4 Some common phamacological sighificant nuclear receptors
Receptor name Abbreviation Ligand Drugs Location Ligard blinding Mechanism of action Type I Androgen AR Testosterone All natural and symthetic Translocation to nucleus. Binding glucocortticoids ( Ch.34) to HREs with to half-sites with an Oestrogen ER𝛼, 𝛽 17𝛽 − 𝑜𝑒𝑠𝑡𝑟𝑎𝑑𝑖𝑜𝑙 mineralocorticoids(Ch. 30) inverted sequence. Rercuitment Glucocorticoid GR𝛼 Cortisol, And sex steroids (Ch. 36) Cytosolic Homodimers of co-activators, transcription corticosterone factors and other proteins. Progesterone PR Progesterone Together with their Mineralocorticoid MR Aldosterone Antagonists (e.g.raloxifene, 4-hydroxy-tamoxifen and Mifepistone) Type II Retinoid X RXR 𝛼, 𝛽, 𝛾 9-cis-retinoic acid Retionds drugs (Ch. 28) Binding to HREs with to half-sites Retinoic Acid RAR 𝛼, 𝛽, 𝛾 Vitamin A with an inverted or simple Thyroid hormone TR 𝛼, 𝛽 T3, T4 Thyroid hormone drugs repeat sequence. Complexed with (Ch.35) co-repessors, which are displaced Peroxisome proliferator PPAR 𝛼, 𝛽, 𝛾, 𝛿 Fatty acids, Rosiglitazone, pioglitazone Nuclear Heterodimers following ligand binding, prostaglandins (Ch. 32) often with PXR allowing the binding of Constitutive CAR Androstane Stimulation of CYP co-activations androstane synthesis and alteration of Pregnane X PXR Xenobiotics drug metebolism (Ch. 10) Only examples from classes I and II are included