Posted on 24 March 1997
Scientists at the University of York and Karo Bio have solved the structure of the estrogen receptor, one of the crucial receptors targeted by drugs in the treatment of a variety of women's health problems.
The discovery will have a significant effect on the development of drugs to treat conditions like breast cancer, osteoporosis and postmenopausal symptoms.
Nuclear receptors, like estrogen, act as molecular 'locks' for hormonal 'keys' like sex hormones and thyroid hormones. The hormones activate the receptor to take part in the regulation of certain genes which have a central role in the way cells and tissue function, both in healthy people and those with a disease. These receptors are thus important pharmaceutical targets.
"For the first time we can see and understand at the atomic level how estrogen binds to its receptor and performs its function," said Professor Rod Hubbard of the University's Chemistry Department. "Drugs can mimic this effect."
Karo Bio now intends to develop improved pharmaceutical compounds which will interact with the receptor in a very specific way in order to avoid undesirable side effects. "We believe that this discovery is very important for future improvements in women's health care," said Per Otteskog, Head of Research at Karo Bio.
"This discovery is the result of a successful collaboration between industry and academia, and one of the most important protein structures our group has worked on," said Professor Rod Hubbard. "It allows us to understand the structural basis for the interaction between this receptor and a number of hormones and drugs, and gain important insights into the mechanisms whereby these molecules elicit particular biological responses.
"Learning more about how the human body organises its communication systems is not only fascinating science, but it also provides essential information for the rational design of new and imporved pharmaceutical products."