The antifungal antibiotic sinefungin as a very active inhibitor of methyltransferases and of the transformation of chick embryo fibroblasts by Rous sarcoma virus
| Autor: | Malka Robert-Gero, Michèle Vedel, Edgar Lederer, Françoise Lawrence |
|---|---|
| Rok vydání: | 1978 |
| Předmět: |
S-Adenosylmethionine
Methyltransferase Adenosine Antifungal Agents Biophysics Chick Embryo Biochemistry Cell Line Sinefungin Structure-Activity Relationship medicine Animals cardiovascular diseases Molecular Biology chemistry.chemical_classification Rous sarcoma virus biology Antifungal antibiotic Cell Biology Methylation Methyltransferases Fibroblasts biology.organism_classification Cell Transformation Viral S-Adenosylhomocysteine In vitro nervous system diseases Kinetics Enzyme chemistry Avian Sarcoma Viruses medicine.drug |
| Zdroj: | Biochemical and biophysical research communications. 85(1) |
| ISSN: | 0006-291X |
| Popis: | Summary The antifungal antibiotic Sinefungin is a structural analogue of S-adenosyl-methionine (SAM) and of S-adenosyl-homocysteine (SAH). It is as active as the synthetic SAH analogue S-isobutyl adenosine (SIBA) in inhibiting Rous Sarcoma Virus (RSV) induced transformation of chick embryo fibroblasts (CEF) in cell culture. Sinefungin, like SAH and SIBA is a competitive inhibitor in vitro of tRNA methylases and of protein methylases I and III of CEF. Its ki value for tRNA methylases of normal and transformed cells is respectively 3 to 10 times lower than the ki of SAH. It is thus in vitro the most active tRNA methylase inhibitor described until now. Protein methylase I and III are inhibited to about the same extent by the two molecules whereas SIBA has much higher ki values for the three enzymes in vitro . When methylation was measured in whole cells SAH, SIBA and Sinefungin inhibited (14C)-methyl incorporation to about the same degree in normal cells, but only SIBA and Sinefungin were active in transformed cells. Download : Download full-size image |
| Databáze: | OpenAIRE |
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