Unfolded protein response in cancer: IRE1α inhibition by selective kinase ligands does not impair tumor cell viability

ACS Medicinal Chemistry Letters

Volumn 6, Issue 1, 2015, Pages 68-72

  Harrington, Paul E ^a   Biswas, Kaustav ^a   Malwitz, David ^a,c   Tasker, Andrew S ^a   Mohr, Christopher ^a   Andrews, Kristin L ^a   Dellamaggiore, Ken ^a   Kendall, Richard ^a   Beckmann, Holger ^b   Jaeckel, Peter ^b   Materna Reichelt, Silvia ^b   Allen, Jennifer R ^a   Lipford, J Russell ^a  

^a AMGEN INC   (United States)

^b Amgen Research GmbH   (Germany)

^c JANSSEN RESEARCH AND DEVELOPMENT   (Belgium)

Author keywords

inhibitor; IRE1 ; kinase; Unfolded protein response

Indexed keywords

BENZIMIDAZOLE; ENDONUCLEASE; ENZYME INHIBITOR; INOSITOL REQUIRING ENZYME 1ALPHA; PROTEIN; RIBONUCLEASE; SULFONAMIDE; UNCLASSIFIED DRUG;

ALPHA HELIX; ARTICLE; CARCINOGENESIS; CELL SURVIVAL; CELL VIABILITY; CONTROLLED STUDY; CRYSTAL STRUCTURE; DOSE RESPONSE; ENDOPLASMIC RETICULUM; ENZYME ACTIVITY; ENZYME INHIBITION; HUMAN; IN VITRO STUDY; NEOPLASM; PRIORITY JOURNAL; STRUCTURE ACTIVITY RELATION; TUMOR CELL LINE; UNFOLDED PROTEIN RESPONSE; X RAY;

EID: 84920722468     PISSN: None     EISSN: 19485875     Source Type: Journal    
DOI: 10.1021/ml500315b     Document Type: Article

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16. 50) was not validated in confirmation studies.
17. See Supporting Information for assay details.
18. A detailed full account of these results will be disclosed separately (manuscript in preparation).