Current Medicinal Chemistry - Volume 12, Issue 9, 2005

Nuclear receptors (NRs) are ligand-dependent transcription factors that play a central role in various physiological processes. The pharmaceutical industry has great interest in this gene-family for the discovery of novel or improved drugs for treatment of, for example, cancer, infertility, or diabetes. The usage of threedimensional coordinates of protein structures to analyse and predict interactions with ligands is an importa Read More

The last ten years much attention has been focused on the finding of non-steroidal ligands for steroidal nuclear receptors for reasons such as diminishing cross-reactivity to eliminate side effect profiles, changing physicochemical properties which might cause different tissue distribution profiles and altering binding modes which influence the binding of cofactors. Compounds with a selective functionality profile are referre Read More

The biological effects of estrogens are thought to be mediated by two receptors referred to as ERα and ERβ. In recent years significant efforts have been devoted to the design of subtype selective ligands. These ligands are valuable tools to establish the precise biological role of each of the subtypes and to develop new generations of therapeutics. The first part of this review briefly summarizes the biology behind the estroge Read More