Characterization of the biological activity of a potent small molecule Hec1 inhibitor TAI-1.

ABSTRACT:

Background

Hec1 (NDC80) is an integral part of the kinetochore and is overexpressed in a variety of human cancers, making it an attractive molecular target for the design of novel anticancer therapeutics. A highly potent first-in-class compound targeting Hec1, TAI-1, was identified and is characterized in this study to determine its potential as an anticancer agent for clinical utility.

Methods

The in vitro potency, cancer cell specificity, synergy activity, and markers for response of TAI-1 were evaluated with cell lines. Mechanism of action was confirmed with western blotting and immunofluorescent staining. The in vivo potency of TAI-1 was evaluated in three xenograft models in mice. Preliminary toxicity was evaluated in mice. Specificity to the target was tested with a ki

SUBMITTER: Huang LY 

PROVIDER: S-EPMC3895848 | biostudies-literature | 2014 Jan

REPOSITORIES: biostudies-literature