Specific inhibitor of puromycin-sensitive aminopeptidase with a homophthalimide skeleton: Identification of the target molecule and a structure-activity relationship study

Masato Komoda; Hiroki Kakuta; Hiroyasu Takahashi; Yasuyuki Fujimoto; Shizuo Kadoya; Fuminori Kato; Yuichi Hashimoto

doi:10.1016/S0968-0896(00)00231-5

Specific inhibitor of puromycin-sensitive aminopeptidase with a homophthalimide skeleton: Identification of the target molecule and a structure-activity relationship study

Masato Komoda, Hiroki Kakuta, Hiroyasu Takahashi, Yasuyuki Fujimoto, Shizuo Kadoya, Fuminori Kato, Yuichi Hashimoto

Research output: Contribution to journal › Article › peer-review

60 Citations (Scopus)

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	https://doi.org/10.1016/S0968-0896(00)00231-5
Publication status	Published - Jan 8 2001
Externally published	Yes

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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10.1016/S0968-0896(00)00231-5

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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, 08.01.2001, p. 121-131.

Research output: Contribution to journal › Article › peer-review

Komoda, M, Kakuta, H, Takahashi, H, Fujimoto, Y, Kadoya, S, Kato, F & Hashimoto, Y 2001, 'Specific inhibitor of puromycin-sensitive aminopeptidase with a homophthalimide skeleton: Identification of the target molecule and a structure-activity relationship study', Bioorganic and Medicinal Chemistry, vol. 9, no. 1, pp. 121-131. https://doi.org/10.1016/S0968-0896(00)00231-5

Komoda, Masato ; Kakuta, Hiroki ; Takahashi, Hiroyasu ; Fujimoto, Yasuyuki ; Kadoya, Shizuo ; Kato, Fuminori ; Hashimoto, Yuichi. / Specific inhibitor of puromycin-sensitive aminopeptidase with a homophthalimide skeleton : Identification of the target molecule and a structure-activity relationship study. In: Bioorganic and Medicinal Chemistry. 2001 ; Vol. 9, No. 1. pp. 121-131.

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