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Title

Development of chromanes as novel inhibitors of the uncoupling proteins

AuthorsRial, Eduardo ; Rodríguez-Sánchez, Leonor ; Aller, Patricio ; Guisado, Arancha; González-Barroso, M. Mar ; Gallardo-Vara, Eunate ; Redondo-Horcajo, Mariano ; Castellanos Santamaría, Esther ; Fernández de la Pradilla, Roberto ; Viso, Alma
KeywordsArsenic trioxide
chemotherapeutic agents
chromane derivatives
chromanes
findings open
HT-29 cells
HT-29 human carcinoma cell
lower superoxide levels
Members
modulate
potential UCP1 regulators
protective role
proton conductance
tumor cells
UCP family
UCPs
uncoupling proteins
Issue Date25-Feb-2011
PublisherElsevier
CitationChemistry & Biology 18(2):264-274(2011)
AbstractThe uncoupling proteins (UCPs) are mitochondrial carriers that modulate the energetic efficiency and, as a result, can lower superoxide levels. Here, we describe the discovery of a small-molecule inhibitor of the UCPs. Screening of potential UCP1 regulators led to the identification of chromane derivatives that inhibit its proton conductance. Members of the UCP family can act as a defense against oxidative stress and, thus, UCP2 plays a protective role in tumor cells. High UCP2 levels have been associated with chemoresistance. We demonstrate that chromanes also inhibit UCP2 and, in HT-29 human carcinoma cells, cause oxidative stress. The chromane derivatives can act synergistically with chemotherapeutic agents; for instance, they increase the toxicity of arsenic trioxide in HT-29 cells. These findings open a promising line in the development of novel anticancer agents
agents chromane derivatives chromanes findings open HT-29 cells HT-29 human carcinoma cells lower superoxide levels Members modulate potential UCP1 regulators protective role proton conductance tumor cells UCP family UCPs uncoupling proteins
Description11 páginas, 6 figuras, 1 tabla, 4 figuras suplementarias -- PAGS nros. 264-274
Publisher version (URL)http://dx.doi.org/10.1016/j.chembiol.2010.12.012
URIhttp://hdl.handle.net/10261/66148
DOI10.1016/j.chembiol.2010.12.012
ISSN1074-5521
E-ISSN1879-1301
Appears in Collections:(CIB) Artículos
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