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Synthesis of Conjugates of 6-aminophenanthridine and Guanabenz, Two Structurally Unrelated Prion Inhibitors, for the Determination of Their Cellular Targets by Affinity Chromatography

Synthesis of Conjugates of 6-aminophenanthridine and Guanabenz, Two Structurally Unrelated Prion Inhibitors, for the Determination of Their Cellular Targets by Affinity Chromatography

Fabienne Gug, Nassima Oumata, Déborah Tribouillard-Tanvier, Cécile Voisset, Nathalie Desban, Stéphane Bach, Marc Blondel, Hervé Galons

Bioconjug Chem. 2010 Feb 17;21(2):279-88.

PMID: 20092293

Abstract:

The synthesis of affinity matrices for 6-aminophenanthridine (6AP) and 2,6-dichlorobenzylidenaminoguanidine (Guanabenz, GA), two unrelated prion inhibitors, is described. In both cases, the same simple spacer, epsilon-aminocaproylaminopentanol, was introduced by a Mitsunobu reaction and the choice of the anchoring position of the linker was determined by the study of the residual antiprion activity of the corresponding 6AP or GA conjugates. Very recently, these two affinity matrices were used for chromatography assays leading to the identification of ribosome (via the rRNA) as a common target of these two antiprion drugs. Here, we show, using competition experiments with Quinacrine (QC) and Chlorpromazine (CPZ), two other antiprion drugs, that QC, but not CPZ, may also directly target the rRNA.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP832688	6-Aminophenanthridine		832-68-8	Price

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