EurekaMag.com logo
+ Site Statistics
References:
53,214,146
Abstracts:
29,074,682
+ Search Articles
+ Subscribe to Site Feeds
EurekaMag Most Shared ContentMost Shared
EurekaMag PDF Full Text ContentPDF Full Text
+ PDF Full Text
Request PDF Full TextRequest PDF Full Text
+ Follow Us
Follow on FacebookFollow on Facebook
Follow on TwitterFollow on Twitter
Follow on Google+Follow on Google+
Follow on LinkedInFollow on LinkedIn

+ Translate

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






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

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

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

PMID: 198984

DOI: 10.1007/bf00283786

Download PDF Full Text: On the function of hormone receptors in the action of steroidal alkylating agents



Related references

Interactions between estrogen receptors and certain steroidal alkylating agents. Cancer Treatment Reports 62(8): 1262-1266, 1978

In vivo interaction between steroidal alkylating agents and estrogen receptors in rabbit uteri. Acta Endocrinologica 87(1): 173-180, 1978

Steroidal derivatives. Part 4: Synthesis and in vitro anabolic and catabolic properties of a new group of steroidal alkylating agents. Die Pharmazie 38(7): 445-448, 1983

The Action Of Alkylating Agents On Deoxyribonucleic Acid In Relation To Biological Effects Of The Alkylating Agents. Experimental Cell Research 24: Suppl9:512-20, 1963

On the mechanism of action of the alkylating agents. I. Interaction of alkylating agents with nucleic acids. Cancer Research 21: 560-566, 1961

Agents for alkylating steroid hormone receptors. 2. 16-alpha substituted progesterone derivatives. Journal of Medicinal Chemistry 14(3): 222-225, 1971

Agents for alkylating steroid hormone receptors. I. Analogs derived from esters of 17-alpha-hydroxyprogesterone. Steroids 11(1): 37-46, 1968

Agents for alkylating steroid hormone receptors I Analogs derived from esters of 17 -hydroxy-progesterone. Steroids: 37-46, 1968

Agents for alkylating steroid hormone receptors. 3. Omega-substituted esters of 17-alpha-hydroxyprogesterone. Journal of Pharmaceutical Sciences 60(7): 1089-1092, 1971

New antitumor agents Cytostatic and cytogenetic activity of two modified steroidal alkylating agents. European Journal of Cancer 35(SUPPL 4): S196, Sept, 1999