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Scientific Report 2007
Scripps Florida
Cancer Biology
Chairman's Overview
Staff
John L. Cleveland, Ph.D.
Professor and Chairman
Howard Petrie, Ph.D.
Professor
Tina Izard, Ph.D.
Associate Professor
Nagi G. Ayad, Ph.D.
Assistant Professor
Philippe R. J. Bois, Ph.D.
Assistant Professor
Michael Conkright, Ph.D.
Assistant Professor
Kendall Nettles, Ph.D.
Assistant Professor
Scientific Associate
Chunying Yang, M.D.
Staff Scientists
Joanne R. Doherty, Ph.D.
Ihn Kyung Jang, Ph.D.
HaJeung Park, Ph.D.
Meredith A. Steeves, Ph.D.
Research Associates
Antonio Amelio, Ph.D.
Mi-Ra Chang, Ph.D.
Frank C. Dorsey, Ph.D.
Rangarajan Erumbi, Ph.D.
Irina Getun, Ph.D.
German Gil, Ph.D.
Ann Griffith, Ph.D.
Mark A. Hall, Ph.D.
Jun Hyuck Lee, Ph.D.
Hiroshi Nakase, Ph.D.
Jianjun Shi, Ph.D.
Zhen Wu, Ph.D.
Bhargavakrishna Yekkala, Ph.D.
Sollepura Yogesha, Ph.D.
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A
novel binding pocket in the estrogen receptor. X-ray crystallography reveals
a novel pharmacologic class of synthetic estrogens, which induce a unique restructuring
of the ligand-binding pocket. Top panel, Part of the estrogen receptor ligand-binding
pocket bound to estradiol. Bottom panel, The novel, extended region of the binding
pocket when it is occupied by trifluoromethyl phenylvinyl estradiol, a 50-pM-affinity
ligand. The 30%–40% increase in the size of the binding pocket indicates a
new site for targeted chemistry, which can be used to develop improved therapeutic
agents for breast cancer and other estrogen-responsive disorders. Reprinted with
permission from Nettles, K.W., Bruning, J.B., Gil, G., et al. Structural plasticity
in the oestrogen receptor ligand-binding domain. EMBO Rep. 8:563, 2007.
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