Inhibitory effects of pentamidine analogues on protein biosynthesis in vitro.

• Authors: Krzysztof Bielawski , Anna Galicka , Anna Bielawska , Krystyna Średzińska
• Languages of publication: EN

Abstracts

EN

Pentamidine despite its rather high toxicity, is currently in clinical use. For development of new drugs of this type it is important to know the mechanism of their action. Two new amidines (I and II) and 4',6-diamidino-2-phenylindole (DAPI) were found in preliminary experiments to inhibit protein synthesis in vitro in the cell-free rat liver system. The three compounds differed in the precise mode of action. The inhibitory effect of I on the activity of the eukaryotic elongation factor eEF-2 and ribosomes seems to suggest that the binding site of eEF-2 on the ribosome was blocked by this compound. eEF-2 has been identified as the primary target of II and eEF-1 as the primary target of DAPI in the system studied.

Keywords

EN

amidine; elongation factors; protein synthesis in vitro; DAPI

• Publisher: Polish Biochemical Society
• Journal: Acta Biochimica Polonica
• Year: 2000
• Volume: 47
• Issue: 1
• Pages: 113-120

Dates

published

2000

received

1999-10-25

Contributors

author

Krzysztof Bielawski

• Department of Medicinal Chemistry and Drug Technology, Medical Academy of Białystok, 15-230 Białystok 8, Poland

author

Anna Galicka

• Department of General and Organic Chemistry, Institute of Chemistry, Medical Academy of Białystok, 15-230 Białystok 8, Poland

author

Anna Bielawska

• Department of Medicinal Chemistry and Drug Technology, Medical Academy of Białystok, 15-230 Białystok 8, Poland

author

Krystyna Średzińska

• Department of General and Organic Chemistry, Institute of Chemistry, Medical Academy of Białystok, 15-230 Białystok 8, Poland

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