TY - JOUR
T1 - A highly selective dual insulin receptor (IR)/insulin-like growth factor 1 receptor (IGF-1R) inhibitor derived from an extracellular signal-regulated kinase (ERK) inhibitor
AU - Anastassiadis, Theonie
AU - Duong-Ly, Krisna C.
AU - Deacon, Sean W.
AU - Lafontant, Alec
AU - Ma, Haiching
AU - Devarajan, Karthik
AU - Dunbrack, Roland L.
AU - Wu, Jinhua
AU - Peterson, Jeffrey R.
PY - 2013/9/27
Y1 - 2013/9/27
N2 - Background: IR/IGF-1R kinase inhibitors are promising therapeutic agents in cancer. Results: Irfin1, a compound closely related to the ERK inhibitor FR180204, inhibits IR/IGF-1R family kinases. Conclusion: Irfin1 is a remarkably selective inhibitor for the inactive states of IR/IGF-1R kinases. Significance: Broad spectrum kinase inhibitor profiling can be exploited to uncover novel targets of small-molecule compounds.
AB - Background: IR/IGF-1R kinase inhibitors are promising therapeutic agents in cancer. Results: Irfin1, a compound closely related to the ERK inhibitor FR180204, inhibits IR/IGF-1R family kinases. Conclusion: Irfin1 is a remarkably selective inhibitor for the inactive states of IR/IGF-1R kinases. Significance: Broad spectrum kinase inhibitor profiling can be exploited to uncover novel targets of small-molecule compounds.
UR - http://www.scopus.com/inward/record.url?scp=84884782820&partnerID=8YFLogxK
U2 - 10.1074/jbc.M113.505032
DO - 10.1074/jbc.M113.505032
M3 - Article
C2 - 23935097
AN - SCOPUS:84884782820
SN - 0021-9258
VL - 288
SP - 28068
EP - 28077
JO - Journal of Biological Chemistry
JF - Journal of Biological Chemistry
IS - 39
ER -
