Identification of mitoxantrone as a new inhibitor of ROS1 fusion protein in non-small cell lung cancer cells

  • Medchemcomm. 2017 Jan 26;8(3):621-624. doi: 10.1039/c6md00643d.
Lian-Xiang Luo  1 ,  Xing-Xing Fan  1 ,  Ying Li  1 ,  Xia Peng  2 ,  Yin-Chun Ji  2 ,  Wendy Wen-Luan Hsiao  1 ,  Liang Liu  1 ,  Elaine Lai-Han Leung  1 ,  Xiao-Jun Yao  1
Affiliations
  • 1. State Key Laboratory of Quality Research in Chinese Medicine, Macau Institute For Applied Research in Medicine and Health , Macau University of Science and Technology , Macau SAR , China . Email: [email protected] ; Email: [email protected] ; Email: [email protected] ; ; Tel: +853 8897 2438.
  • 2. State Key Laboratory of Drug Research , Shanghai Institute of Materia Medica , Chinese Academic of Sciences , Shanghai , China.
Abstract

Mitoxantrone, an FDA-approved drug for Multiple Sclerosis and hormone refractory Prostate Cancer, is identified as a potent inhibitor of ROS1 fusion protein by in silico screening in Non-Small Cell Lung Cancer cells. Mitoxantrone can suppress the phosphorylation of ROS1 and subsequently inhibit its downstream signaling pathway and thus induce cell Apoptosis.