Matches in SemOpenAlex for { <https://semopenalex.org/work/W4319971680> ?p ?o ?g. }
- W4319971680 endingPage "584" @default.
- W4319971680 startingPage "584" @default.
- W4319971680 abstract "Multidrug resistance (MDR) is a serious hurdle to successful cancer therapy. Here, we examined the efficiency of novel semi-synthetic dihydrotestosterone derivatives, more specifically androstano-arylpyrimidines in inhibiting the efflux activity of ATP-binding cassette (ABC) transporters and sensitizing inherently MDR colon cancer cells to various chemotherapy drugs. Using the Rhodamine123 accumulation assay, we evaluated the efflux activity of cancer cells following treatments with androstano-arylpyrimidines. We found that acetylated compounds were capable of attenuating the membrane efflux of inherently MDR cells; however, deacetylated counterparts were ineffective. To delineate the possible molecular mechanisms underlying these unique activities of androstano-arylpyrimidines, the degree of apoptosis induction was assessed by AnnexinV-based assays, both upon the individual as well as by steroid and chemotherapy agent combination treatments. Five dihydrotestosterone derivatives applied in combination with Doxorubicin or Epirubicin triggered massive apoptosis in MDR cells, and these combinations were more efficient than chemotherapy drugs together with Verapamil. Furthermore, our results revealed that androstano-arylpyrimidines induced significant endoplasmic reticulum stress (ER stress) but did not notably modulate ABC transporter expression. Therefore, ER stress triggered by acetylated androstano-arylpyrimidines is probably involved in the mechanism of efflux pump inhibition and drug sensitization which can be targeted in future drug developments to defeat inherently multidrug-resistant cancer." @default.
- W4319971680 created "2023-02-11" @default.
- W4319971680 creator A5024719326 @default.
- W4319971680 creator A5034051353 @default.
- W4319971680 creator A5034171215 @default.
- W4319971680 creator A5037385625 @default.
- W4319971680 creator A5043317787 @default.
- W4319971680 creator A5048699266 @default.
- W4319971680 creator A5057824431 @default.
- W4319971680 creator A5076326038 @default.
- W4319971680 creator A5076571987 @default.
- W4319971680 creator A5086462876 @default.
- W4319971680 date "2023-02-09" @default.
- W4319971680 modified "2023-09-25" @default.
- W4319971680 title "Semi-Synthetic Dihydrotestosterone Derivatives Modulate Inherent Multidrug Resistance and Sensitize Colon Cancer Cells to Chemotherapy" @default.
- W4319971680 cites W1483939381 @default.
- W4319971680 cites W1553345136 @default.
- W4319971680 cites W1880480947 @default.
- W4319971680 cites W1890354534 @default.
- W4319971680 cites W1976279720 @default.
- W4319971680 cites W1979595420 @default.
- W4319971680 cites W1989487207 @default.
- W4319971680 cites W1997730952 @default.
- W4319971680 cites W2001120217 @default.
- W4319971680 cites W2018289835 @default.
- W4319971680 cites W2031407900 @default.
- W4319971680 cites W2040613549 @default.
- W4319971680 cites W2049210214 @default.
- W4319971680 cites W2056422677 @default.
- W4319971680 cites W2078532650 @default.
- W4319971680 cites W2081104776 @default.
- W4319971680 cites W2088343576 @default.
- W4319971680 cites W2089771474 @default.
- W4319971680 cites W2101108802 @default.
- W4319971680 cites W2102099949 @default.
- W4319971680 cites W2104085655 @default.
- W4319971680 cites W2107277218 @default.
- W4319971680 cites W2114918609 @default.
- W4319971680 cites W2122753182 @default.
- W4319971680 cites W2128635872 @default.
- W4319971680 cites W2131487381 @default.
- W4319971680 cites W2162695817 @default.
- W4319971680 cites W2164578725 @default.
- W4319971680 cites W2169172001 @default.
- W4319971680 cites W2169302611 @default.
- W4319971680 cites W2190667064 @default.
- W4319971680 cites W2192080449 @default.
- W4319971680 cites W2257833110 @default.
- W4319971680 cites W2528568595 @default.
- W4319971680 cites W2586629973 @default.
- W4319971680 cites W2587862832 @default.
- W4319971680 cites W2622523929 @default.
- W4319971680 cites W2685284983 @default.
- W4319971680 cites W2753051611 @default.
- W4319971680 cites W2769426045 @default.
- W4319971680 cites W2793281803 @default.
- W4319971680 cites W2796552195 @default.
- W4319971680 cites W2810954382 @default.
- W4319971680 cites W2900213477 @default.
- W4319971680 cites W2918677618 @default.
- W4319971680 cites W2938150871 @default.
- W4319971680 cites W2949407848 @default.
- W4319971680 cites W2967586142 @default.
- W4319971680 cites W2977303957 @default.
- W4319971680 cites W3021909056 @default.
- W4319971680 cites W3092285225 @default.
- W4319971680 cites W3167783924 @default.
- W4319971680 cites W4225126408 @default.
- W4319971680 cites W4281758936 @default.
- W4319971680 cites W4283391086 @default.
- W4319971680 cites W4292801150 @default.
- W4319971680 cites W4293247451 @default.
- W4319971680 cites W4293539435 @default.
- W4319971680 doi "https://doi.org/10.3390/pharmaceutics15020584" @default.
- W4319971680 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/36839907" @default.
- W4319971680 hasPublicationYear "2023" @default.
- W4319971680 type Work @default.
- W4319971680 citedByCount "0" @default.
- W4319971680 crossrefType "journal-article" @default.
- W4319971680 hasAuthorship W4319971680A5024719326 @default.
- W4319971680 hasAuthorship W4319971680A5034051353 @default.
- W4319971680 hasAuthorship W4319971680A5034171215 @default.
- W4319971680 hasAuthorship W4319971680A5037385625 @default.
- W4319971680 hasAuthorship W4319971680A5043317787 @default.
- W4319971680 hasAuthorship W4319971680A5048699266 @default.
- W4319971680 hasAuthorship W4319971680A5057824431 @default.
- W4319971680 hasAuthorship W4319971680A5076326038 @default.
- W4319971680 hasAuthorship W4319971680A5076571987 @default.
- W4319971680 hasAuthorship W4319971680A5086462876 @default.
- W4319971680 hasBestOaLocation W43199716801 @default.
- W4319971680 hasConcept C104317684 @default.
- W4319971680 hasConcept C114851261 @default.
- W4319971680 hasConcept C121608353 @default.
- W4319971680 hasConcept C126322002 @default.
- W4319971680 hasConcept C133936738 @default.
- W4319971680 hasConcept C149011108 @default.
- W4319971680 hasConcept C185592680 @default.
- W4319971680 hasConcept C190283241 @default.