Kinase inhibitor conjugates Journal Article


Authors: Harmsen, S.; Kok, R. J.
Article 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. © 2012 Bentham Science Publishers.
Keywords: signal transduction; unclassified drug; review; erlotinib; sunitinib; nonhuman; antineoplastic agents; drug targeting; neoplasms; animals; imatinib; enzyme inhibition; protein kinases; protein kinase inhibitor; drug structure; drug resistance; drug resistance, neoplasm; dasatinib; chronic myeloid leukemia; drug delivery systems; protein kinase inhibitors; gefitinib; vatalanib; target cell; nilotinib; arginylglycylaspartic acid; drug conjugation; drug delivery system; drug carrier; drug carriers; human serum albumin; conjugation; kinase inhibitors; lysozyme; off-organ toxicity; 4 (1 aminoethyl) n (4 pyridyl)cyclohexanecarboxamide; 4 (4 fluorophenyl) 2 (4 hydroxyphenyl) 5 (4 pyridyl)imidazole; [1 (4 oxo 8 phenyl 4h 1 benzopyran 2 yl)morpholinio]methoxysuccinylarginylglycylaspartylserine acetate; cell penetrating peptide; ly 364947; mannose 6 phosphate; polyamidoamine
Journal Title: Current Pharmaceutical Design
Volume: 18
Issue: 20
ISSN: 1381-6128
Publisher: Bentham Science Publishers  
Date Published: 2012-07-01
Start Page: 2891
End Page: 2900
Language: English
PROVIDER: scopus
PUBMED: 22571658
DOI/URL:
Notes: --- - "Cited By (since 1996): 1" - "Export Date: 2 July 2012" - "CODEN: CPDEF" - "Source: Scopus"
Citation Impact
MSK Authors
  1. Stefan Harmsen
    17 Harmsen