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Selective tyrosine kinase inhibitors
Emerging Drugs, 2000The tyrosine specific protein kinases (TK) are a subgroup of the largest known gene family, the kinases. Latest estimates suggest that there are over 2000 kinases encoded in the human genome [1]. TKs catalyse the transfer of phosphate to the phenolic hydroxyl of tyrosine residues in substrate proteins, consequently modifying the target protein ...
Sandra E. Wilkinson, Harris William
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Cardiovascular toxicity of tyrosine kinase inhibitors
Expert Opinion on Drug Safety, 2013Small-molecule tyrosine kinase inhibitors (TKIs) have revolutionized the management of many malignancies. However, they also have been shown to be associated with a certain degree of cardiovascular side effects that are often reversible.As the number of new TKIs continues to grow, it is expected that clinicians will be facing the challenge of early ...
Jorge E. Cortes +2 more
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Imatinib: a selective tyrosine kinase inhibitor
European Journal of Cancer, 2002The understanding of the pathophysiology of a large number of cancer types provides a strategy to target cancer cells with minimal effect on normal cells. Protein phosphorylation and dephosphorylation play a pivotal role in intracellular signaling; to regulate signal transduction pathways, there are approximately 700 protein kinases and 100 protein ...
G. Fendrich +7 more
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Are catechins natural tyrosine kinase inhibitors?
Drug News & Perspectives, 2002Enhanced activity of tyrosine kinase receptors (RTKs) has been implicated as a contributing factor in the development of malignant and nonmalignant proliferative diseases such as cancer and atherosclerosis. Several growth factors traducing mitogenic signals through RTKs are implicated in the development of tumor and cardiovascular diseases.
Jürgen Hescheler, Agapios Sachinidis
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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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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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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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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—ZD1839 (Iressa)
Current Opinion in Oncology, 2001Several epithelial tumors display epidermal growth factor receptor (EGFR) overexpression (with or without EGFR gene amplification) that is often associated with increased production of EGFR ligands. This permits the activation of endogenous tumor EGFR via autocrine mechanisms, resulting in cellular proliferation and tumor growth.
David H. Johnson, Carlos L. Arteaga
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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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