Journal
ADVANCED DRUG DELIVERY REVIEWS
Volume 65, Issue 13-14, Pages 1828-1851Publisher
ELSEVIER
DOI: 10.1016/j.addr.2013.09.002
Keywords
ATP-binding casette superfamily pumps (ABCs); Multidrug resistance; Cancer; Infectious diseases; Generally Recognized As Safe (GRAS); pharmaceutical excipients; Nanopharmaceuticals; Polymeric amphiphiles
Categories
Ask authors/readers for more resources
Pumps of the ATP-binding cassette superfamily (ABCs) regulate the access of drugs to the intracellular space. In this context, the overexpression of ABCs is a well-known mechanism of multidrug resistance (MDR) in cancer and infectious diseases (e.g., viral hepatitis and the human immunodeficiency virus) and is associated with therapeutic failure. Since their discovery, ABCs have emerged as attractive therapeutic targets and the search of compounds that inhibit their genetic expression and/or their functional activity has gained growing interest. Different generations of pharmacological ABC inhibitors have been explored over the last four decades to address resistance in cancer, though clinical results have been somehow disappointing. Generally Recognized As Safe (GRAS) is a U.S. Food and Drug Administration designation for substances that are accepted as safe for addition in food. Far from being inert, some amphiphilic excipients used in the production of pharmaceutical products have been shown to inhibit the activity of ABCs in MDR tumors, emerging as a clinically translatable approach to overcome resistance. The present article initially overviews the classification, structure and function of the different ABCs, with emphasis on those pumps related to drug resistance. Then, the different attempts to capitalize on the activity of GRAS nanopharmaceuticals as ABC inhibitors are discussed. (C) 2013 Elsevier B.V. All rights reserved.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available