Receptor modulators, nuclear hormone

The farnesoid X receptor is a member of the class of nuclear hormone receptors, which have key roles in development and homeostasis, as well as in many diseases like obesity, diabetes and cancer. The farnesoid X receptor shows structural similarity to the estrogen receptor (ER ), which mediates a broad spectrum of physiological functions such as regulation of reproduction, modulation of bone density, cholesterol transport and breast cancer. The farnesoid X receptor also shows similarity with the peroxisome proliferation-activated receptor y (PPARy), which is involved in fat metabolism, inflammatory and immune responses. The estrogen receptor (ER ), the peroxisome proliferation-activated receptor y (PPARy) and the farnesoid X receptor (FXR) can be clustered in a... 

The retinoid X receptor (RXR) forms a functional heterodimer with PPARy as well as other nuclear hormone receptors. The RXR modulators can activate the RXR-PPARy complex, improving glucose tolerance in animal models however, selectivity for this particular heterodimer is required to avoid undesirable side effects. Analogues acting by this mechanism are in earlier stages of development. 

Handbook of Metalloproteins, Vol. 3, ed. A. Messerschmidt, John Wiley Sons Ltd., Chichester, UK, 2004 R 198 S. Devarakonda and F. Restinejad, Zinc Modules in Nuclear Hormone Receptors , p. 324... 

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