An evaluation of a C-glucuronide as a liver targeting group: conjugate of a glucocorticoid antagonist.

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Sorensen BK, Link JT, von Geldern T, Emery M, Wang J, Hickman B, Grynfarb M, Goos-Nilsson A, Carroll S

An evaluation of a C-glucuronide as a liver targeting group: conjugate of a glucocorticoid antagonist.

Bioorg Med Chem Lett. 2003 Jul 21;13(14):2307-10.

PubMed ID
12824023 [ View in PubMed
]
Abstract

A beta-C-glucuronide conjugate of the glucocorticoid receptor antagonist, Mifepristone 1, was prepared which maintained binding affinity, had modest in vitro activity, and was metabolically more stable than the parent. Pharmacokinetic studies suggest that the conjugate is recognized by the liver like O-glucuronides and may undergo a portion of the enterohepatic recirculation loop.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
MifepristoneGlucocorticoid receptorIC 50 (nM)1.1N/AN/ADetails
MifepristoneGlucocorticoid receptorIC 50 (nM)5N/AN/ADetails