Title : Key structural features of ligands for activation of human pregnane X receptor.

Pub. Date : 2004 Apr

PMID : 15039302






3 Functional Relationships(s)
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1 The aim of this study was to determine the structure-activity relationships for hPXR-mediated transactivation by barbiturates, hydantoins, and macrolide antibiotics. Hydantoins nuclear receptor subfamily 1 group I member 2 Homo sapiens
2 In the case of hydantoins, only mephenytoin and ethotoin, which have an alkylchain at the R1-position, strongly activated hPXR at 300 microM. Hydantoins nuclear receptor subfamily 1 group I member 2 Homo sapiens
3 These results suggest that the presence of an alkyl-chain at the R1-position and the presence of bulky and hydrophobic moieties at both R2- and R3-positions are important factors for activation of hPXR by hydantoins. Hydantoins nuclear receptor subfamily 1 group I member 2 Homo sapiens