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生物物理学报 2001
STRUCTURAL BASIS OF FUNCTIONAL SPECIFICITYOF STEROID RECEPTORS
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Abstract:
The steroid receptors include the estrogen receptor, androgen receptor, progesterone receptor, glucocorticoid receptor and mineralocorticoid receptor. They are involved in almost all physiological activities, including reproduction,homeostasis,cell proliferation, differentiation and death. Elucidating the specificity of steroid receptors' subfamily will deepen understanding of their functions and has potential pharmaceutical applications. The evolutionary trace method was used to analyze structural basis of functional specificity of steroid receptors. Results indicated that steroid receptors and its endogenous ligands may experience some coevolutionary process;trace residues in ligand-binding sites display different hydrogen-bond interactions and van der Waals contacts between receptors and its ligands,which decide subfamilies' ligand binding specificity.These informations can be used to modify ligand specificity of steroid receptors and design tissue-selective ligands(e.g. selective estrogen receptor modulator).