Lifescience Global

Editor’s Choice : The Reciprocal Interaction of Small Molecule Protein Kinase Inhibitors and ATP-Binding Cassette Transporters in Targeted Cancer Therapy

Cancer-Research-UpdatesWEB

The Reciprocal Interaction of Small Molecule Protein Kinase Inhibitors and ATP-Binding Cassette Transporters in Targeted Cancer Therapy
Pages 68-86
Hong-Ye Zhao, Hongjiang Wei and Xin Wang

DOI: http://dx.doi.org/10.6000/1929-2279.2013.02.01.8

Published: 14 February 2013 


Abstract: Protein kinaseshave become the second most important group of drug targets, after G-protein-coupled receptors. Currently,15 small molecule protein kinase inhibitors (PKIs) have received food and drug administrator (FDA) approval to be used as cancer treatments. However, in the course of clinical use of these small molecule PKIs, drug resistance has become a recurring problem. Their therapeutic potential depends on access to their intracellular targets, which significantly affected by certain membrane ATP-binding cassette(ABC) transporters. ABC transporters were major causesof clinical multiple drug resistance (MDR) and might be resulting in the development of resistance to PKIs in cancer patients. Some PKIs could modulate the activity of ABC transporters and affect the metabolism of themselves and other chemically unrelated drugs. Moreover, it has been recently reported that some PKIs could regulate the expression of ABC transporters in tumor cells, thereby affect their intracellular accumulation and antitumor efficacy. In this review,the reciprocal interaction of clinically important PKIs with the MDR-related ABC transporters, in particular ABCB1 and ABCG2,wassummarized.

Keywords: Protein Kinase Inhibitors, ABC Transporters, P-gp/ABCB1, BCRP/ABCG2, Targeted Cancer Therapy.
Download Full Article
Submit to FacebookSubmit to Google PlusSubmit to TwitterSubmit to LinkedIn

OUR STRENGTHS

♦  Worldwide readership
♦  High quality content
♦  Maximum visibility
♦  Efficient publishing
♦  Optional Open Access

Publish your Research

Survey

As an author what type of publishing model you prefer?

780
Open Access
493
Optional Open Access
338
Subscription based
5 Votes left