| Synthesis of isoornithines and methylputrescines. An evaluation of their inhibitory effects on ornithine decarboxylase. | |
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MedLine Citation:
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PMID: 7473562 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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2-(Aminomethyl)-4-aminobutyric acid (isoornithine), 3-methylisoornithine, and 2,3-dimethylisoornithine were not decarboxylated by liver ornithine decarboxylase (ODC, EC 4.1.1.17) of thioacetamide-treated rats but were good competitive inhibitors of the enzyme (Ki ranged from 0.72 to 1.79 mM). When assayed in vivo in the treated rats, the above mentioned isoornithines were also found to inhibit liver ODC when administered 1 h before sacrifice. When the methylputrescines formally derived from the decarboxylation of several isoornithines were assayed on rat liver ODC, it was found that only 2,3-dimethylputrescine decreased the enzymatic activity. When assayed in vivo, it was found to decrease ODC activity by 60%, when the latter was measured 1 h after administration. The effect was reverted 4 h after administration of the drug. Isoornithines were not taken up by H-35 hepatoma cells; hence they did not affect their ODC activity. 2,3-Dimethylputrescine however, was transported into the cells and significantly decreased its ODC activity. |
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Authors:
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G Aizencang; R B Frydman; S Giorgieri; L Sambrotta; L Guerra; B Frydman |
Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: Journal of medicinal chemistry Volume: 38 ISSN: 0022-2623 ISO Abbreviation: J. Med. Chem. Publication Date: 1995 Oct |
Date Detail:
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Created Date: 1995-11-28 Completed Date: 1995-11-28 Revised Date: 2006-11-15 |
Medline Journal Info:
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Nlm Unique ID: 9716531 Medline TA: J Med Chem Country: UNITED STATES |
Other Details:
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Languages: eng Pagination: 4337-41 Citation Subset: IM |
Affiliation:
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Facultad de Farmacia y Bioquímica, Universidad de Buenos Aires, Argentina. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Animals Binding, Competitive Carcinoma, Hepatocellular Enzyme Inhibitors / pharmacology* Liver / drug effects, enzymology Liver Neoplasms Ornithine / analogs & derivatives*, chemistry*, metabolism Ornithine Decarboxylase / antagonists & inhibitors* Putrescine / analogs & derivatives*, chemistry*, metabolism Rats Structure-Activity Relationship Thioacetamide / pharmacology Tumor Cells, Cultured |
| Chemical | |
Reg. No./Substance:
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0/Enzyme Inhibitors; 110-60-1/Putrescine; 62-55-5/Thioacetamide; 7006-33-9/Ornithine; EC 4.1.1.17/Ornithine Decarboxylase |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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