Corpus ID: 16242000

Circumvention of breast cancer resistance protein (BCRP)-mediated resistance to camptothecins in vitro using non-substrate drugs or the BCRP inhibitor GF120918.

@article{Maliepaard2001CircumventionOB,
  title={Circumvention of breast cancer resistance protein (BCRP)-mediated resistance to camptothecins in vitro using non-substrate drugs or the BCRP inhibitor GF120918.},
  author={Marc Maliepaard and Marg{\^o}t A van Gastelen and Akiko Tohgo and Frederick H. Hausheer and Robert C A M van Waardenburg and Laurina A de Jong and Dick Pluim and Jos H. Beijnen and Jan H. M. Schellens},
  journal={Clinical cancer research : an official journal of the American Association for Cancer Research},
  year={2001},
  volume={7 4},
  pages={
          935-41
        }
}
This study was aimed at characterizing the role of BCRP/MXR/ABCP (BCRP) in resistance of the human ovarian tumor cell lines T8 and MX3 to camptothecins more extensively and investigating whether resistance can be reversed by inhibiting BCRP by GF120918. Camptothecins studied were topotecan, CPT-11, and its active metabolite SN-38, 9-aminocamptothecin, and the novel experimental camptothecins NX211, DX8951f, and BNP1350. Notably, DX8951f and BNP1350 appeared to be very poor substrates for BCRP… Expand
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250 Citations
Highly Influential Citations
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250 Citations

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Citation Type

Differential effects of the breast cancer resistance protein on the cellular accumulation and cytotoxicity of 9-aminocamptothecin and 9-nitrocamptothecin.
TLDR
It is suggested that wild-type as well as R482T BCRP mediates cellular efflux of 9-AC but not 9-NC, and polar groups at the 9 or 10 position of the CPT A ring facilitate interaction with B CRP and have implications for the clinical development of new CPT analogues. Expand
Modulation of breast cancer resistance protein (BCRP/ABCG2) gene expression using RNA interference.
TLDR
It is found that expression of BCRP protein was inducible by 17beta-estradiol and that this effect was ameliorated by the introduction of siRNAs, indicating that siRN as could modulate MDR in vitro and may present a new approach to overcome B CRP-mediated drug resistance. Expand
Ixabepilone, a Novel Microtubule-Targeting Agent for Breast Cancer, Is a Substrate for P-Glycoprotein (P-gp/MDR1/ABCB1) but not Breast Cancer Resistance Protein (BCRP/ABCG2)
  • H. Shen, F. Lee, J. Gan
  • Biology, Medicine
  • Journal of Pharmacology and Experimental Therapeutics
  • 2011
TLDR
It is suggested that P-gp could cause resistance to ixabepilone in tumors and affect the disposition of the drug, but it is unlikely that BCRP mediates any drug resistance to the drug. Expand
Induction of breast cancer resistance protein by the camptothecin derivative DX-8951f is associated with minor reduction of antitumour activity
TLDR
In vivo experiments in well-established 2780DX8 human tumour xenografts demonstrated that the growth inhibition induced by CPT-11 was more affected by breast cancer resistance protein expression than that of DX-8951f, indicating for the first time that DX- 8951f is able to induce breast cancer resistant protein as a mechanism of resistance. Expand
EFFECTS OF DIHYDROPYRIDINES AND PYRIDINES ON MULTIDRUG RESISTANCE MEDIATED BY BREAST CANCER RESISTANCE PROTEIN: IN VITRO AND IN VIVO STUDIES
TLDR
The effects of the dihydropyridine and pyridine compounds on mitoxantrone cytotoxicity paralleled their effects on mitxantrone accumulation, providing proof-of-concept for in vivo inhibition of BCRP by these agents. Expand
Role of the Breast Cancer Resistance Protein (BCRP/ABCG2) in Drug Transport—an Update
TLDR
This review provides an update of current knowledge on basic biochemistry and pharmacological functions of BCRP as well as its relevance to drug resistance and drug disposition. Expand
Overexpression of wild-type breast cancer resistance protein mediates methotrexate resistance.
TLDR
A novel role for BCRP as a mediator of MTX resistance is demonstrated and further evidence for the importance of amino acid 482 in substrate specificity is provided. Expand
Modulation of the atypical multidrug-resistant phenotype by a hammerhead ribozyme directed against the ABC transporter BCRP/MXR/ABCG2
TLDR
The data suggest that the BCRP-mediated contingent to the drug resistance was overcome nearly completely and indicate that ribozyme-based gene therapy may be clinically applicable in preventing and reversing BCRp-mediated atypical MDR. Expand
Breast Cancer Resistance Protein (BCRP) in Acute Leukaemia
TLDR
The role of BCRP in the physiology of hematopoietic stem cells is addressed, as well as the involvement of B CRP in multidrug resistance in acute leukemia. Expand
Breast cancer resistance protein-mediated topotecan resistance in ovarian cancer cells.
  • P. Jia, S. Wu, +8 authors D. Ma
  • Biology, Medicine
  • International journal of gynecological cancer : official journal of the International Gynecological Cancer Society
  • 2005
TLDR
Introduction of antisense-phosphorothioate oligonucleotide derived from BCRP mRNA into TPT-resistant cells resulted in a significant increase in the concentration of intracellular Rh123, which suggested a novel mechanism in which a reduced intrACEllular drug concentration may be mediated by B CRP gene products in human ovarian cancer cells. Expand
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References

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TLDR
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TLDR
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TLDR
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TLDR
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TLDR
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TLDR
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