Nuclear Hormone Receptors and Gene Expression Fayig El-Migdadi, MD, PhD

Nuclear Hormone Receptors and Gene Expression Ana Aranda and Angel Pascual Physiol Rev July 2001 vol. 81 no. 3 1269-1304

Mechanism of action of nuclear receptors.

Aranda A , Pascual A Physiol Rev 2001;81:1269-1304

2001 by American Physiological Society

Subfamilies of mammalian nuclear receptors

Receptor Subtype Denomination Ligand Response Element Monomer, Homodimer, or Heterodimer Class ITR RAR , Thyroid hormone receptor , , Retinoic acid receptor ( Thyroid hormone (T 3 Retinoic acid Pal, DR-4, IP DR-2, DR-5 H H

Pal, IP

VDR

Vitamin D receptor

OH)2vitamin D3)1-25

DR-3, IP-9

PPAR

, , Peroxisome proliferator activated receptor

Benzotriene B4; Wy 14.643Eicosanoids; thiazolidinediones (TZDS); 15-deoxy-12,41-prostaglandin J2; polyunsaturated fatty acids

DR-1

PXR

Pregnane X receptor

Pregnanes; C21 steroids

DR-3

CAR/MB67

, Constitutive androstane receptor

Androstanes; 1,4-bis[2-(3,5-dichloropyridyloxy)]benzene

DR-5

LXR

, Liver X receptor

Oxysterols

DR-4

FXR

Farnesoid X receptor

Bile acids

DR-4, IR-1

RevErb

, Reverse ErbA

Unknown

DR-2, Hemisite

M, D

RZR/ROR

, , Retinoid Z receptor/retinoic acid-related orphan receptor

Unknown

Hemisite

UR

Ubiquitous receptor

Unknown

DR-4

Class IIRXR COUP-TF

, , Retinoid X receptor , , Chicken ovalbumin upstream promoter transcription factor

Cis-retinoic acid- 9 Unknown

Pal, DR-1 Pal, DR-5

D D, H

HNF-4

, , Hepatocyte nuclear factor 4

Fatty acyl-CoA thioesters

DR-1, DR-2

TLX

Tailles-related receptor

Unknown

DR-1, Hemisite

M, D

PNR

Photoreceptor-specific nuclear receptor

Unknown

DR-1, Hemisite

M, D

TR2

, Testis receptor

Unknown

DR-1 to DR5

D, H

Class IIIGR

Glucocorticoid receptor

Glucocorticoids

Pal

Schematic representation of a nuclear receptor.

Aranda A , Pascual A Physiol Rev 2001;81:1269-1304

2001 by American Physiological Society

The DNA binding domain of the nuclear receptors.

Aranda A , Pascual A Physiol Rev 2001;81:1269-1304

2001 by American Physiological Society

Schematic drawing of the nuclear receptor ligand-binding domain (LBD).

Aranda A , Pascual A Physiol Rev 2001;81:1269-1304

2001 by American Physiological Society

Binding of receptors to the hormone response elements (HREs).

Aranda A , Pascual A Physiol Rev 2001;81:1269-1304

2001 by American Physiological Society

Permissive and nonpermissive heterodimers.

Aranda A , Pascual A Physiol Rev 2001;81:1269-1304

2001 by American Physiological Society

Domains of p160 and CBP/p300 families of receptor coactivators.

Aranda A , Pascual A Physiol Rev 2001;81:1269-1304

2001 by American Physiological Society

Structure of the nuclear receptor corepressors SMRT and NCoR.

Aranda A , Pascual A Physiol Rev 2001;81:1269-1304

2001 by American Physiological Society

Coactivator and corepressor complexes and histone acetylation.

Aranda A , Pascual A Physiol Rev 2001;81:1269-1304

2001 by American Physiological Society