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Molecules 2017, 22(4), 589;

ABC Transport Proteins in Cardiovascular Disease—A Brief Summary

Institute of Pharmacy, Department of Clinical Pharmacy and Pharmacotherapy, Martin-Luther-University Halle-Wittenberg, Wolfgang-Langenbeck-Strasse 4, D-06120 Halle (Saale), Germany
Author to whom correspondence should be addressed.
Academic Editor: Maria Emília de Sousa
Received: 31 January 2017 / Revised: 29 March 2017 / Accepted: 3 April 2017 / Published: 6 April 2017
(This article belongs to the Special Issue Can Membrane Transporters Contribute to Drug Discovery?)
Full-Text   |   PDF [280 KB, uploaded 7 April 2017]


Adenosine triphosphate (ATP)-binding cassette (ABC) transporters may play an important role in the pathogenesis of atherosclerotic vascular diseases due to their involvement in cholesterol homeostasis, blood pressure regulation, endothelial function, vascular inflammation, as well as platelet production and aggregation. In this regard, ABC transporters, such as ABCA1, ABCG5 and ABCG8, were initially found to be responsible for genetically-inherited syndromes like Tangier diseases and sitosterolemia. These findings led to the understanding of those transporter’s function in cellular cholesterol efflux and thereby also linked them to atherosclerosis and cardiovascular diseases (CVD). Subsequently, further ABC transporters, i.e., ABCG1, ABCG4, ABCB6, ABCC1, ABCC6 or ABCC9, have been shown to directly or indirectly affect cellular cholesterol efflux, the inflammatory response in macrophages, megakaryocyte proliferation and thrombus formation, as well as vascular function and blood pressure, and may thereby contribute to the pathogenesis of CVD and its complications. Furthermore, ABC transporters, such as ABCB1, ABCC2 or ABCG2, may affect the safety and efficacy of several drug classes currently in use for CVD treatment. This review will give a brief overview of ABC transporters involved in the process of atherogenesis and CVD pathology. It also aims to briefly summarize the role of ABC transporters in the pharmacokinetics and disposition of drugs frequently used to treat CVD and CVD-related complications. View Full-Text
Keywords: ABC transporter; cardiovascular diseases; atherosclerosis; pharmacokinetic interactions; pharmacogenetics ABC transporter; cardiovascular diseases; atherosclerosis; pharmacokinetic interactions; pharmacogenetics
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Schumacher, T.; Benndorf, R.A. ABC Transport Proteins in Cardiovascular Disease—A Brief Summary. Molecules 2017, 22, 589.

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