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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.

 

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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