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Current Pharmaceutical Design

Editor-in-Chief

ISSN (Print): 1381-6128
ISSN (Online): 1873-4286

Kinase Inhibitor Conjugates

Author(s): Stefan Harmsen and Robbert Jan Kok

Volume 18 , Issue 20 , 2012

Page: [2891 - 2900] Pages: 10

DOI: 10.2174/138161212800672778

Price: $65

Abstract

In the last decade kinase inhibitors have emerged as a new class of very potent and relatively safe anticancer drugs. However, despite their success, off-target toxicities and induction of rapid resistance are major drawbacks that highly compromise successful longterm administration. In the current review, we provide an overview of the approaches that have been undertaken to overcome these issues by conjugation of these agents to carriers that enable their cellular and/or intracellular targeted delivery. Eventually, targeting kinase inhibitors will provide powerful treatment options not only for cancer, but also for other less-life threatening diseases that involve deregulated kinase signaling pathways.

Keywords: Drug targeting, kinase inhibitors, conjugation, drug resistance, off-organ toxicity, anticancer drugs, long-term administration, intracellular targeted delivery, kinase signaling pathways, CML patients


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