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Comparative Study
. 1995 Aug 25;50(5):723-6.
doi: 10.1016/0006-2952(95)00186-4.

Comparison between inhibition of protein kinase C and antagonism of calmodulin by tamoxifen analogues (V体育官网入口)

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Comparative Study

Comparison between inhibition of protein kinase C and antagonism of calmodulin by tamoxifen analogues

M G Rowlands et al. Biochem Pharmacol. .

Abstract

A variety of analogues of tamoxifen were tested for inhibition of protein kinase C (PKC) activity in MCF-7 breast cancer cells. These results were compared with the calmodulin antagonism exhibited by the analogues as measured by inhibition of calmodulin-dependent cyclic AMP phosphodiesterase. The same structural features that enhanced PKC inhibition also led to an increase in calmodulin antagonism, namely 4-iodination and elongation of the basic side-chain. The most potent analogue has a 4-iodine substituent and eight carbon atoms in its basic side-chain with IC50 values of 38 microM for PKC inhibition and 0. 3 microM for calmodulin antagonism, which compares with 92 and 6. 8 microM, respectively, for tamoxifen VSports手机版. Some selectivity was achieved with a ring-fused analogue that retained the potency of tamoxifen as a PKC inhibitor, but lacked calmodulin antagonism. .

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