Nuclear Receptors as Drug Targets

Nuclear receptors are the site of action for some of the most widely used medications, namely oral contraceptives and related drugs derived from steroid hormones. Recent research has uncovered their pivotal role in a range of human diseases, including diabetes and metabolic syndrome, triggering a new wave of drug discovery efforts focused on this class of molecular targets.
Edited by two experts working at the pioneering pharmaceutical company and major global player in hormone–derived drugs, this handbook systematically treats the drug development aspects of all human nuclear receptors, including such recently characterized receptors as PPAR, FXR and LXR, and modern tools for nuclear receptor research.
With its contributions from authors working at leading pharmaceutical companies around the world providing examples and real–life data from their own experience, this is an invaluable reference for medicinal chemists, biochemists, molecular biologists, pharmacologists and those working in the pharmaceutical industry.

Nuclear Receptors as Modern Drug Targets – a Historic Perspective
Targeting the Nuclear Receptor –
Cofactor Interaction
Untangling the Estrogen Receptor Web
Subtype Selective Estrogens
Estrogen Receptors as Therapeutic Targets in Breast Cancer
Progesterone Receptor and Progestines
Progesterone Receptor Antagonists
Nonsteroidal Tissue Selective Androgen Receptor Modulators
The Glucocorticoid Receptor as Target for Classic and Novel Anti–inflammatory Therapy and Novel Glucocorticoid Receptor Ligands
Vitamin D Analogs as Modulators of Vitamin D Receptor Action
PPARs: Therapeutic Targets for Metabolic Disease and Type 2 Diabetes
Retinoids in Clinical Use
Nuclear Receptors as Targets in Cardiovascular Diseases
NURR77 Family of Nuclear Receptors and its Modulators
Induction of Drug Metabolism: The Role of Nuclear Receptors
Nuclear Receptor Targeted Screening Libraries and Chemogenomics Approaches


Eckard Ottow is the head of medicinal chemistry at Schering AG in Berlin (Germany). He studied Chemistry at the University of Hannover (Germany) and received his PhD degree in 1982. He joined Schering AG in 1983, first in the field of endocrinology and later in oncology and CNS. In 2002, he was appointed to his present position as head of medicinal chemistry. He is also a honorary professor at the Technical University of Berlin.

Hilmar Weinmann studied Chemistry at the universities of Tübingen and Hannover (Germany). He joined Schering in 1995, where he is currently a department head of Medicinal Chemistry. His main fields of expertise are in oncology, dermatology and gender healthcare.


"With increasing importance attributed to this area, the text is a welcome review of the current field.... The quality of the text is good with very readable chapters and many useful original literature references. The book will be clearly valuable for both academic and industrial groups engaged in drug discovery." ( Journal of Medicinal Chemistry, March 2009)

"This is an excellent book for scientists interested in adding or expanding expertise in nuclear receptor drug discovery to their skill set. The chapters are timely, well referenced into the 2008 literature, and focused on the chemistry of successful and emerging therapeutic small molecules." (Journal of the American Chemical Society, March 10, 2009)

"The book is a good reference for medicinal chemists, pharmacologists and those working in the pharmaceutical industry." (RoSearch, December 2008)