Drug Efflux Pumps in Cancer Resistance Pathways: From Molecular Recognition and Characterization to Possible Inhibition Strateg 2020
DOI: 10.1016/b978-0-12-816434-1.00003-6
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Efflux transporters in cancer resistance: Molecular and functional characterization of breast cancer resistance protein

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Cited by 5 publications
(4 citation statements)
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“…In the quantification of substrate transport, we suggest the use of fluorescent substrates first because of the easiness of the quantification of the fluorescence strength. However, it should be noted that rhodamine 123 and Hoechst 33,324 are not highly specific to P -gp and BCRP [ 38 , 39 ], respectively. We therefore recommend the confirmation of the results obtained in fluorescence quantification using more specific substrates: digoxin for P -gp, dantrolene and SASP for BCRP.…”
Section: Resultsmentioning
confidence: 99%
“…In the quantification of substrate transport, we suggest the use of fluorescent substrates first because of the easiness of the quantification of the fluorescence strength. However, it should be noted that rhodamine 123 and Hoechst 33,324 are not highly specific to P -gp and BCRP [ 38 , 39 ], respectively. We therefore recommend the confirmation of the results obtained in fluorescence quantification using more specific substrates: digoxin for P -gp, dantrolene and SASP for BCRP.…”
Section: Resultsmentioning
confidence: 99%
“…One of its major compounds, the 5,3′,5′-trihydroxy-3,6,7,4′-tetramethoxyflavone, strongly suppressed the breast cancer resistance protein (BCRP/ABCG2) [ 346 ] which belongs to the family of ATP-binding cassette proteins. BCRP mediates multidrug resistance and promotes an efflux of such potent drugs, such as methotrexate, irinotecan, topotecan, sorafenib, gefitinib, and doxorubicin, from cancer cells [ 347 ].…”
Section: Plants From Different Continents Used In Ethnomedicine For T...mentioning
confidence: 99%
“…Structurally, BCRP2 is a-72 kDa protein comprised of a transmembrane domain (TMD) of 6 alfa-helices and a nucleotide binding domain (NBD) at the N-terminal where an ATP is hydrolyzed into ADP during transport. To be functional, two BCRP2 monomers associate in a homodimer forming a transmembrane channel that allows the efflux of a large spectrum of xenotoxic substrates, including different types of mycotoxins and their conjugates [ 8 , 66 , 67 , 68 ] ( Figure 2 d). During lactation, BCRP2 is upregulated with a concomitant increase in the yield of milk and excretion of mycotoxins [ 8 , 69 , 70 , 71 , 72 , 73 , 74 ].…”
Section: Physiological Mechanisms Of Afm1 Secretion Into Breast Milkmentioning
confidence: 99%
“…As the multidrug and xenobiotic efflux transporters are beyond the scope of this review, for more information on the structural diversity, classification, and molecular functioning, the readers are referred to relevant literature reviews, e.g., refs. [ 67 , 68 , 81 , 82 , 83 ].…”
Section: Physiological Mechanisms Of Afm1 Secretion Into Breast Milkmentioning
confidence: 99%