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HER-Targeted Tyrosine-Kinase Inhibitors
Oncology, 2002Improved understanding of tumor biology has led to the identification of numerous growth factors that are involved in malignant transformation and tumor progression. Many of these factors induce cellular responses through receptors with intrinsic tyrosine kinase (TK) activity. Therefore, inhibiting receptor TK activity is a way to effectively block the
José Baselga, Lisa A. Hammond
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Tyrosine kinase inhibitors: A clinical perspective
Current Oncology Reports, 2002Cancer treatment has so far been restricted to cytotoxic and hormonal agents. These have been of limited value in their efficacy and their toxicity profile. A new era of targeted therapies is rapidly evolving. A key target being actively pursued is the receptor tyrosine kinase.
Sanjay Goel +2 more
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2007
The extraordinary success of imatinib for the treatment of chronic myeloid leukemia (CML), gastrointestinal stromal tumors and subgroups of patients with hypereosinophilic syndrome and chronic myelomonocytic leukemia has greatly stimulated the development of small molecule inhibitors for targeted therapy of malignant diseases.
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The extraordinary success of imatinib for the treatment of chronic myeloid leukemia (CML), gastrointestinal stromal tumors and subgroups of patients with hypereosinophilic syndrome and chronic myelomonocytic leukemia has greatly stimulated the development of small molecule inhibitors for targeted therapy of malignant diseases.
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Tyrosine Kinase Inhibitors: The First Decade
Current Hematologic Malignancy Reports, 2010The treatment of chronic myeloid leukemia (CML) drastically changed with the introduction of imatinib mesylate, a Bcr-Abl1 tyrosine kinase inhibitor (TKI), in 1998. By directly targeting this leukemogenic protein kinase, imatinib affords patients with CML sustained chromosomal remissions, which translate into prolonged survival. However, there has been
Meetu Agrawal +3 more
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Future Oncology, 2015
Ten years ago, somatic mutations in EGFR were identified in patients with non-small-cell lung cancer. Demonstration of the antitumor efficacy of EGF receptor-directed tyrosine kinase inhibitors resulted in their approval for the treatment of advanced non-
N. Reguart, J. Remon
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Ten years ago, somatic mutations in EGFR were identified in patients with non-small-cell lung cancer. Demonstration of the antitumor efficacy of EGF receptor-directed tyrosine kinase inhibitors resulted in their approval for the treatment of advanced non-
N. Reguart, J. Remon
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Forthcoming receptor tyrosine kinase inhibitors
Expert Opinion on Therapeutic Targets, 2006Receptor tyrosine kinases play a significant role in carcinogenesis and have been successfully targeted with monoclonal antibodies and small-molecule inhibitors. There have been recent developments in the understanding of receptor tyrosine kinase signal transduction which have enabled better drug development.
Ezra E.W. Cohen, Nicholas W. Choong
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Tyrosine Kinase Inhibitors in Preclinical Development
Investigational New Drugs, 1999Due to the limited efficacy of cytotoxic chemotherapy in the treatment of advanced malignancy and its excessive toxicity precluding its use in chemoprevention, new therapeutic and preventive strategies have been sought. One of the most interesting of these new approaches is the manipulation of signal transduction pathways.
Patrick P. Koty, Mark L. Levitt
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Clinical pharmacokinetics of tyrosine kinase inhibitors
Cancer Treatment Reviews, 2009In the recent years, eight tyrosine kinase inhibitors (TKIs) have been approved for cancer treatment and numerous are under investigation. These drugs are rationally designed to target specific tyrosine kinases that are mutated and/or over-expressed in cancer tissues.
Henk-Jan Guchelaar +2 more
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Treatment with Tyrosine Kinase Inhibitors [PDF]
, 2007 Leukemias have traditionally served as model systems for research on neoplasia because of the easy availability of cell material from blood and marrow for diagnosis, monitoring, and studies on pathophysiology. Beyond these more technical aspects, chronic myeloid leukemia (CML) became the first neoplasia in which the elucidation of the genotype led to a
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