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Biochemistry, Biophysics, and Structural Biology

Nova Southeastern University

Kinase inhibitors

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Full-Text Articles in Life Sciences

Effect Of Egf-Receptor Tyrosine Kinase Inhibitor On Rab5 Function During Endocytosis, Ivan Jozic, Samar C. Saliba, M. Alejandro Barbieri Sep 2012

Effect Of Egf-Receptor Tyrosine Kinase Inhibitor On Rab5 Function During Endocytosis, Ivan Jozic, Samar C. Saliba, M. Alejandro Barbieri

Biology Faculty Articles

Tyrosine autophosphorylation within the cytoplasmic tail of EGF-receptor is a key event, which in turn recruits several factors including Shc, Grb2 and Rin1 that are essential activities for receptor-mediated endocytosis and signaling. In this study, we demonstrated that treatment with AG1478, an EGF-receptor kinase inhibitor, blocked the formation of Rab5-positive endosomes as well as the activation of Rab5 upon addition of EGF. We also found that EGF-receptor catalytically inactive mutant failed to activate Rab5 upon EGF stimulation. Additionally, endosomal co-localization of Rab5 and EGF-receptor was inhibited by AG1478. Interestingly, AG1478 inhibitor did not block the formation of enlarged Rab5-positive endosomes …