Nuclear Hormone Receptors/NHRs as Drug Targets

Nuclear hormone receptors (NHRs) are ligand-activated transcription factors which are involved in crucial physiological processes such as cancer, diabetes, rheumatoid arthritis, asthma or hormoneresistance syndromes. Therefore, these nuclear hormone receptors are still of great interest in modern biomedical research and drug discovery.

Nuclear Hormone Receptors (NHRs) are soluble proteins that can regulate gene expression by interacting with specific DNA sequences, and that's why therapeutic drugs can act on specific targets at the level of transcription.

In contrast to other transcription factors, the activity of nuclear hormone receptors can be modulated by binding to the corresponding ligands – small lipophilic molecules that easily penetrate biological membranes. A number of nuclear receptors identified in recent years do not have any known ligands. These so-called orphan receptors have attracted considerable interest since they could lead to the discovery of new endocrine regulatory systems.