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(Section A: Molecular, Structural, and Cellular Biology of Drug Transporters) The MRP-Related and BCRP / ABCG2 Multidrug Resistance Proteins: Biology, Substrate Specificity and Regulation
Abstract
Several members of different families of the ATP-binding cassette (ABC) superfamily of transport proteins are capable of transporting an extraordinarily structurally diverse array of endo- and xenobiotics and their metabolites across cell membranes. Together, these transporters play an important role in the absorption, disposition and elimination of these chemicals in the body. In tumor cells, increased expression of these drug transporters is associated with resistance to multiple chemotherapeutic agents. In this review, current knowledge of the biochemical, physiological and pharmacological properties of nine members of the multidrug resistance protein (MRP)-related ABCC family (MRP1, MRP2, MRP3, MRP4, MRP5, MRP6, MRP7, ABCC11 and ABCC12) as well as the G family member, ABCG2/BCRP, are summarized. A focus is placed on the structural similarities and differences of these drug transporters as well as the molecular determinants of their substrate specificities and transport activities. Factors that regulate expression of the MRP-related proteins and ABCG2/BCRP are also reviewed.
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Cited by
Targeting multidrug resistance in cancer
Szakács, G., Paterson, J. K., Ludwig, J. A., Booth-Genthe, C., & Gottesman, M. M. (2006) · Nature Reviews Drug Discovery · doi:10.1038/nrd1984 · Cited by 3,609
Blood-brain barrier active efflux transporters: ATP-binding cassette gene family
Löscher, W., & Potschka, H. (2005) · NeuroRX · doi:10.1602/neurorx.2.1.86 · Cited by 872
Deeley, R. G., Westlake, C., & Cole, S. P. C. (2006) · Physiological Reviews · doi:10.1152/physrev.00035.2005 · Cited by 761
Self-citationAn overview of cancer multidrug resistance: a still unsolved problem
Lage, H. (2008) · Cellular and Molecular Life Sciences · doi:10.1007/s00018-008-8111-5 · Cited by 408
The apical conjugate efflux pump ABCC2 (MRP2)
Nies, A. T., & Keppler, D. (2007) · Pflügers Archiv - European Journal of Physiology · doi:10.1007/s00424-006-0109-y · Cited by 398
Metadata
- Authors
- Haimeur, A., Conseil, G., Deeley, R., & Cole, S.
- Venue
- Current Drug Metabolism
- Publisher
- Bentham Science Publishers Ltd.
- Published
- 2004-02-01
- Volume
- 5
- Issue
- 1
- Pages
- 21-53
- ISSN
- 1389-2002 (ISSN-L)
- OpenAlex
- W43589343
- Cited by
- 485
- References
- 0
- FWCI
- 26.29
- Type
- journal article
- Language
- en
- Open access
- closed
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- Haimeur, A., Conseil, G., Deeley, R., & Cole, S. (2004). (Section A: Molecular, Structural, and Cellular Biology of Drug Transporters) The MRP-Related and BCRP / ABCG2 Multidrug Resistance Proteins: Biology, Substrate Specificity and Regulation. Current Drug Metabolism. https://doi.org/10.2174/1389200043489199
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