Mechanisms of resistance to anticancer drugs: The role of the polymorphic ABC transporters ABC1 and ABCG2

Erin R. Lepper; Kees Nooter; Jaap Verweij; Milin R. Acharya; William D. Figg; Alex Sparreboom

doi:10.1517/14622416.6.2.115

Mechanisms of resistance to anticancer drugs: The role of the polymorphic ABC transporters ABC1 and ABCG2

Erin R. Lepper, Kees Nooter, Jaap Verweij, Milin R. Acharya, William D. Figg, Alex Sparreboom^*

^*Corresponding author for this work

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

112 Scopus citations

Abstract

ATP-binding cassette (ABC) genes play a role in the resistance of malignant cells to anticancer agents. The ABC gene products, including ABCB1 (P-glycoprotein) and ABCG2 (breast cancer-resistance protein [BCRP], mitoxantrone-resistance protein [MXR], or ABC transporter in placenta [ABCP]), are also known to influence oral absorption and disposition of a wide variety of drugs. As a result, the expression levels of these proteins in humans have important consequences for an individual's susceptibility to certain drug-induced side effects, interactions, and treatment efficacy. Naturally occurring variants in ABC transporter genes have been identified that might affect the function and expression of the protein. This review focuses on recent advances in the pharmacogenetics of the ABC transporters ABCB1 and ABCG2, and discusses potential implications of genetic variants for the chemotherapeutic treatment of cancer.

Original language	English
Pages (from-to)	115-138
Number of pages	24
Journal	Pharmacogenomics
Volume	6
Issue number	2
DOIs	https://doi.org/10.1517/14622416.6.2.115
State	Published - Mar 2005
Externally published	Yes

Keywords

ABC transporters
ABCB1
ABCG2
BCRP
Breast cancer resistance protein
Chemotherapy
P-glycoprotein
Pharmacogenetics
Polymorphisms

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10.1517/14622416.6.2.115

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title = "Mechanisms of resistance to anticancer drugs: The role of the polymorphic ABC transporters ABC1 and ABCG2",

abstract = "ATP-binding cassette (ABC) genes play a role in the resistance of malignant cells to anticancer agents. The ABC gene products, including ABCB1 (P-glycoprotein) and ABCG2 (breast cancer-resistance protein [BCRP], mitoxantrone-resistance protein [MXR], or ABC transporter in placenta [ABCP]), are also known to influence oral absorption and disposition of a wide variety of drugs. As a result, the expression levels of these proteins in humans have important consequences for an individual's susceptibility to certain drug-induced side effects, interactions, and treatment efficacy. Naturally occurring variants in ABC transporter genes have been identified that might affect the function and expression of the protein. This review focuses on recent advances in the pharmacogenetics of the ABC transporters ABCB1 and ABCG2, and discusses potential implications of genetic variants for the chemotherapeutic treatment of cancer.",

keywords = "ABC transporters, ABCB1, ABCG2, BCRP, Breast cancer resistance protein, Chemotherapy, P-glycoprotein, Pharmacogenetics, Polymorphisms",

author = "Lepper, {Erin R.} and Kees Nooter and Jaap Verweij and Acharya, {Milin R.} and Figg, {William D.} and Alex Sparreboom",

year = "2005",

month = mar,

doi = "10.1517/14622416.6.2.115",

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pages = "115--138",

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T2 - The role of the polymorphic ABC transporters ABC1 and ABCG2

AU - Lepper, Erin R.

AU - Nooter, Kees

AU - Verweij, Jaap

AU - Acharya, Milin R.

AU - Figg, William D.

AU - Sparreboom, Alex

PY - 2005/3

Y1 - 2005/3

N2 - ATP-binding cassette (ABC) genes play a role in the resistance of malignant cells to anticancer agents. The ABC gene products, including ABCB1 (P-glycoprotein) and ABCG2 (breast cancer-resistance protein [BCRP], mitoxantrone-resistance protein [MXR], or ABC transporter in placenta [ABCP]), are also known to influence oral absorption and disposition of a wide variety of drugs. As a result, the expression levels of these proteins in humans have important consequences for an individual's susceptibility to certain drug-induced side effects, interactions, and treatment efficacy. Naturally occurring variants in ABC transporter genes have been identified that might affect the function and expression of the protein. This review focuses on recent advances in the pharmacogenetics of the ABC transporters ABCB1 and ABCG2, and discusses potential implications of genetic variants for the chemotherapeutic treatment of cancer.

AB - ATP-binding cassette (ABC) genes play a role in the resistance of malignant cells to anticancer agents. The ABC gene products, including ABCB1 (P-glycoprotein) and ABCG2 (breast cancer-resistance protein [BCRP], mitoxantrone-resistance protein [MXR], or ABC transporter in placenta [ABCP]), are also known to influence oral absorption and disposition of a wide variety of drugs. As a result, the expression levels of these proteins in humans have important consequences for an individual's susceptibility to certain drug-induced side effects, interactions, and treatment efficacy. Naturally occurring variants in ABC transporter genes have been identified that might affect the function and expression of the protein. This review focuses on recent advances in the pharmacogenetics of the ABC transporters ABCB1 and ABCG2, and discusses potential implications of genetic variants for the chemotherapeutic treatment of cancer.

KW - ABC transporters

KW - ABCB1

KW - ABCG2

KW - BCRP

KW - Breast cancer resistance protein

KW - Chemotherapy

KW - P-glycoprotein

KW - Pharmacogenetics

KW - Polymorphisms

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EP - 138

JO - Pharmacogenomics

JF - Pharmacogenomics

IS - 2

ER -

Mechanisms of resistance to anticancer drugs: The role of the polymorphic ABC transporters ABC1 and ABCG2

Abstract

Keywords

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