核受体最新综述(包括LXR、RXR、FXR等)

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1521-0081/65/2/710–778$25.00/10.1124/pr.112.006833 P HARMACOLOGICAL R EVIEWS Pharmacol Rev65:710–778,April2013 Copyright©2013by The American Society for Pharmacology and Experimental Therapeutics

ASSOCIATE EDITOR:DIANNE M.PEREZ

Nuclear Receptors and Their Selective

Pharmacologic Modulators

Thomas P.Burris,Laura A.Solt,Yongjun Wang,Christine Crumbley,Subhashis Banerjee,Kristine Griffett,

Thomas Lundasen,Travis Hughes,and Douglas J.Kojetin

The Scripps Research Institute,Jupiter,Florida

Abstract (711)

I.Introduction (711)

A.Discovery of Nuclear Receptors (712)

B.Ligand Regulation of Nuclear Receptor Function (713)

C.Nuclear Receptor Modulators and Selective Modulators (716)

II.Selective Estrogen Receptor Modulators (718)

A.Estrogen Receptor Structure (718)

B.Estrogen Receptor Function (719)

C.Selective Estrogen Receptor Modulators (720)

III.Vitamin D Receptor Modulators (725)

A.Vitamin D Receptor Structure (725)

B.Vitamin D Receptor Function (725)

C.Vitamin D Receptor Modulators (728)

IV.Thyroid Hormone Receptor Modulators (735)

A.Thyroid Hormone Receptor Structure (735)

B.Thyroid Hormone Receptor Action (735)

C.Selective Thyroid Hormone Receptor Modulators (737)

V.Selective Androgen Receptor Modulators (739)

A.Androgen Receptor Structure (739)

B.Androgen Receptor Function (740)

C.Selective Androgen Receptor Modulators (740)

VI.Selective Glucocorticoid Receptor Modulators (742)

A.Glucocorticoid Receptor Structure (742)

B.Glucocorticoid Receptor Action (743)

C.Selective Glucocorticoid Receptor Modulators (744)

VII.Selective Peroxisome Proliferator-Activated Receptor g Modulators (748)

A.Peroxisome Proliferator-Activated Receptor g Structure (748)

B.Peroxisome Proliferator-Activated Receptor g Function (749)

C.Selective Peroxisome Proliferator-Activated Receptor g Modulator (750)

VIII.Liver X Receptor Modulators (754)

A.Liver X Receptor Structure (754)

B.Liver X Receptor Function (755)

C.Selective Liver X Receptor Modulators (755)

IX.Selective Progesterone Receptor Modulators (758)

A.Progesterone Receptor Structure (758)

B.Progesterone Receptor Function (759)

C.Selective Progesterone Receptor Modulators (759)

References (763)

Address correspondence to:Thomas P.Burris,The Scripps Research Institute,130Scripps Way2A1,Jupiter,FL33458.E-mail: tburris@

/10.1124/pr.112.006833.

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