Dorrigocins: novel antifungal antibiotics that change the morphology of ras-transformed NIH/3T3 cells to that of normal cells. III. Biological properties and mechanism of action.
The dorrigocins are unique glutarimide antibiotics which were found to reverse the morphology of ras-transformed NIH/3T3 cells from a transformed phenotype to a normal one. The compounds also inhibited the release of yeast mating pheromone, a-factor. The activity of these compounds was not dependent on inhibition of prenylation or protein synthesis. Dorrigocin A was instead found to inhibit the carboxyl methylation in K-ras transformed cells.
Kadam
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Abbott Laboratories, Abbott Park, Illinois 60064.
McAlpine
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JB
D016475:3T3 Cells / Q000166:cytology* / Q000187:drug effects* / Q000378:metabolism; D019883:Alkyl and Aryl Transferases; D000818:Animals; D000935:Antifungal Agents / Q000494:pharmacology*; D002471:Cell Transformation, Neoplastic / Q000187:drug effects* / Q000235:genetics*; D011905:Genes, ras; D000072235:Mating Factor; D008745:Methylation; D051379:Mice; D015689:Oncogene Protein p21(ras) / Q000378:metabolism; D010455:Peptides / Q000378:metabolism; D010881:Piperidones / Q000494:pharmacology; D014176:Protein Biosynthesis; D011497:Protein O-Methyltransferase / Q000037:antagonists & inhibitors; D015398:Signal Transduction / Q000187:drug effects; D014166:Transferases / Q000096:biosynthesis / Q000378:metabolism
D000935:Antifungal Agents; D010455:Peptides; D010881:Piperidones; C089606:dorrigocin A; C089607:dorrigocin B; D000072235:Mating Factor; D014166:Transferases; D011497:Protein O-Methyltransferase; D019883:Alkyl and Aryl Transferases; C064911:p21(ras) farnesyl-protein transferase; D015689:Oncogene Protein p21(ras)