Joseph P. Errico,Benjamin Mugrage,Ignatius Turchi,Matthew Sills,Jane Ong,John Allocco,Pam Wines
申请号:
US14096618
公开号:
US09073858B2
申请日:
2013.12.04
申请国别(地区):
US
年份:
2015
代理人:
摘要:
Provided herein are compounds having anti-proliferative effect. Also provided are compounds that can modulate the activity of multi-domain proteins comprising a dimerization arm and interdomain tether, such as EGFR, where an untethered, extended conformation is the active state and a tethered conformation is the inactive state, resulting in an autoinhibited configuration. Also provided are methods and pharmacophores for identifying such compounds. Other aspects provide methods or therapeutic treatment for proliferative diseases, disorders, or conditions, such as those associated with EGFR.