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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Review Article

ABC Transporters in Extrahepatic Tissues: Pharmacological Regulation in Heart and Intestine

Author(s): Silvina Villanueva, Wei Zhang, Felipe Zecchinati, Aldo Mottino and Mary Vore*

Volume 26, Issue 7, 2019

Page: [1155 - 1184] Pages: 30

DOI: 10.2174/0929867325666180327092639

Price: $65


ATP binding cassette (ABC) transporters are transmembrane proteins expressed in secretory epithelia like the liver, kidneys and intestine, in the epithelia exhibiting barrier function such as the blood-brain barrier and placenta, and to a much lesser extent, in tissues like reproductive organs, lungs, heart and pancreas, among others. They regulate internal distribution of endogenous metabolites and xenobiotics including drugs of therapeutic use and also participate in their elimination from the body. We here describe the function and regulation of ABC transporters in the heart and small intestine, as examples of extrahepatic tissues, in which ABC proteins play clearly different roles. In the heart, they are involved in tissue pathogenesis as well as in protecting this organ against toxic compounds and druginduced oxidative stress. The small intestine is highly exposed to therapeutic drugs taken orally and, consequently, ABC transporters localized on its surface strongly influence drug absorption and pharmacokinetics. Examples of the ABC proteins currently described are Multidrug Resistance-associated Proteins 1 and 2 (MRP1 and 2) for heart and small intestine, respectively, and P-glycoprotein (P-gp) and Breast Cancer Resistance Protein (BCRP) for both organs.

Keywords: ATP binding cassette transporters, P-glycoprotein, multidrug resistance-associated proteins, breast cancer resistance protein, heart, intestine, drug transport.

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