Phorbol esters alter muscarinic receptor binding and inhibit polyphosphoinositide breakdown in human neuroblastoma (SH-SY5Y) cells.

作者: Mariangela Serra , Thomas L. Smith , Henry I. Yamamura

DOI: 10.1016/0006-291X(86)91071-5

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摘要: Abstract Many recent reports have indicated that the effect of phorbol ester tumor promoters is mediated through Ca 2+ phospholipid dependent protein kinase C. We investigated two biologically active esters, 4 β-phorbol 12 β-myristate 13 α-acetate (PMA) and β-phorbol12 β,13 α-didecanoate (βPDD) on muscarinic agonist binding receptor-stimulated phosphoinositide breakdown in cultured human neuroblastoma (SH-SY5Y) cells. Preincubation these cells with esters significantly reduced carbachol-stimulated inositol phospholipids caused a decrease affinity for [3H](-)methyl quinuclidinyl benzilate ([3H](-)MQNB) without affecting antagonist to receptor. The nontumor promoting α-phorbol12^β,12 (αPDD) was ineffective our studies. These results suggest activation C may play an important role regulating receptor system.

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