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Inhibition of Protein Synthesis by RA-VII

✍ Scribed by B.V. Sirdeshpande; P.L. Toogood


Publisher
Elsevier Science
Year
1995
Tongue
English
Weight
476 KB
Volume
23
Category
Article
ISSN
0045-2068

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✦ Synopsis


The antitumor natural product RA-VII has been evaluated as an inhibitor of protein synthesis in vitro. Complete inhibition of protein synthesis in rabbit reticulocyte lysates is observed with (5 \mu \mathrm{m}) RA-VII. Mechanistic studies using purified elongation factors and ribosomes identify RA-VII as a peptidyltransferase inhibitor. Thus. similar to the related natural products bouvardin and RA-XII, RA-VII appears to function by binding to eukaryotic ribosomes. 1945 Academic Press. Inc.


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## Abstract Point mutations in __ras__ genes have been found in a large number and wide variety of human tumors. These oncogenic Ras mutants are locked in an active GTP‐bound state that leads to a constitutive and deregulated activation of Ras function. The dogma that __ras__ oncogenes are dominant