Abstract：
:The screening of bioactive compound libraries can be an effective approach for repositioning FDA-approved drugs or discovering new treatments for human diseases. Previous studies have reported polyphosphate (PolyP)-mediated vascular inflammatory responses such as disruption of vascular integrity. Dabrafenib is a B-Raf inhibitor and initially used for the treatment of metastatic melanoma therapy. This study illustrates drug repositioning with dabrafenib (DAB) for the modulation of PolyP-mediated vascular inflammatory responses in human umbilical vein endothelial cells (HUVECs) and mice. The survival rates, septic biomarker levels, behavior of human neutrophils, and vascular permeability were determined in PolyP-activated HUVECs and mice. Dabrafenib suppressed the PolyP-mediated vascular barrier permeability, upregulation of inflammatory biomarkers, adhesion/migration of leukocytes, and activation and/or production of nuclear factor-κB, tumor necrosis factor-α, and interleukin-6. Furthermore, dabrafenib demonstrated protective effects on PolyP-mediated lethal death and the levels of the related septic biomarkers. Therefore, these results indicated the therapeutic potential of dabrafenib on various systemic inflammatory diseases, such as sepsis or septic shock.
journal_name
Chem Biol Interactjournal_title
Chemico-biological interactionsauthors
Lee S,Ku SK,Bae JSdoi
10.1016/j.cbi.2016.07.024subject
Has Abstractpub_date
2016-08-25 00:00:00pages
266-73eissn
0009-2797issn
1872-7786pii
S0009-2797(16)30298-8journal_volume
256pub_type
杂志文章abstract：:The feasibility of an oxygen-independent mechanism of chloroform bioactivation was indicated by the covalent binding to lipid and protein occurring in anaerobic incubations of CHCl3 and microsomes in the presence of NADPH. Under these conditions, the loss of cytochrome P-450 and the inhibition of related monoxygenases...
journal_title：Chemico-biological interactions
pub_type： 杂志文章
doi：10.1016/s0009-2797(86)80063-1
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abstract：:The cytochrome P450 expression profile was determined in the MCF10A human breast epithelial cell line, as was the ability of this cell line to catalyze the bioactivation of the cooked food mutagen, 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine (PhIP). Using non-quantitative reverse transcription-polymerase chain rea...
journal_title：Chemico-biological interactions
pub_type： 杂志文章
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journal_title：Chemico-biological interactions
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journal_title：Chemico-biological interactions
pub_type： 杂志文章
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journal_title：Chemico-biological interactions
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journal_title：Chemico-biological interactions
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journal_title：Chemico-biological interactions
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journal_title：Chemico-biological interactions
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journal_title：Chemico-biological interactions
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doi：10.1016/j.cbi.2009.07.009
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journal_title：Chemico-biological interactions
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journal_title：Chemico-biological interactions
pub_type： 杂志文章
doi：10.1016/j.cbi.2006.12.007
更新日期：2007-02-20 00:00:00
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journal_title：Chemico-biological interactions
pub_type： 杂志文章
doi：10.1016/j.cbi.2015.09.013
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journal_title：Chemico-biological interactions
pub_type： 杂志文章
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journal_title：Chemico-biological interactions
pub_type： 杂志文章
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更新日期：2016-11-25 00:00:00
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journal_title：Chemico-biological interactions
pub_type： 杂志文章
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journal_title：Chemico-biological interactions
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journal_title：Chemico-biological interactions
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journal_title：Chemico-biological interactions
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journal_title：Chemico-biological interactions
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journal_title：Chemico-biological interactions
pub_type： 杂志文章
doi：10.1016/j.cbi.2017.06.007
更新日期：2017-08-01 00:00:00
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journal_title：Chemico-biological interactions
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doi：10.1016/j.cbi.2018.01.007
更新日期：2018-02-25 00:00:00
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journal_title：Chemico-biological interactions
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更新日期：2009-05-15 00:00:00
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journal_title：Chemico-biological interactions
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journal_title：Chemico-biological interactions
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更新日期：2019-04-01 00:00:00
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journal_title：Chemico-biological interactions
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doi：10.1016/j.cbi.2003.12.006
更新日期：2004-03-15 00:00:00
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journal_title：Chemico-biological interactions
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更新日期：2016-11-25 00:00:00
abstract：:The alkylation of hemoglobin is a proposed dose monitor for chemical carcinogens and mutagens. The binding of fifteen chemical carcinogens and mutagens to rat hemoglobin was determined. Direct acting carcinogens and indirect acting carcinogens including aromatic amines, halogenated hydrocarbons, nitrosamines, polycycl...
journal_title：Chemico-biological interactions
pub_type： 杂志文章
doi：10.1016/0009-2797(81)90048-x
更新日期：1981-01-01 00:00:00
abstract：:HPV infections in the oral cavity that progress to cancer are on the increase in the USA. Model systems to study co-factors for progression of these infections are lacking as HPVs are species-restricted and cannot grow in preclinical animal models. We have recently developed a mouse papillomavirus (MmuPV1) oral mucosa...
journal_title：Chemico-biological interactions
pub_type： 杂志文章
doi：10.1016/j.cbi.2020.109321
更新日期：2021-01-05 00:00:00
