Ontology highlight
ABSTRACT:
SUBMITTER: Wieczorek M
PROVIDER: S-EPMC5291303 | biostudies-literature | 2016 Nov
REPOSITORIES: biostudies-literature
Wieczorek Michal M Tcherkezian Joseph J Bernier Cynthia C Prota Andrea E AE Chaaban Sami S Rolland Yannève Y Godbout Claude C Hancock Mark A MA Arezzo Joseph C JC Ocal Ozhan O Rocha Cecilia C Olieric Natacha N Hall Anita A Ding Hui H Bramoullé Alexandre A Annis Matthew G MG Zogopoulos George G Harran Patrick G PG Wilkie Thomas M TM Brekken Rolf A RA Siegel Peter M PM Steinmetz Michel O MO Shore Gordon C GC Brouhard Gary J GJ Roulston Anne A
Science translational medicine 20161101 365
Microtubule-targeting agents (MTAs) are widely used anticancer agents, but toxicities such as neuropathy limit their clinical use. MTAs bind to and alter the stability of microtubules, causing cell death in mitosis. We describe DZ-2384, a preclinical compound that exhibits potent antitumor activity in models of multiple cancer types. It has an unusually high safety margin and lacks neurotoxicity in rats at effective plasma concentrations. DZ-2384 binds the vinca domain of tubulin in a distinct w ...[more]