Abstract
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.
| Original language | English |
|---|---|
| Pages (from-to) | 121-131 |
| Number of pages | 11 |
| Journal | Bioorganic and Medicinal Chemistry |
| Volume | 9 |
| Issue number | 1 |
| DOIs | |
| Publication status | Published - 2001 |
| Externally published | Yes |
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ASJC Scopus subject areas
- Biochemistry
- Molecular Biology
- Organic Chemistry
- Drug Discovery
- Pharmaceutical Science
Cite this
Specific inhibitor of puromycin-sensitive aminopeptidase with a homophthalimide skeleton : Identification of the target molecule and a structure-activity relationship study. / Komoda, Masato; Kakuta, Hiroki; Takahashi, Hiroyasu; Fujimoto, Yasuyuki; Kadoya, Shizuo; Kato, Fuminori; Hashimoto, Yuichi.
In: Bioorganic and Medicinal Chemistry, Vol. 9, No. 1, 2001, p. 121-131.Research output: Contribution to journal › Article
}
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
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.
UR - http://www.scopus.com/inward/record.url?scp=0035185530&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=0035185530&partnerID=8YFLogxK
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 -