TY - JOUR
T1 - Specific inhibitor of puromycin-sensitive aminopeptidase with a homophthalimide skeleton
T2 - Identification of the target molecule and a structure-activity relationship study
AU - Komoda, Masato
AU - Kakuta, Hiroki
AU - Takahashi, Hiroyasu
AU - Fujimoto, Yasuyuki
AU - Kadoya, Shizuo
AU - Kato, Fuminori
AU - Hashimoto, Yuichi
N1 - Funding Information:
The work described in this paper was partially supported by funds for the Promotion of Fundamental Studies in Health Science from the Organization for Pharmaceutical Safety Research, and Grants-in-Aid from the Ministry of Education, Science, Sports, and Culture of Japan. The authors are grateful to Dr. Naoko Morisaki and Dr. Hisayoshi Kobayashi (IMCB, University of Tokyo) for their assistance.
PY - 2001
Y1 - 2001
N2 - 2-(2,6-Diethylphenyl)-1,2,3,4-tetrahydroisoquinoline-1,3-dione (2: PIQ-22) was found to be a potent and specific inhibitor of puromycin-sensitive aminopeptidase (PSA). Lineweaver-Burk plot analysis showed that PSA is inhibited by PIQ-22 in a non-competitive manner. Structure-activity relationship studies indicated that tautomerism of the imidobenzoylketone group in the cyclic imide moiety of the PIQ-22 skeleton is important for the inhibitory activity.
AB - 2-(2,6-Diethylphenyl)-1,2,3,4-tetrahydroisoquinoline-1,3-dione (2: PIQ-22) was found to be a potent and specific inhibitor of puromycin-sensitive aminopeptidase (PSA). Lineweaver-Burk plot analysis showed that PSA is inhibited by PIQ-22 in a non-competitive manner. Structure-activity relationship studies indicated that tautomerism of the imidobenzoylketone group in the cyclic imide moiety of the PIQ-22 skeleton is important for the inhibitory activity.
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U2 - 10.1016/S0968-0896(00)00231-5
DO - 10.1016/S0968-0896(00)00231-5
M3 - Article
C2 - 11197332
AN - SCOPUS:0035185530
VL - 9
SP - 121
EP - 131
JO - Bioorganic and Medicinal Chemistry
JF - Bioorganic and Medicinal Chemistry
SN - 0968-0896
IS - 1
ER -