Comparative effect of a family of substituted thiopseudoureas on protein synthesis by rat liver and Walker carcinoma ribosomes

Chemico-biological Interactions
A Carmona, N F González-Cadavid

Abstract

In order to assess the role played respectively by the pseudothiourea group and the alkylic chain in the inhibition of protein synthesis and tumour growth caused by compound AHR-1911, a series of eight related substances were studied. The blockade of protein synthesis on liver and Walker carcinoma ribosomes and on suspensions of Walker carcinoma cells, depended essentially on the length of the alkylic chain and the substitution in C-1. The minimum chain was 9 carbons and a plateau in the activity was reached at 11 carbons. Replacement of the thiourea group in C-1 by an NH2 group did not change the pattern. A double bond in the distal section of the chain (AHR-1911) increased inhibition on intact cells with a parallel decrease in cytotoxicity, and reduced the aggregation of ribosomes, protein synthesis factors and other proteins. The antitumor effect depends on the pseudothiourea group and is not caused primarily by interference with protein synthesis. Aminoacyl tRNA binding and transfer appeared to be targets of AH4-1911, but this did not affect significantly tRNA change or nascent peptide release. Drug binding to ribosomes and their subsequent aggregation can be regulated by K+ concentration and temperature. It is assumed that...Continue Reading

References

Mar 23, 1974·FEBS Letters·D Vazquez
Feb 1, 1974·The Biochemical Journal·N F González-Cadavid, F Herrera Quijada
Dec 1, 1968·European Journal of Biochemistry·M Cannon
Mar 12, 1970·Biochemical and Biophysical Research Communications·D Richter
Oct 1, 1971·The Biochemical Journal·N F González-CadavidM González
Nov 1, 1966·Experimental Cell Research·K NorrbyP M Lundin

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Citations

Sep 4, 2012·Medicinal Chemistry Research : an International Journal for Rapid Communications on Design and Mechanisms of Action of Biologically Active Agents·Mirosława KoronkiewiczZygmunt Kazimierczuk

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