All three peroxisome proliferator-activated receptor (PPAR) subtypes share a high degree of structural homology while exhibiting differences in function, tissue distribution, and ligand specificity. In Peroxisome Proliferator-Activated Receptors: Discovery and Recent Advances, the authors trace the history of PPAR discovery and detail the receptor structure and its posttranslational modifications. Furthermore, endogenous ligands as well as various classes of exogenous ligands, subtype-selective, dual and pan agonists as well as antagonists, are discussed. In addition, the tissue distribution and versatile functions of PPAR subtypes in major organs are described.

I. Introduction

II. History of PPAR Discovery

A. Peroxisomes

B. Peroxisomal biogenesis and diseases

C. Peroxisome proliferation

III. Peroxisome Proliferator-Activated Receptors

A. Chromosomal location and gene polymorphism

i. PPARa

ii. PPARb/d

iii. PPARg

B. Protein structure

i. N-terminal end (A/B domain)

ii. DNA binding domain (DBD, C domain)

iii. Hinge region (D domain)

iv. Carboxyl terminal end (E/F domain)

IV. PPAR Ligands

A. Endogenous ligands

B. Exogenous PPAR modulators

V. Tissue Distribution and Versatile Functions of PPARs

B. PPARs and the cardiovascular system

C. PPARs in pulmonary physiology and disease

D. Gastrointestinal roles of PPARs

E. PPAR functions in the liver

F. Roles of PPARs in the pancreas

G. PPARs in the urinary tract physiology and pathophysiology

H. PPARs in the reproductive system

I. Bone metabolism and PPARs

J. Roles of PPARs in skeletal muscle biology

K. Skin PPARs

VI. PPARs and Drug Metabolism

VII. Molecular Aspects of PPAR Actions

A. Posttranslational control of PPARs

B. Mechanism of action

VIII. Animal Models in PPAR Research

IX. Safety of PPAR Agonists

X. The Future of PPAR Research

XI. References