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On the function of hormone receptors in the action of steroidal alkylating agents

On the function of hormone receptors in the action of steroidal alkylating agents

Zeitschrift fuer Krebsforschung und Klinische Onkologie 89(3): 321-330

Steroidal alkylating agents are supposed to bind to steroid hormone receptors in target tissues. By this interaction the steroid portion might act as a carrier for the alkylating group. Three steroidal agents (phenesterin, estradiol mustard, dehydroepiandrosterone mustard) were tested for their capacity to combine with estrogen and androgen receptors in calf uterus and human breast cancer target tissues. For measuring steroid receptor complexes ager gel electrophoresis was used. All 3 compounds (added at a 103-fold excess) revealed no competition for receptor sites (estrogen and androgen binding) in vitro. After preincubation of intact tissue estrogen mustard was effective in inhibiting the binding of 3H-estradiol and dehydroepiandrosterone mustard reduced the uptake of 3H-5.alpha.-DHT [dihydrotestosterone]. This may be due to liberating of estradiol and dehydroepiandrosterone, respectively, from the intact molecule. From these data it is unlikely that cytostatic steroidal agents are more effective than other alkylating drugs.

Accession: 006027347

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PMID: 198984

DOI: 10.1007/bf00283786

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