On the putative co-transport of drugs by multidrug resistance proteins

P. Borst; N. Zelcer; K. van de Wetering; B. Poolman

doi:https://doi.org/10.1016/j.febslet.2005.12.039

On the putative co-transport of drugs by multidrug resistance proteins

P. Borst, N. Zelcer, K. van de Wetering, B. Poolman

Research output: Contribution to journal › Review article › Academic › peer-review

68 Citations (Scopus)

Abstract

Experiments with multidrug resistance-associated protein 1 (MRP1) showed 10-years ago that transport of vincristine (VCR) by MRP1 could be stimulated by GSH, and transport of GSH by VCR. Since then many examples of stimulated transport have been reported for MRP1, 2, 3, 4 and 8. We discuss here three models to explain stimulated transport. We favour a model in which a large promiscuous binding site can bind more than one ligand, allowing cooperative/competitive interactions between ligands within the binding site. We conclude that there is no unambiguous proof for co-transport of two different ligands by MRPs, but that cross-stimulated transport can explain the published data

Original language	English
Pages (from-to)	1085-1093
Journal	FEBS letters
Volume	580
Issue number	4
DOIs	https://doi.org/10.1016/j.febslet.2005.12.039
Publication status	Published - 2006

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https://doi.org/10.1016/j.febslet.2005.12.039

Cite this

@article{2f608baad48c4e1f800cce75f5d15505,

title = "On the putative co-transport of drugs by multidrug resistance proteins",

abstract = "Experiments with multidrug resistance-associated protein 1 (MRP1) showed 10-years ago that transport of vincristine (VCR) by MRP1 could be stimulated by GSH, and transport of GSH by VCR. Since then many examples of stimulated transport have been reported for MRP1, 2, 3, 4 and 8. We discuss here three models to explain stimulated transport. We favour a model in which a large promiscuous binding site can bind more than one ligand, allowing cooperative/competitive interactions between ligands within the binding site. We conclude that there is no unambiguous proof for co-transport of two different ligands by MRPs, but that cross-stimulated transport can explain the published data",

author = "P. Borst and N. Zelcer and {van de Wetering}, K. and B. Poolman",

year = "2006",

doi = "https://doi.org/10.1016/j.febslet.2005.12.039",

language = "English",

volume = "580",

pages = "1085--1093",

journal = "FEBS letters",

issn = "0014-5793",

publisher = "Elsevier",

number = "4",

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TY - JOUR

T1 - On the putative co-transport of drugs by multidrug resistance proteins

AU - Borst, P.

AU - Zelcer, N.

AU - van de Wetering, K.

AU - Poolman, B.

PY - 2006

Y1 - 2006

N2 - Experiments with multidrug resistance-associated protein 1 (MRP1) showed 10-years ago that transport of vincristine (VCR) by MRP1 could be stimulated by GSH, and transport of GSH by VCR. Since then many examples of stimulated transport have been reported for MRP1, 2, 3, 4 and 8. We discuss here three models to explain stimulated transport. We favour a model in which a large promiscuous binding site can bind more than one ligand, allowing cooperative/competitive interactions between ligands within the binding site. We conclude that there is no unambiguous proof for co-transport of two different ligands by MRPs, but that cross-stimulated transport can explain the published data

AB - Experiments with multidrug resistance-associated protein 1 (MRP1) showed 10-years ago that transport of vincristine (VCR) by MRP1 could be stimulated by GSH, and transport of GSH by VCR. Since then many examples of stimulated transport have been reported for MRP1, 2, 3, 4 and 8. We discuss here three models to explain stimulated transport. We favour a model in which a large promiscuous binding site can bind more than one ligand, allowing cooperative/competitive interactions between ligands within the binding site. We conclude that there is no unambiguous proof for co-transport of two different ligands by MRPs, but that cross-stimulated transport can explain the published data

U2 - https://doi.org/10.1016/j.febslet.2005.12.039

DO - https://doi.org/10.1016/j.febslet.2005.12.039

M3 - Review article

C2 - 16386247

SN - 0014-5793

VL - 580

SP - 1085

EP - 1093

JO - FEBS letters

JF - FEBS letters

IS - 4

ER -