Chapter 5: Structure-Based Design of Estrogen-Related Receptors Modulators
5.1 Introduction
5.2 Structure and Function
5.3 Medicinal Chemistry of ERR Modulators
5.3.1 ERR Inverse Agonists
5.3.2 ERRs Agonists
References
Chapter 6: PPAR[alpha] and Ligand Design: Honing the Traditional Empirical Method with a More Holistic Overview
6.1 Introduction to the PPAR Protein
6.1.1 Overall PPAR LBD Protein Structure
6.1.2 Mechanism of PPAR Gene Transcription
6.1.3 Differences in LBD Between PPAR Subtypes
6.2 Catalogue of Known Ligands
6.2.1 PPAR[alpha] Ligands

Intro
Preface
Contents
About the Editor
Chapter 1: Molecular Pharmacology of the Youngest Member of the Nuclear Receptor Family: The Mineralocorticoid Receptor
1.1 An Overview of the MR Physiology
1.2 Evolutionary Profile of the MR
1.3 The Hsp90-Based Heterocomplex
1.4 MR Trafficking
1.5 Agonist Structure-Activity Relationship
1.6 MR Antagonism
1.7 MR Regulation by Phosphorylation and Redox Potential
1.8 Conclusions
References
Chapter 2: A Simple Method for Visual Assessment and Quantification of Altered Subcellular Localization of Nuclear Receptors

2.1 Introduction
2.2 Materials and Methods
2.3 Notes
References
Chapter 3: Multifaceted Effects of Ligand on Nuclear Receptor Mobility
3.1 Introduction
3.2 Nucleocytoplasmic Shuttling of the Nuclear Receptors
3.2.1 Nuclear Pore Complexes: Gatekeepers of the Nucleus
3.2.2 Nuclear Import Pathways
3.2.3 Nuclear Export Pathways
3.2.4 Dynamics of Movement Within the Nucleus
3.3 Ligand-Dependent Nuclear Accumulation of Nuclear Receptors
3.3.1 Glucocorticoid Receptor Nuclear Accumulation and Intranuclear Dynamics
3.3.1.1 GR Nuclear Accumulation

3.3.1.2 GR Intranuclear Dynamics
3.3.2 Mineralocorticoid Receptor Nuclear Accumulation and Intranuclear Dynamics
3.3.2.1 MR Nuclear Accumulation
3.3.2.2 MR Intranuclear Dynamics
3.3.3 Androgen Receptor Nuclear Accumulation and Intranuclear Dynamics
3.3.3.1 Androgen Receptor Nuclear Accumulation
3.3.3.2 Androgen Receptor Intranuclear Dynamics
3.4 Ligand-Dependent Intranuclear Localization
3.5 Ligand-Independent Trafficking
3.5.1 Thyroid Hormone Receptor Intracellular Trafficking
3.5.2 Retinoic Acid Receptor Intracellular Trafficking

3.6 Retinoid X Receptor and Vitamin D Receptor Intracellular Trafficking: A Bin of Their Own?
3.7 Conclusions
References
Chapter 4: Chemical Considerations in Discovery of Receptor Modulators
4.1 Introduction
4.2 Intermolecular Binding Forces Drive Ligand Action
4.3 Sterics and Hydrophobicity in Ligand Binding
4.4 Stereochemical Considerations
4.5 Molecular Dynamics as a Tool for Modulator Design
4.6 Case Study: A Holistic Approach to Liver X Receptor Modulator Design
4.7 Conclusions
References