DURHAM, N.C. -- A new study of how drugs plug into the human progesterone
receptor in the cell supports a new and different view of how drugs and
hormones act on steroid hormone receptors that trigger cellular responses.
The new view holds that steroid receptors are not merely on-off switches,
but are far more complicated molecular "control panels" that could
be manipulated by drugs customized to produce more targeted effects on the
body, said the scientists who made the discovery. The drugs could cause
the same receptor to trigger only certain of its normal effects in the body,
but not others.
The finding, if confirmed, could point the way to a new wave of drugs with
fewer side effects for contraception, hormone replacement therapy, breast
and prostate cancer, inflammation, osteoporosis and endometriosis, said
the researchers.
The scientists published their findings in the Aug. 6 issue of the Proceedings
of the National Academy of Sciences. They are Brandee Wagner, Giuseppe
Pollio and Donald McDonnell of the Duke University Medical Center departments
of pharmacology and molecular cancer biology; Mansukh Wani, David Lee and
C. Edgar Cook of the Research Triangle Institute (RTI), and Susan Leonhardt
and Dean Edwards of the University of Colorado Health Science Center department
of pathology. Their research was supported by the U.S. Public Health Service.
The researchers used living cells and test tube preparations to analyze
how a range of compounds known to plug into the progesterone receptor affected
its action.
Compounds that plug into receptors are known as ligands. Steroid receptors
are complex proteins that are the principal switches activating cellular
responses to steroid hormones. Steroid receptors reside deep in the cell's
nucleus, activating genes that produce cellular responses. When a hormone
or drug plugs into a receptor, that action changes the shape, or conforma
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Contact: Karyn George
georg016@mc.duke.edu
919-660-1301
Duke University
20-Aug-1996