FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2049823629> ?p ?o ?g. }

• W2049823629 endingPage "3041" @default.
• W2049823629 startingPage "3029" @default.
• W2049823629 abstract "Abstract Sildenafil is a potent and selective inhibitor of the type 5 cGMP (cyclic guanosine 3′,5′-monophosphate)-specific phosphodiesterase that is used clinically to treat erectile dysfunction and pulmonary arterial hypertension. Here, we report that sildenafil has differential effects on cell surface ABC transporters such as ABCB1, ABCC1, and ABCG2 that modulate intracompartmental and intracellular concentrations of chemotherapeutic drugs. In ABCB1-overexpressing cells, nontoxic doses of sildenafil inhibited resistance and increased the effective intracellular concentration of ABCB1 substrate drugs such as paclitaxel. Similarly, in ABCG2-overexpressing cells, sildenafil inhibited resistance to ABCG2 substrate anticancer drugs, for example, increasing the effective intracellular concentration of mitoxantrone or the fluorescent compound BODIPY-prazosin. Sildenafil also moderately inhibited the transport of E217βG and methotrexate by the ABCG2 transporter. Mechanistic investigations revealed that sildenafil stimulated ABCB1 ATPase activity and inhibited photolabeling of ABCB1 with [125I]-iodoarylazidoprazosin (IAAP), whereas it only slightly stimulated ABCG2 ATPase activity and inhibited photolabeling of ABCG2 with [125I]-IAAP. In contrast, sildenafil did not alter the sensitivity of parental, ABCB1-, or ABCG2-overexpressing cells to non-ABCB1 and non-ABCG2 substrate drugs, nor did sildenafil affect the function of another ABC drug transporter, ABCC1. Homology modeling predicted the binding conformation of sildenafil within the large cavity of the transmembrane region of ABCB1. Overall, we found that sildenafil inhibits the transporter function of ABCB1 and ABCG2, with a stronger effect on ABCB1. Our findings suggest a possible strategy to enhance the distribution and potentially the activity of anticancer drugs by jointly using a clinically approved drug with known side effects and drug–drug interactions. Cancer Res; 71(8); 3029–41. ©2011 AACR." @default.
• W2049823629 created "2016-06-24" @default.
• W2049823629 creator A5004086293 @default.
• W2049823629 creator A5004261103 @default.
• W2049823629 creator A5013592290 @default.
• W2049823629 creator A5016410708 @default.
• W2049823629 creator A5017735292 @default.
• W2049823629 creator A5029653357 @default.
• W2049823629 creator A5043393789 @default.
• W2049823629 creator A5044867727 @default.
• W2049823629 creator A5048003025 @default.
• W2049823629 creator A5050699960 @default.
• W2049823629 creator A5051562975 @default.
• W2049823629 creator A5060837722 @default.
• W2049823629 creator A5081938413 @default.
• W2049823629 date "2011-04-13" @default.
• W2049823629 modified "2023-10-17" @default.
• W2049823629 title "Sildenafil Reverses ABCB1- and ABCG2-Mediated Chemotherapeutic Drug Resistance" @default.
• W2049823629 cites W1530050855 @default.
• W2049823629 cites W1549117291 @default.
• W2049823629 cites W1697899995 @default.
• W2049823629 cites W1803435936 @default.
• W2049823629 cites W1967839568 @default.
• W2049823629 cites W2001852299 @default.
• W2049823629 cites W2004640774 @default.
• W2049823629 cites W2008935282 @default.
• W2049823629 cites W2010421456 @default.
• W2049823629 cites W2012834147 @default.
• W2049823629 cites W2019346113 @default.
• W2049823629 cites W2023695537 @default.
• W2049823629 cites W2039108002 @default.
• W2049823629 cites W2040906015 @default.
• W2049823629 cites W2050767064 @default.
• W2049823629 cites W2051381895 @default.
• W2049823629 cites W2055904567 @default.
• W2049823629 cites W2058394127 @default.
• W2049823629 cites W2064111887 @default.
• W2049823629 cites W2072517578 @default.
• W2049823629 cites W2075749214 @default.
• W2049823629 cites W2082843436 @default.
• W2049823629 cites W2084600496 @default.
• W2049823629 cites W2090380729 @default.
• W2049823629 cites W2098064809 @default.
• W2049823629 cites W2098142549 @default.
• W2049823629 cites W2115830553 @default.
• W2049823629 cites W2120539661 @default.
• W2049823629 cites W2125329951 @default.
• W2049823629 cites W2138365326 @default.
• W2049823629 cites W2157393167 @default.
• W2049823629 cites W2169120362 @default.
• W2049823629 cites W2332171508 @default.
• W2049823629 cites W85951151 @default.
• W2049823629 doi "https://doi.org/10.1158/0008-5472.can-10-3820" @default.
• W2049823629 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/3078184" @default.
• W2049823629 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/21402712" @default.
• W2049823629 hasPublicationYear "2011" @default.
• W2049823629 type Work @default.
• W2049823629 sameAs 2049823629 @default.
• W2049823629 citedByCount "146" @default.
• W2049823629 countsByYear W20498236292012 @default.
• W2049823629 countsByYear W20498236292013 @default.
• W2049823629 countsByYear W20498236292014 @default.
• W2049823629 countsByYear W20498236292015 @default.
• W2049823629 countsByYear W20498236292016 @default.
• W2049823629 countsByYear W20498236292017 @default.
• W2049823629 countsByYear W20498236292018 @default.
• W2049823629 countsByYear W20498236292019 @default.
• W2049823629 countsByYear W20498236292020 @default.
• W2049823629 countsByYear W20498236292021 @default.
• W2049823629 countsByYear W20498236292022 @default.
• W2049823629 countsByYear W20498236292023 @default.
• W2049823629 crossrefType "journal-article" @default.
• W2049823629 hasAuthorship W2049823629A5004086293 @default.
• W2049823629 hasAuthorship W2049823629A5004261103 @default.
• W2049823629 hasAuthorship W2049823629A5013592290 @default.
• W2049823629 hasAuthorship W2049823629A5016410708 @default.
• W2049823629 hasAuthorship W2049823629A5017735292 @default.
• W2049823629 hasAuthorship W2049823629A5029653357 @default.
• W2049823629 hasAuthorship W2049823629A5043393789 @default.
• W2049823629 hasAuthorship W2049823629A5044867727 @default.
• W2049823629 hasAuthorship W2049823629A5048003025 @default.
• W2049823629 hasAuthorship W2049823629A5050699960 @default.
• W2049823629 hasAuthorship W2049823629A5051562975 @default.
• W2049823629 hasAuthorship W2049823629A5060837722 @default.
• W2049823629 hasAuthorship W2049823629A5081938413 @default.
• W2049823629 hasBestOaLocation W20498236291 @default.
• W2049823629 hasConcept C104317684 @default.
• W2049823629 hasConcept C126322002 @default.
• W2049823629 hasConcept C149011108 @default.
• W2049823629 hasConcept C185592680 @default.
• W2049823629 hasConcept C2776768464 @default.
• W2049823629 hasConcept C2780994212 @default.
• W2049823629 hasConcept C44312359 @default.
• W2049823629 hasConcept C512196 @default.
• W2049823629 hasConcept C519581460 @default.
• W2049823629 hasConcept C55493867 @default.
• W2049823629 hasConcept C63443662 @default.
• W2049823629 hasConcept C71924100 @default.

• next