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Finasteride has been shown to be a mechanism based inhibitor
2024-12-23
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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However cancer and fibrotic diseases are
2024-12-23
However, cancer and fibrotic diseases are the most extensively studied disease states. ATX is connected to various cancers because it can stimulate chemokinesis and chemotaxis in melanoma cells. Upregulated ATX Rhodamine B labeling has been reported in breast cancer,, prostate cancer, thyroid canc
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To identify the kinase s mediating H S phosphorylation
2024-12-23
To identify the kinase(s) mediating H3.3S31 phosphorylation, we devised a 96-well-plate-compatible immunostaining assay, with TNP-ATP triethylammonium salt synthesis specific for H3.3S31ph, and utilized it to screen both a Qiagen siRNA library covering 720 human kinases and a kinase inhibitor libra
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In response to DSB the lesion recognition factor Mre
2024-12-23
In response to DSB, the lesion recognition factor Mre11-Rad50-Nbs1 (MRN) complex helps the recruitment of ATM to the damage site and its activation by phosphorylation [29]. However, whether UV-damage recognition factors directly influence ATR and ATM recruitment and their phosphorylation is not clea
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br Concluding remarks It is clear that a disordered l
2024-12-23
Concluding remarks It is clear that a disordered l-arginine homeostasis by changes in arginase, NOS and ADMA activity and expression, is not only vital in the chronic airway diseases, lipoxygenase inhibitor and COPD, but also seems to play an important role in many co-morbidities. Unknown, howev
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At Johns Hopkins Aramco Health
2024-12-23
At Johns Hopkins Aramco Health (JHAH), we started an ASP in 2011 with an educational program of physicians and pharmacist. The program was enhanced mid-2012 with the following interventions: a re-designed antibiotic sensitivity report [2], intravenous to oral conversion program, vancomycin pharmacok
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Recent genome wide association studies have indicated
2024-12-21
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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Aberrant or a sustained activation
2024-12-21
Aberrant or a sustained activation of AhR signaling pathway, triggered by exogenous toxic ligands such as dioxins, PAHs or polychlorinated biphenyls (PCBs), is a well-described biological process engaged during tumor initiation and/or promotion in various tissues (e.g. liver, lung, skin)(reviewed in
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br Conclusions Triptans are HT B D F receptors
2024-12-21
Conclusions Triptans are 5-HT1B/1D/(1F) receptors agonists and are considered as the gold standard for acute migraine treatment that have been proven effective. Unfortunately, they are contraindicated in patients with cardiovascular diseases due to their vasoconstrictor (side) effects (MaassenVan
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As noted earlier the PfkB
2024-12-21
As noted earlier, the PfkB family of carbohydrate kinases can phosphorylate the hydroxymethyl group of a wide variety of sugar moieties [1], [3]. Recent searches of the Swiss-Prot database with the two conserved sequence motifs found in these proteins (Accession nos. PS00583 and PS00584) identified
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DiscoveryProbe™ Inhibitor Library Compounds were profiled fo
2024-12-21
Compounds – were profiled for their inhibitory activity against dipeptidyl peptidase-IV Activity and/or Structure Homologues (DASH) [e.g. DPP2, DPP8 and DPP9] and non-DASH [eg. post-proline cleaving enzyme (PPCE), neutral endopeptidase (NEP), aminopeptidase P (APP), aminopeptidase N (APN)] enzymes.
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In this review we will present the traditional
2024-12-20
In this review, we will present the traditional and actual strategies to study orphan receptors and identify their ligands. An extensive description of the orphan GPCR field has been published in 2013 by Davenport et al. [22]. Therefore, we will focus on the deorphanizations that were reported since
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Apoptosis signal regulating kinase ASK also referred
2024-12-20
Apoptosis signal-regulating kinase 1 (ASK1, also referred to as MAP3K5)(Ichijo et al., 1997) participates in many different stress responses, including apoptosis (Chang et al., 1998, Chen et al., 1999, Ichijo et al., 1997, Kanamoto et al., 2000, Noguchi et al., 2008, Saitoh et al., 1998, Tobiume et
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It is now well established that the cumulative exposure to
2024-12-20
It is now well established that the cumulative exposure to endogenous estrogens throughout a woman's life, mainly due to her reproductive history, has an impact on the risk of hormone-dependent breast cancer (Lambertini et al., 2016). Prolonged exposure to estrogens in the case of early age at menar
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br Activity and expression of aromatase in the
2024-12-20
Activity and expression of aromatase in the hippocampus The brain, like the adrenals, gonads and the placenta, is a steroidogenic organ. This paradigm emerged from studies carried out as early as the 1980s by Baulieu and co-workers; these studies showed that steroids such as pregnenolone and dehy
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