Importance of ABC Transporters in Drug Development.

Abstract:

:ATP-binding cassette (ABC) transporters are a huge family of ATP-dependent transmembrane proteins whose main function is exporting or importing substances or molecules through the cell membranes, plasma cell membrane, or inner membranes in organelles. They fulfill these functions by maintaining cell integrity, metabolism, and homeostasis. They are expressed in a variety of tissues as they transport numerous essential compounds including lipids and other signaling molecules. ABC transporters became widely studied since the discovery of their ability to carry a multitude of xenobiotics, including therapeutic drugs, and in light of the fact that they represent a hurdle for the treatment of resistant cancers. In contrast, the role of ABC transporters in neurological diseases like Alzheimer`s and Parkinson`s, depression, schizophrenia, and epilepsy remains controversial and their mechanism of action in these pathologies remains elusive, thus hindering the implementation of therapies aimed at modulating the functions of these transporters. To date, a number of natural and synthetic compounds are known to act as inhibitors, substrates, and even inducers of these transporters, being able to modulate their expression and/or function; however, their implication as therapeutic agents is far from reaching wide clinical utilization. This review highlights the importance of overcoming the challenges posed by ABC transporters in drug development.

journal_name

Curr Pharm Des

authors

Benadiba M,Maor Y

doi

10.2174/1381612822666160810120359

subject

Has Abstract

pub_date

2016-01-01 00:00:00

pages

5817-5829

issue

38

eissn

1381-6128

issn

1873-4286

pii

CPD-EPUB-77673

journal_volume

22

pub_type

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