TAS-116, a Highly Selective Inhibitor of Heat Shock Protein 90α and β, Demonstrates Potent Antitumor Activity and Minimal Ocular Toxicity in Preclinical Models
TAS-116, a Highly Selective Inhibitor of Heat Shock Protein 90α and β, Demonstrates Potent Antitumor Activity and Minimal Ocular Toxicity in Preclinical Models
S. Ohkubo,Y. Kodama,10 Authors,K. Yonekura
2014 · DOI: 10.1158/1535-7163.MCT-14-0219
Molecular Cancer Therapeutics · 111 Citations
TLDR
Oral administration of TAS-116 led to tumor shrinkage in human tumor xenograft mouse models accompanied by depletion of multiple HSP90 clients, demonstrating that the inhibition of H SP90α and β alone was sufficient to exert antitumor activity in certain tumor models.