Steroidal Pure Antioestrogens

Overview

Journal J Endocrinol

Specialty Endocrinology

Date 1987 Mar 1

PMID 3559447

Citations 45

Authors

A E Wakeling

J Bowler

Affiliations

Soon will be listed here.

Abstract

The effects of some novel 7 alpha-alkyl amide analogues of oestradiol on the rat and mouse uterus have been measured. The compound ICI 164,384 [N-n-butyl-N-methyl-11-(3,17 beta-dihydroxyoestra-1,3,5(10)-trien-7 alpha-yl) undecamide] was entirely devoid of oestrogenic activity in the rat and mouse uterus but completely blocked the uterine stimulatory effects of oestradiol and of tamoxifen. Biological activity was confined to 7 alpha-isomers. The affinity of ICI 164,384 for the rat uterus oestrogen receptor (0.19) was substantially greater than that of tamoxifen (0.025 c.f. oestradiol = 1). The compound inhibited oestradiol-induced growth of ZR-71-1 cells in a dose-dependent manner in vitro. ICI 164,384 thus has the characteristics of a pure antagonist of oestrogen action.

Citing Articles

Dynamic proximity interaction profiling suggests that YPEL2 is involved in cellular stress surveillance.

Turan G, Olgun C, Ayten H, Toker P, Ashyralyyev A, Savas B Protein Sci. 2023; 33(2):e4859.

PMID: 38145972 PMC: 10804680. DOI: 10.1002/pro.4859.

Elacestrant demonstrates strong anti-estrogenic activity in PDX models of estrogen-receptor positive endocrine-resistant and fulvestrant-resistant breast cancer.

Pancholi S, Simigdala N, Ribas R, Schuster E, Leal M, Nikitorowicz-Buniak J NPJ Breast Cancer. 2022; 8(1):125.

PMID: 36446866 PMC: 9709100. DOI: 10.1038/s41523-022-00483-1.

Oral Selective Estrogen Receptor Degraders (SERDs) in Breast Cancer: Advances, Challenges, and Current Status.

Downton T, Zhou F, Segara D, Jeselsohn R, Lim E Drug Des Devel Ther. 2022; 16:2933-2948.

PMID: 36081610 PMC: 9447452. DOI: 10.2147/DDDT.S380925.

17-Estradiol Increases APE1/Ref-1 Secretion in Vascular Endothelial Cells and Ovariectomized Mice: Involvement of Calcium-Dependent Exosome Pathway.

Lee Y, Joo H, Lee E, Kim S, Jin H, Choi Y Biomedicines. 2021; 9(8).

PMID: 34440244 PMC: 8394342. DOI: 10.3390/biomedicines9081040.

From Pure Antagonists to Pure Degraders of the Estrogen Receptor: Evolving Strategies for the Same Target.

Mottamal M, Kang B, Peng X, Wang G ACS Omega. 2021; 6(14):9334-9343.

PMID: 33869913 PMC: 8047716. DOI: 10.1021/acsomega.0c06362.