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Updated: May 13, 2026

Reverse Yeast Two-hybrid System to Identify Mammalian Nuclear Receptor Residues that Interact with Ligands and/or Antagonists
Published on: November 15, 2013
Opportunities for development of novel therapies targeting steroid hormone receptors
Chang Bai1, Osvaldo Flores, Azriel Schmidt
1Merck Research Laboratories, Department of Molecular Endocrinology, WP26A-1000, West Point, PA 19486-0004, USA +1 215 652 5914 ; +1 215 652 4328 ; chang_bai@merck.com.
Abstract:
Steroid hormone receptors belong to the nuclear receptor superfamily of ligand-dependent transcription factors and are the main effectors of steroid hormone action. A number of marketed drugs currently used in the management of multiple disorders target steroid receptors, reflecting their broad homeostatic function and therapeutic potential. The discovery and development of selective estrogen receptor modulators (SERMs), such as tamoxifen and raloxifene, that mimic the natural hormone in certain tissues but antagonize it in others, led to a new approach to exploit and expand the therapeutic utility of synthetic steroid receptor ligands. Indeed, recent work suggests that the 'SERM' or 'selective nuclear receptor modulator' concept can be expanded to other members of the nuclear receptor family. Here, the authors discuss opportunities and challenges in the development of novel therapeutic agents targeting members of the steroid hormone receptors.
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