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Tyrosine Kinase Inhibitors

Current Cancer Drug Targets, 2010
Over the last ten years, several new and therapeutically relevant cancer drugs targeting tyrosine kinases signaling pathways have been developed. Tyrosine kinase inhibitors (TKIs) are a pharmaceutical class of small molecules, orally available, well-tolerated, worldwide approved drugs for the treatment of several neoplasms, including lung, breast ...
NATOLI, Clara   +5 more
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Inhibitors of tyrosine kinase

Current Opinion in Oncology, 1997
This review covers the literature on significant studies of small molecule inhibitors of the epidermal growth factor receptor (EGFR), platelet-derived growth factor receptor (PDGFR), fibroblast growth factor receptor (FGFR), Flk-1, and src family tyrosine kinases from 1996 through mid-1997. During this period, there has been substantial progress in the
W D, Klohs, D W, Fry, A J, Kraker
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FLT3 Tyrosine Kinase Inhibitors

International Journal of Hematology, 2005
The receptor tyrosine kinase FLT3 is an important regulatory molecule in hematopoiesis and is expressed on the blasts in most cases of acute leukemia. Activating mutations of this receptor are present in roughly 30% of acute myeloid leukemia (AML) patients and are associated with a distinctly worse clinical outcome.
Mark, Levis, Donald, Small
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Tyrosine Kinase Inhibitors

2016
Breast cancer is the most common cancer in women worldwide. Although various subgroups are defined according to the expression of hormones and ErbB family receptors, it is well known that this disease is more heterogeneous than its classification system suggests.
Cakar B., Göker E.
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Tyrosine Kinase Inhibitors

Bulletin du cancer, 2012
Membrane receptors with tyrosine kinase activity and cytoplasmic tyrosine kinases have emerged as important potential targets in oncology. Starting from basic structures such as anilino-quinazoline, numerous compounds have been synthesised, with the help of tyrosine kinase crystallography, which has allowed to optimise protein-ligand interactions.
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Tyrosine kinase inhibitor induced pancreatitis

Journal of Oncology Pharmacy Practice, 2012
Sorafenib and sunitinib are oral tyrosine kinase inhibitors, commonly used in the treatment of metastatic renal cell carcinoma. Known adverse events associated with tyrosine kinase inhibitors include hypertension and palmarplantar erythrodysesthesia. We report two cases of acute pancreatitis associated with tyrosine kinase inhibitors.
Adrienne, Sevin   +2 more
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HER-Targeted Tyrosine-Kinase Inhibitors

Oncology, 2002
Improved 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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Forthcoming receptor tyrosine kinase inhibitors

Expert Opinion on Therapeutic Targets, 2006
Receptor 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.
Nicholas W, Choong, Ezra E W, Cohen
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Tyrosine kinase inhibitors—ZD1839 (Iressa)

Current Opinion in Oncology, 2001
Several 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.
C L, Arteaga, D H, Johnson
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Tyrosine kinase inhibitors.

Seminars in cancer biology, 1993
Tyrosine kinases are associated with the cytoplasmic domains of growth factor receptors as well as oncoproteins and many have the potential to cause transformation if mutated or hyperexpressed. Tyrosine kinases therefore represent an excellent target for the development of cancer drugs.
P, Workman, V G, Brunton, D J, Robins
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