Oncogene function inhibitor

Screening of Oncogene Function Inhibitors from Microbial Secondary Metabolites... 

The present volume reflects these developments, and there is a growing emphasis on bioactive natural products. Articles in this volume include those on structure-activity relationships of highly sweet natural products, chemical constituents of cchinodenns, diterpenoids from Rabdosia and Eremophila sp., structural studies on saponins, marine sesquiterpene quinoncs and antimicrobial activity of amphibian venoms. The reviews on bioactive metabolites of Phomopsis, cardenolide detection by ELISA, xenocoumacins and bioactive dihydroisocoumarins, CD studies of carbohydrate-molybdate complexes, oncogene function inhibitors from microbial secondary metabolites and Gelsemium and Lupin alkaloids present frontier developments in several areas of natural product chemistry. It is hoped that the present volume, which contains articles by eminent authorities in each field, will be received with the same enthusiasm as the previous volumes of this series. 

Nechers, L.M. (1989) Antisense oligonucleotides as a tool for studying cell regulation mechanism of uptake and application to the study of oncogene function. In J.S.Cohen (ed.) Oligodeoxyribonucleotides Antisense Inhibitors of Gene Expression. Macmillan Press, London. 

To function, Ras must be attached to the plasma membrane. Translocation from the cytoplasm to membrane requires a series of posttranslational modifications that begin with farnesylation of the cysteine residue, the fourth amino acid residue from the C terminus of the protein, by famesyl protein transferase (FPTase) (64). Attachment of the hydrophobic 15-carbon lipid farnesyl group allows Ras molecule insertion into the plasma membrane and is crucial for Ras signaling activity and transformation properties. As farnesylation is required for oncogenic Ras function, FPTase inhibitors (FTIs) are obvious candidate antineoplastic agents. Several drugs that inhibit Ras farnesylation are at various stages of clinical development (65). 

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