Estrogen and Nerve Cell Protection

[Judith Richards <judithr@xxxxxxxxxxxxxxxxxxxxxx>]

Scientists Pinpoint Structure on Estrogen That Blocks Nerve Cell Damage

Discovery Opens Way to Designing Non-Feminizing, Estrogen-Like Drugs
For Alzheimer's Disease, Stroke and Other Neurodegenerative Diseases

CAMBRIDGE, Mass., Dec. 17 /PRNewswire/ -- Apollo BioPharmaceutics, Inc.
(Cambridge, Mass.) today announced that scientists at the University of
Florida School of Pharmacy (Gainesville, Fla.) and scientists at Apollo have
discovered a specific structure on the estrogen molecule responsible for
estrogen's ability to protect nerve cells from death.  The estrogen structure
study was published in the December 19th issue (Vol. 63, number 4-6,
pgs.229-235) of The Journal of Steroid Biochemistry and Molecular Biology.

"This is an important discovery," said Katherine Gordon, Ph.D., chief
executive officer of Apollo and one of the study's authors.  "We now know that
estrogen's potency and neuroprotective activity come from different parts of
the estrogen molecule.  This means we should be able to design drugs for
Alzheimer's disease and stroke that protect against nerve cell death but do
not produce hormonal 'feminizing' side effects."

Previously, several studies have shown that postmenopausal women taking
estrogen have a lower incidence and significantly later onset of Alzheimer's
disease than women who do not take estrogen.  Estrogens also have been found,
in some studies, to reduce the death rate from stroke.

In laboratory tests, the research team found that the neuroprotective
effects of estrogens reside on the "phenolic A ring" of the four-ring estrogen
molecule.  Even certain "weak" estrogens with little or no hormonal activity
had a strong neuroprotective effect, leading the authors to state that the
"study provides evidence for the dissociation of the estrogenic potency of
steroids and their neuroprotectivity."

Twenty-two estrogen-like compounds and steroids were tested for their
ability to block damage in a cultured cell line when it was deprived of
essential nutrients.  Estrogenic activity of the compounds was measured in
other, earlier studies using estrogen receptor binding assays.  The results,
the authors wrote, suggest "that the neuroprotectivity of these compounds is
not mediated primarily through the nuclear estrogen receptor."

SOURCE  Apollo BioPharmaceutics, Inc.
1997 PR Newswire. All rights reserved.

Judith Richards
judithr@xxxxxxxxxxxxxx