Steroid ligand selectivity

Fig. 1.13 Interactions of DHT with AR. As in other steroid NHR complexes, the ligand is oriented on both ends by polar interactions. Mutagenesis experiments have implicated Thr-877 as a key residue that determines ligand selectivity.

Fig. 1.16 Examples of interactions in the D-rings of steroids that account for ligand selectivity.

Geistlinger, T.R., McReynolds, A.C. and Guy, R.K. (2004) Ligand-selective inhibition of the interaction of steroid receptor coactivators and estrogen receptor isoforms. Chemistry et Biology, 11,273-281. 

Jacobs MN, Lewis DF (2002) Steroid hormone receptors and dietary ligands a selected review. ProcNutrSoc 61 105... 

Enzymes that are involved in steroid hormone biosynthesis or in steroid metabolism are also targets of anti-hormonal therapy. Recently, it was discovered that certain co-factors modulate the signalling of steroid hormone receptors in a tissue-selective fashion. By binding the receptor ligand complex, these co-activators and co-repressors are capable of either activating or repressing transcription, respectively [5j. 

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