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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 December 18, 1997 CAMBRIDGE, Mass., Dec. 17 /PRNewswire/ via Individual Inc. -- 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." According to the Alzheimer's Association 4 million Americans have Alzheimer's disease. That number is projected to reach 14 million by the middle of the next century. The National Stroke Association reports that 550,000 Americans experience a new or recurrent stroke each year. Stroke is the third leading cause of death in the United States. Apollo BioPharmaceutics, a privately held company founded in 1992, is pioneering the development of estrogen and estrogen-like neuroprotective drugs. Apollo holds the rights to key intellectual property covering the use of estrogenic compounds in the treatment of neurodegenerative diseases. The company has several estrogen-related compounds in development, including one which uses an implantable sustained-release formulation. A test which predicts how well an individual will respond to estrogen therapy is also in development. SOURCE Apollo BioPharmaceutics, Inc. /CONTACT: Katherine Gordon, Ph.D., Chief Executive Officer of Apollo BioPharmaceutics, Inc., 617-621-7154 or Douglas Johnson, Ph.D. of GreenTree Communications, 800-428-8796, [log in to unmask]