Receptor tyrosine kinase inhibitors: Are they real tumor killers?

Gaumann, Andreas K. A. and Kiefer, Friedemann and Alfer, Joachim and Lang, Sven A. and Geissler, Edward K. and Breier, Georg (2016) Receptor tyrosine kinase inhibitors: Are they real tumor killers? INTERNATIONAL JOURNAL OF CANCER, 138 (3). pp. 540-554. ISSN 0020-7136, 1097-0215

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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.

Item Type: Article
Uncontrolled Keywords: ENDOTHELIAL-GROWTH-FACTOR; CELL LUNG-CANCER; MEDULLARY-THYROID CANCER; ADVANCED SOLID TUMORS; RANDOMIZED PHASE-II; ADVANCED COLORECTAL-CANCER; METASTATIC BREAST-CANCER; GASTROINTESTINAL STROMAL TUMORS; ORAL ANGIOGENESIS INHIBITOR; ADVANCED PANCREATIC-CANCER; VEGF receptor; receptor tyrosine kinase; small molecule inhibitor; tumor angiogenesis
Subjects: 600 Technology > 610 Medical sciences Medicine
Divisions: Medicine > Lehrstuhl für Chirurgie
Medicine > Lehrstuhl für Pathologie
Depositing User: Petra Gürster
Date Deposited: 03 Sep 2020 06:29
Last Modified: 03 Sep 2020 06:29
URI: https://pred.uni-regensburg.de/id/eprint/2489

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