Discovery of a new class of glucosylceramide synthase inhibitors.

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Koltun E, Richards S, Chan V, Nachtigall J, Du H, Noson K, Galan A, Aay N, Hanel A, Harrison A, Zhang J, Won KA, Tam D, Qian F, Wang T, Finn P, Ogilvie K, Rosen J, Mohan R, Larson C, Lamb P, Nuss J, Kearney P

Discovery of a new class of glucosylceramide synthase inhibitors.

Bioorg Med Chem Lett. 2011 Nov 15;21(22):6773-7. doi: 10.1016/j.bmcl.2011.09.037. Epub 2011 Sep 17.

PubMed ID

21974949 [ View in PubMed

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Abstract

A novel series of potent inhibitors of glucosylceramide synthase are described. The optimization of biochemical and cellular potency as well as ADME properties led to compound 23c. Broad tissue distribution was obtained following oral administration to mice. Thus 23c could be another useful tool compound for studying the effects of GCS inhibition in vitro and in vivo.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Miglustat	Ceramide glucosyltransferase	IC 50 (nM)	22000	N/A	N/A	Details