Endocrine Abstracts

The production of oestradiol (E2) is paramount for the growth of oestrogen receptor α positive breast cancer. Various strategies have been used, including the use of enzyme inhibitors against either aromatase (AROM) or steroid sulphatase (STS), in an attempt to ablate E2 levels. Both these enzymes play a critical role in the formation of oestrogenic steroids (see figure 1) and their inhibitors are now showing success in the clinic. The studies presented here demonstrate t...

2-Methoxyoestrogens are emerging as a new class of anti-neoplastic agents. 2-Methoxyoestradiol (2-MeOE2), an endogenous oestrogen metabolite, has shown anti-proliferative effects in ER+ve and ER-ve breast cancer cell lines. In this study we have investigated the effects of sulphamoylated derivatives of 2-MeOE2, 2-methoxyoestradiol-3-O-monosulphamate (2-MeOE2MATE) and 2-methoxyoestradiol 3,17 bis sulphamate (2-MeOE2bisMATE) in ER-ve MDA-MB-231 cells. Both 2-MeOE2MATE and 2-MeOE...

2-Methoxyoestradiol (2-MeOE2) is a human endogenous metabolite of oestradiol which is known to inhibit the proliferation of breast cancer cells. Sulphamoylation of 2-MeOE2 greatly enhances its ability to inhibit breast cancer cell proliferation and induce apoptosis. To establish whether 2-MeOE2 and its mono- and bis-sulphamoylated derivatives would also be an effective treatment for other endocrine cancers, we have investigated their effects, and those of 2-ethyloestradiol (2-...

Ovarian cancer is the leading cause of death from all gynaecological malignancies. The observation that decreased levels of the natural oestrogen-17beta metabolite, 2-methoxyoestradiol (2-MeOE2) may create a predisposition to oestrogen dependent cancer, has led to considerable interest in the potential use of oestrogen derivatives for the prevention and treatment of hormone dependent cancers. The sulphamoylated oestrone derivative 2-methoxyoestrone-3-O-sulphamate (2-MeO...