Open Access. Powered by Scholars. Published by Universities.®
Articles 1 - 1 of 1
Full-Text Articles in Entire DC Network
Identification And Characterization Of A New Tubulin-Binding, Susan L. Mooberry, Kimberly N. Weiderhold, Sivanesan Dakshanamurthy, Ernest Hamel, Edith J. Banner, Anastasia Kharlamova, Jonathan Hempel, John T. Gupton, Milton L. Brown
Identification And Characterization Of A New Tubulin-Binding, Susan L. Mooberry, Kimberly N. Weiderhold, Sivanesan Dakshanamurthy, Ernest Hamel, Edith J. Banner, Anastasia Kharlamova, Jonathan Hempel, John T. Gupton, Milton L. Brown
Chemistry Faculty Publications
We studied the mechanism of action of 3,5-dibromo-4-(3,4-dimethoxyphenyl)-1H-pyrrole-2-carboxylic acid ethyl ester (JG-03-14) and found that it is a potent microtubule depolymerizer. JG-03-14 caused a dose-dependent loss of cellular microtubules, formation of aberrant mitotic spindles, accumulation of cells in the G2/M phase of the cell cycle, and Bcl-2 phosphorylation. These events culminated in the initiation of apoptosis, as evidenced by the caspase 3-dependent cleavage of poly(ADP-ribose) polymerase (PARP). JG-03-14 has antiproliferative activity against a wide range of cancer cell lines, with an average IC50 value of 62 nM, and it is a poor substrate for transport …