Research ArticleDRUG DESIGN

Design of pathway preferential estrogens that provide beneficial metabolic and vascular effects without stimulating reproductive tissues

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Science Signaling  24 May 2016:
Vol. 9, Issue 429, pp. ra53
DOI: 10.1126/scisignal.aad8170

Designing better estrogens

Estrogen and synthetic versions can enhance the repair of blood vessels after injury or improve metabolism in the liver and adipose tissue, but they can also cause breast or uterine cancer, because they stimulate cell proliferation in these reproductive tissues. Madak-Erdogan et al. designed estrogen-like molecules that had reduced receptor affinity and that did not enhance ductal mammary gland branching (a sign of mammary gland growth) or increase uterine weight in ovariectomized mice. These estrogens provided vascular and metabolic benefits and thus could be further developed as postmenopausal hormone replacement therapies.