Receptor Tyrosine Kinase Inhibition, Hypertension, and Proteinuria

Receptor tyrosine kinase inhibition, hypertension, and proteinuria: is endothelin the smoking gun?

Angiogenesis is a key feature in the development and progression of malignancy, and antiangiogenic therapies are now well established as a cornerstone in the treatment of several cancers.1 Vascular endothelial growth factor (VEGF) not only drives angiogenesis but also acts as a survival factor for endothelial cells and promotes the abnormal phenotype of blood vessels in malignancy.2 By contrast...

Editorial Commentary Receptor Tyrosine Kinase Inhibition, Hypertension, and Proteinuria Is Endothelin the Smoking Gun?

Angiogenesis is a key feature in the development and progression of malignancy, and antiangiogenic therapies are now well established as a cornerstone in the treatment of several cancers.1 Vascular endothelial growth factor (VEGF) not only drives angiogenesis but also acts as a survival factor for endothelial cells and promotes the abnormal phenotype of blood vessels in malignancy.2 By contrast...

Receptor Tyrosine Kinase Inhibitory Activities and Molecular Docking Studies of Some Pyrrolo[2,3-d]pyrimidine Derivatives

In this study, we aimed to determine VEGFR-2, EGFR and PDGFR-β tyrosine kinase inhibitory activities of some pyrrolo[2,3-d]pyrimidine derivatives previously synthesized and showed potent cytotoxic and apoptotic effects against several cancer cell lines by our group and to evaluate the relationships between inhibitory activities and binding properties of the active compounds by molecular docking...

Inhibition of c-kit receptor tyrosine kinase activity by STI 571, a selective tyrosine kinase inhibitor.

STI 571 (formerly known as CGP 57148B) is a known inhibitor of the c-abl, bcr-abl, and platelet-derived growth-factor receptor (PDGFR) tyrosine kinases. This compound is being evaluated in clinical trials for the treatment of chronic myelogenous leukemia. We sought to extend the activity profile of STI 571 by testing its ability to inhibit the tyrosine kinase activity of c-kit, a receptor struc...

Inhibition of Tyrosine Kinase Activation