title: Kinase inhibitor conjugates.
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.
authors.affiliation: Department of Pharmaceutics, Utrecht Institute of Pharmaceutical Sciences, Utrecht University, Utrecht, the Netherlands.
authors.forename: Stefan
authors.initials: S
authors.lastname: Harmsen
authors.forename: Robbert Jan
authors.initials: RJ
authors.lastname: Kok
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000009:adverse effects / Q000494:pharmacology; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems; D019008:Drug Resistance, Neoplasm; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy / Q000201:enzymology; D047428:Protein Kinase Inhibitors / Q000009:adverse effects / Q000494:pharmacology*; D011494:Protein Kinases / Q000187:drug effects* / Q000378:metabolism; D015398:Signal Transduction / Q000187:drug effects
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D047428:Protein Kinase Inhibitors; D011494:Protein Kinases