Characterization of a Novel PERK Kinase Inhibitor with Antitumor and Antiangiogenic Activity

• Published in: Cancer research (Chicago, Ill.) Vol. 73; no. 6; pp. 1993 - 2002
• Main Authors: Atkins, Charity, Liu, Qi, Minthorn, Elisabeth, Zhang, Shu-Yun, Figueroa, David J., Moss, Katherine, Stanley, Thomas B., Sanders, Brent, Goetz, Aaron, Gaul, Nathan, Choudhry, Anthony E., Alsaid, Hasan, Jucker, Beat M., Axten, Jeffrey M., Kumar, Rakesh
• Format: Journal Article
• Language: English
• Published: Philadelphia, PA American Association for Cancer Research 15.03.2013
• Subjects: Adenine - analogs & derivatives; Adenine - pharmacology; Angiogenesis Inhibitors - pharmacology; Animals; Antineoplastic agents; Antineoplastic Agents - pharmacology; Biological and medical sciences; eIF-2 Kinase - antagonists & inhibitors; Female; Gene Expression Profiling; Indoles - pharmacology; Medical sciences; Mice; Pharmacology. Drug treatments; Protein Kinase Inhibitors - pharmacology; Tumors; Antineoplastic agent; Characterization; Enzyme; Kinase; Transferases; Inhibitor; Antiangiogenic agent; Biological activity

The unfolded protein response (UPR) is a signal transduction pathway that coordinates cellular adaptation to microenvironmental stresses that include hypoxia, nutrient deprivation, and change in redox status. These stress stimuli are common in many tumors and thus targeting components of the UPR sig...