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6 Protein Tyrosine Kinase Inhibitors
1996Publisher Summary This chapter describes the classification and structure of protein tyrosine kinases (PTKs), their mode of action, their cellular targets, and the processes in which they are involved. A vast amount of research has been carried out to try to identify the role of PTKs in the general functioning and development of normal mammalian ...
Kevin R. H. Solomons +3 more
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Tyrosine Kinase Inhibitors in Pediatric Malignancies
Cancer Investigation, 2007Tyrosine kinase inhibitors have been used to treat adult cancers for over a decade. Since the discovery of imatinib mesylate (STI-571, Gleevec; Novartis), tyrosine kinase inhibitors have ushered in a new age of targeted therapy. Although the United States Food and Drug Administration has approved several kinase inhibitors for use in adult cancers ...
Peter C. Adamson, Jeffrey M. Skolnik
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Tyrosine kinase inhibitor induced pancreatitis
Journal of Oncology Pharmacy Practice, 2012Sorafenib 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 H. Chen +2 more
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Tyrosine Kinase Inhibitors and Hepatocellular Carcinoma
Clinics in Liver Disease, 2020Sorafenib was the first tyrosine kinase inhibitor (TKI) that showed success in extending survival in patients with advanced hepatocellular carcinoma (HCC). In recent years, additional TKIs have been shown to improve survival and expanded the armamentarium for treating this malignancy.
Maria Reig +2 more
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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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Tyrphostins and Other Tyrosine Kinase Inhibitors [PDF]
Annual Review of Biochemistry, 2006 The development of tyrosine phosphorylation inhibitors has transformed the approach to cancer therapy and is likely to affect other fields of medicine. In spite of the conservation among protein tyrosine kinases (PTKs), one can develop small molecules that block the activity of a narrow spectrum of PTKs and that exhibit much less toxicity than the ...
Eyal Mishani, Alexander Levitzki
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Journal of Medicinal Chemistry, 2016
Heat shock protein 90 (Hsp90) is a ubiquitous chaperone of all of the oncogenic tyrosine kinases. Many Hsp90 inhibitors, alone or in combination, have shown significant antitumor efficacy against the kinase-positive naïve and mutant models.
Meining Wang +9 more
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Heat shock protein 90 (Hsp90) is a ubiquitous chaperone of all of the oncogenic tyrosine kinases. Many Hsp90 inhibitors, alone or in combination, have shown significant antitumor efficacy against the kinase-positive naïve and mutant models.
Meining Wang +9 more
semanticscholar +1 more source
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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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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