Publications

Publications Search

Search for publications by author
Search for publications by abstract keyword(s)

Changes in cell morphology guide identification of tubulin as the off-target for protein kinase inhibitors

Abstract

In the field of kinase inhibitors for applications in cancer research, tubulin is emerging as a targeted cellular protein that can significantly contribute to their activities. However, investigation of kinase inhibitors beyond the kinome is an area often neglected. Herein, we describe the results of pharmacological studies using drugs targeting kinases, tubulin or both. A key finding is that if cells are treated with a kinase inhibitor unintentionally targeting tubulin, their characteristic shape will diminish within a short timeframe. These changes in cell morphology are not seen when cells are treated with bona fide kinase inhibitors that do not directly target tubulin. Thus, early changes in cell morphology upon treatments are a strong indication that the inhibitor is directly targeting tubulin. Recognizing tubulin as a target of kinase inhibitors will build confidence in the future mechanistic studies using kinase inhibitors.

Type Journal
ISBN 1096-1186 (Electronic) 1043-6618 (Linking)
Authors Hoque, M.; Abbassi, R. H.; Froio, D.; Man, J.; Johns, T. G.; Stringer, B. W.; Day, B. W.; Pajic, M.; Kassiou, M.; Munoz, L.
Responsible Garvan Author Dr Marina Pajic
Publisher Name PHARMACOLOGICAL RESEARCH
Published Date 2018-06-23
Published Volume 134
Published Pages 166-178
Status Published in-print
DOI 10.1016/j.phrs.2018.06.023
URL link to publisher's version https://www.ncbi.nlm.nih.gov/pubmed/29944980