Matches in SemOpenAlex for { <https://semopenalex.org/work/W2895729583> ?p ?o ?g. }
- W2895729583 endingPage "1469.e6" @default.
- W2895729583 startingPage "1456" @default.
- W2895729583 abstract "5-Nitrofurans are antibiotic pro-drugs that have potential as cancer therapeutics. Here, we show that 5-nitrofurans can be bio-activated by aldehyde dehydrogenase (ALDH) 1A1/1A3 enzymes that are highly expressed in a subpopulation of cancer-initiating (stem) cells. We discover that the 5-nitrofuran, nifuroxazide, is selective for bio-activation by ALDH1 isoforms over ALDH2, whereby it both oxidizes ALDH1 and is converted to cytotoxic metabolites in a two-hit pro-drug mechanism. We show that ALDH1High melanoma cells are sensitive to nifuroxazide, while ALDH1A3 loss-of-function mutations confer drug resistance. In tumors, nifuroxazide targets ALDH1High melanoma subpopulations with the subsequent loss of melanoma-initiating cell potential. BRAF and MEK inhibitor therapy increases ALDH1 expression in patient melanomas, and effectively combines with nifuroxazide in melanoma cell models. The selective eradication of ALDH1High cells by nifuroxazide-ALDH1 activation goes beyond current strategies based on inhibiting ALDH1 and provides a rational basis for the nifuroxazide mechanism of action in cancer." @default.
- W2895729583 created "2018-10-12" @default.
- W2895729583 creator A5011548408 @default.
- W2895729583 creator A5012671311 @default.
- W2895729583 creator A5015025645 @default.
- W2895729583 creator A5017522749 @default.
- W2895729583 creator A5022534990 @default.
- W2895729583 creator A5024623465 @default.
- W2895729583 creator A5031403355 @default.
- W2895729583 creator A5033198674 @default.
- W2895729583 creator A5039639608 @default.
- W2895729583 creator A5040571738 @default.
- W2895729583 creator A5048432357 @default.
- W2895729583 creator A5048615638 @default.
- W2895729583 creator A5049465372 @default.
- W2895729583 creator A5055498999 @default.
- W2895729583 creator A5055949749 @default.
- W2895729583 creator A5059560149 @default.
- W2895729583 creator A5059996836 @default.
- W2895729583 creator A5066808283 @default.
- W2895729583 creator A5069782695 @default.
- W2895729583 creator A5091699198 @default.
- W2895729583 date "2018-12-01" @default.
- W2895729583 modified "2023-10-17" @default.
- W2895729583 title "ALDH1 Bio-activates Nifuroxazide to Eradicate ALDHHigh Melanoma-Initiating Cells" @default.
- W2895729583 cites W1542109034 @default.
- W2895729583 cites W1950829641 @default.
- W2895729583 cites W1958877028 @default.
- W2895729583 cites W1974466912 @default.
- W2895729583 cites W1978874148 @default.
- W2895729583 cites W2002646075 @default.
- W2895729583 cites W2004878973 @default.
- W2895729583 cites W2010973115 @default.
- W2895729583 cites W2013414297 @default.
- W2895729583 cites W2019774245 @default.
- W2895729583 cites W2029589773 @default.
- W2895729583 cites W2031211461 @default.
- W2895729583 cites W2040706741 @default.
- W2895729583 cites W2052911318 @default.
- W2895729583 cites W2067401961 @default.
- W2895729583 cites W2068713081 @default.
- W2895729583 cites W2070826332 @default.
- W2895729583 cites W2082088498 @default.
- W2895729583 cites W2086434836 @default.
- W2895729583 cites W2095950689 @default.
- W2895729583 cites W2109689528 @default.
- W2895729583 cites W2114843025 @default.
- W2895729583 cites W2118453722 @default.
- W2895729583 cites W2122721237 @default.
- W2895729583 cites W2144190812 @default.
- W2895729583 cites W2149441684 @default.
- W2895729583 cites W2150479858 @default.
- W2895729583 cites W2163655212 @default.
- W2895729583 cites W2170776626 @default.
- W2895729583 cites W2276370059 @default.
- W2895729583 cites W2413114447 @default.
- W2895729583 cites W2531053278 @default.
- W2895729583 cites W2533419568 @default.
- W2895729583 cites W2563042458 @default.
- W2895729583 cites W2570483783 @default.
- W2895729583 cites W2605233023 @default.
- W2895729583 doi "https://doi.org/10.1016/j.chembiol.2018.09.005" @default.
- W2895729583 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/6309505" @default.
- W2895729583 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/30293938" @default.
- W2895729583 hasPublicationYear "2018" @default.
- W2895729583 type Work @default.
- W2895729583 sameAs 2895729583 @default.
- W2895729583 citedByCount "38" @default.
- W2895729583 countsByYear W28957295832018 @default.
- W2895729583 countsByYear W28957295832019 @default.
- W2895729583 countsByYear W28957295832020 @default.
- W2895729583 countsByYear W28957295832021 @default.
- W2895729583 countsByYear W28957295832022 @default.
- W2895729583 countsByYear W28957295832023 @default.
- W2895729583 crossrefType "journal-article" @default.
- W2895729583 hasAuthorship W2895729583A5011548408 @default.
- W2895729583 hasAuthorship W2895729583A5012671311 @default.
- W2895729583 hasAuthorship W2895729583A5015025645 @default.
- W2895729583 hasAuthorship W2895729583A5017522749 @default.
- W2895729583 hasAuthorship W2895729583A5022534990 @default.
- W2895729583 hasAuthorship W2895729583A5024623465 @default.
- W2895729583 hasAuthorship W2895729583A5031403355 @default.
- W2895729583 hasAuthorship W2895729583A5033198674 @default.
- W2895729583 hasAuthorship W2895729583A5039639608 @default.
- W2895729583 hasAuthorship W2895729583A5040571738 @default.
- W2895729583 hasAuthorship W2895729583A5048432357 @default.
- W2895729583 hasAuthorship W2895729583A5048615638 @default.
- W2895729583 hasAuthorship W2895729583A5049465372 @default.
- W2895729583 hasAuthorship W2895729583A5055498999 @default.
- W2895729583 hasAuthorship W2895729583A5055949749 @default.
- W2895729583 hasAuthorship W2895729583A5059560149 @default.
- W2895729583 hasAuthorship W2895729583A5059996836 @default.
- W2895729583 hasAuthorship W2895729583A5066808283 @default.
- W2895729583 hasAuthorship W2895729583A5069782695 @default.
- W2895729583 hasAuthorship W2895729583A5091699198 @default.
- W2895729583 hasBestOaLocation W28957295831 @default.
- W2895729583 hasConcept C181199279 @default.
- W2895729583 hasConcept C185592680 @default.