Structure-activity relationship studies of small-molecule inhibitors of Wnt response.
Suppression of oncogenic Wnt-mediated signaling holds promise as an anti-cancer therapeutic strategy. We previously reported a novel class of small molecules (IWR-1/2, inhibitors of Wnt response) that antagonize Wnt signaling by stabilizing the Axin destruction complex. Herein, we present the results of structure-activity relationship studies of these compounds.
Lu
Jianming
J
Department of Biochemistry, The University of Texas Southwestern Medical Center at Dallas, Dallas, TX 75390, USA.
Ma
Zhiqiang
Z
Hsieh
Jen-Chieh
JC
Fan
Chih-Wei
CW
Chen
Baozhi
B
Longgood
Jamie C
JC
Williams
Noelle S
NS
Amatruda
James F
JF
Lum
Lawrence
L
Chen
Chuo
C
D000634:Aminoquinolines / Q000737:chemistry*; D000818:Animals; D060466:Axin Protein; D007094:Imides / Q000737:chemistry*; D012097:Repressor Proteins / Q000378:metabolism; D015398:Signal Transduction; D013329:Structure-Activity Relationship; D013623:Tail; D051153:Wnt Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D015027:Zebrafish / Q000378:metabolism
D000634:Aminoquinolines; D060466:Axin Protein; D007094:Imides; D012097:Repressor Proteins; D051153:Wnt Proteins