overexpressing malignant glioma leading to reduced glioma growth. This antiangiogenic phenotype is paralleled by a significant upregulation of the antiangiogenic gene TNFSF15. TNFSF15 upregulation i
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Evidence from basic science studies suggests that Cd
2024-03-05
Evidence from basic science studies suggests that Cd may play a role in prostate cancer through disruption of the androgen receptor (AR). AR, a hormone-activated transcription factor, is the key driver of prostate cancer progression [6]. Ironically, the AR is also required for normal prostate growth
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br Distribution of OCT in rat brain
2024-03-04
Distribution of OCT3 in rat brain To understand the potential roles of this corticosterone-sensitive monoamine clearance mechanism in the regulation of monoaminergic neurotransmission and behavior, and its potential contribution to corticosteroid actions on behavior, we examined the rostrocaudal
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Corticosterone induced inhibition of OCT mediated transport
2024-03-04
Corticosterone-induced inhibition of OCT-mediated transport is rapid and appears to involve direct interaction of the steroid with the transporter at a specific site. Volk et al. (2003) studied OCT2-mediated transport by measuring substrate-induced currents using patch clamp of Xenopus oocytes exoge
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br Author contributions br Acknowledgements We thank
2024-03-04
Author contributions Acknowledgements We thank Dr. Bob Hammer and the Transgenic Core Facility at UTSW for the generation of the transgenic lines, John Shelton and the Histology Core for assistance with histology and the UTSW Metabolic Core Unit for help in phenotyping. We acknowledge support
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Having established the structural requirements
2024-03-04
Having established the structural requirements for potency in both the biochemical and biomarker (CRA) assays, we evaluated key compounds in the metabolic stability assay. Disappointingly, we found that all compounds had high intrinsic clearances in mouse microsomes. To ascertain whether the in vitr
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br Disclosure br Acknowledgments br Introduction Deeper unde
2024-03-02
Disclosure Acknowledgments Introduction Deeper understanding of the pathobiology of non-small cell lung cancer (NSCLC) has led to the development of small p450 inhibitors that target genetic mutations known to play critical roles in the progression to metastatic disease. Mutations in epide
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The overall adjustment the non toxicity and the addiction
2024-03-02
The overall adjustment, the non-toxicity and the addiction-free treatment methods are the advantages of EA. EA treatment for depression has achieved great clinical effect in recent years (Dong et al., 2017). The clinical practice guideline of the American college of physicians (ACP) have pointed out
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NOXA a BH only protein is
2024-03-02
NOXA, a BH3-only protein, is best known as a selective inhibitor of MCL-1, which is a highly expressed pro-survival protein in many human malignancies [30]. In addition, NOXA was recently proven to act as a direct activator via directly binding to BAX to induce apoptosis [31]. Given that its levels
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Compound was docked into the active site of
2024-03-02
Compound was docked into the active site of Aurora B kinase using Tripos sybyl-X ver. 2.1.1. The crystal structure of human Aurora B kinase cocrystallized with its potent inhibitor VX-680 was used for the docking analysis (PDB ID: ). The most likely binding conformations were selected based on the d
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