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ABSTRACT The antitumour agent 5-(3,3-dimethyl-1-triazeno)imidazole-4-carboxamide (DTIC) was found to inhibit competitively the low-Km cyclic AMP phosphodiesterase activity in an

ammonium-sulphate-precipitable fraction of the 2,000g supernatant of rat liver. With substrate concentration at 0.25 microM, I50 was 790 microM for DTIC and 350 microM for theophylline. DTIC

at 2 mM more than doubled the cAMP response to glucagon in hepatocytes and to adrenaline in MH1C1 hepatoma cells, indicating that it also exerts its inhibitory effect on the

phosphodiesterase in intact cells. The possible contribution of the phosphodiesterase inhibition to the growth-inhibitory and cytotoxic effects of DTIC is discussed. Access through your

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access 10 September 2021 Authors * P G Larsson View author publications You can also search for this author inPubMed Google Scholar * F Haffner View author publications You can also search

for this author inPubMed Google Scholar * G O Brønstad View author publications You can also search for this author inPubMed Google Scholar * T Christoffersen View author publications You

can also search for this author inPubMed Google Scholar RIGHTS AND PERMISSIONS Reprints and permissions ABOUT THIS ARTICLE CITE THIS ARTICLE Larsson, P., Haffner, F., Brønstad, G. _et al._

The antitumour agent 5-(3,3-dimethyl-1-triazeno) imidazole-4-carboxamide (DTIC) inhibits rat liver cAMP phosphodiesterase and amplifies hormone effects in hepatocytes and hepatoma cells. _Br

J Cancer_ 40, 768–773 (1979). https://doi.org/10.1038/bjc.1979.259 Download citation * Issue Date: 01 November 1979 * DOI: https://doi.org/10.1038/bjc.1979.259 SHARE THIS ARTICLE Anyone you

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