TY - JOUR
T1 - An apoptosis-inducing small molecule that binds to heat shock protein 70
AU - Williams, Darren R.
AU - Ko, Sung Kyun
AU - Park, Sungjin
AU - Lee, Myung Ryul
AU - Shin, Injae
PY - 2008/9/15
Y1 - 2008/9/15
N2 - (Chemical Equation Presented) A cell-based screening approach in which annexin V was used as a staining agent identified apoptozole (Az; see scheme) as an imidazole-based molecule which induces apoptosis. Az binds to Hsc70 and Hsp70 (anti-apoptotic chaperone proteins), with dissociation constants of 0.21 and 0.14 μm, respectively, thereby inhibiting their function. Thus, Az possesses antitumor activity and is, therefore, a potential cancer therapeutic agent.
AB - (Chemical Equation Presented) A cell-based screening approach in which annexin V was used as a staining agent identified apoptozole (Az; see scheme) as an imidazole-based molecule which induces apoptosis. Az binds to Hsc70 and Hsp70 (anti-apoptotic chaperone proteins), with dissociation constants of 0.21 and 0.14 μm, respectively, thereby inhibiting their function. Thus, Az possesses antitumor activity and is, therefore, a potential cancer therapeutic agent.
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U2 - 10.1002/anie.200802801
DO - 10.1002/anie.200802801
M3 - Article
C2 - 18729127
AN - SCOPUS:54749143530
SN - 1433-7851
VL - 47
SP - 7466
EP - 7469
JO - Angewandte Chemie - International Edition
JF - Angewandte Chemie - International Edition
IS - 39
ER -