title: Receptor tyrosine kinase inhibitors: Are they real tumor killers?
abstract: Inhibiting tumor growth by targeting the tumor vasculature was first proposed by Judah Folkman almost 40 years ago. Since then, different approaches and numerous drugs and agents have been developed to achieve this goal, either with the aim of inhibiting tumor neoangiogenesis or normalizing the tumor vasculature. Among the most promising therapeutic targets are receptor tyrosine kinases (RTKs), some of which are predominantly expressed on tumor endothelial cells, although they are sometimes also present on tumor cells. The majority of RTK inhibitors investigated over the past two decades competes with ATP at the active site of the kinase and therefore block the phosphorylation of intracellular targets. Some of these drugs have been approved for therapy, whereas others are still in clinical trials. Here, we discuss the scientific basis, current status, problems and future prospects of RTK inhibition in anti-tumor therapy.
authors.affiliation: Institute of Pathology Kaufbeuren-Ravensburg, Kaufbeuren, Germany.|Institute of Pathology, University of Regensburg, Medical Center, Regensburg, Germany.
authors.forename: Andreas K A
authors.initials: AK
authors.lastname: Gaumann
authors.affiliation: Mammalian Cell Signaling Laboratory, Max Planck Institute for Molecular Biomedicine, Münster, North Rhine-Westphalia, Germany.
authors.forename: Friedemann
authors.initials: F
authors.lastname: Kiefer
authors.affiliation: Institute of Pathology Kaufbeuren-Ravensburg, Kaufbeuren, Germany.
authors.forename: Joachim
authors.initials: J
authors.lastname: Alfer
authors.affiliation: Department of Surgery, University of Regensburg, Medical Center, Regensburg, Germany.
authors.forename: Sven A
authors.initials: SA
authors.lastname: Lang
authors.affiliation: Department of Surgery, University of Regensburg, Medical Center, Regensburg, Germany.
authors.forename: Edward K
authors.initials: EK
authors.lastname: Geissler
authors.affiliation: Institute of Pathology, Technical University Dresden, Dresden, Germany.
authors.forename: Georg
authors.initials: G
authors.lastname: Breier
mesh_terms: D020533:Angiogenesis Inhibitors / Q000494:pharmacology; D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D019008:Drug Resistance, Neoplasm; D006801:Humans; D051379:Mice; D009362:Neoplasm Metastasis; D047428:Protein Kinase Inhibitors / Q000494:pharmacology*; D020794:Receptor Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors*
chemical_list: D020533:Angiogenesis Inhibitors; D000970:Antineoplastic Agents; D047428:Protein Kinase Inhibitors; D020794:Receptor Protein-Tyrosine Kinases
keywords: VEGF receptor; receptor tyrosine kinase; small molecule inhibitor; tumor angiogenesis