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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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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.
Nicholas W, Choong, Ezra E W, Cohen
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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.
C L, Arteaga, D H, Johnson
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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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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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Novel FLT3 tyrosine kinase inhibitors
Expert Opinion on Investigational Drugs, 2003Acute myeloid leukaemia (AML) is an aggressive haematological malignancy that is curable in approximately 40% of cases. Activating mutations of the receptor tyrosine kinase FLT3 (FMS-like tyrosine kinase-3) are the single most common molecular abnormalities in AML and are associated with a distinctly worse prognosis.
Mark, Levis, Donald, Small
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Inhibitors of protein tyrosine kinases
Current Opinion in Biotechnology, 1995The description in the past year of several novel protein tyrosine kinase inhibitors, which exhibit dramatic improvements in potency and specificity over earlier agents, will be considered a major turning point in the field. These compounds appear to have the necessary pharmacological properties to finally allow clarification of whether suppression of ...
D W, Fry, A J, Bridges
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Tyrosine Kinase Inhibitor-Induced Hypertension
Current Oncology Reports, 2018The purpose of this paper is to identify commonly used tyrosine kinase inhibitors (TKIs) that are associated with hypertension, primarily, vascular endothelial growth factor (VEGF) signaling pathway (VSP) inhibitors. We review the incidence, mechanism, and strategies for management of TKI-induced HTN.
Megha, Agarwal +4 more
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Tyrosine Kinase Inhibitors and Cancer Therapy
Clinical Biochemistry, 2004Cancer is the second leading cause of death in the western world. Despite advances in diagnosis and treatment, overall survival of patients remains poor. Scientific advances in recent years have enhanced our understanding of the biology of cancer. Human protein tyrosine kinases (PTKs) play a central role in human carcinogenesis and have emerged as the ...
Srinivasan, Madhusudan +1 more
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Receptor Tyrosine Kinase Inhibitors
2015Receptor tyrosine kinases (RTKs) are a diverse group of transmembrane proteins involved in signal transduction. Their function in many cell types is to drive a wide variety of cellular functions, including growth, differentiation and angiogenesis, by transducing growth factor signals from the external milieu to intracellular processes. In malignancies,
Antony M. Latham +2 more
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