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 - 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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Cite this
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, 9(1), 121-131. https://doi.org/10.1016/S0968-0896(00)00231-5