Bioorganic & Medicinal Chemistry Letters 1998-02-03

Selective inhibition of the chymotrypsin-like activity of the 20S proteasome by 5-methoxy-1-indanone dipeptide benzamides.

R T Lum, M G Nelson, A Joly, A G Horsma, G Lee, S M Meyer, M M Wick, S R Schow

Index: Bioorg. Med. Chem. Lett. 8(3) , 209-14, (1998)

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Abstract

Potent inhibitors of the 20S proteasome that contain a novel indanone head group coupled to di and tripeptides are described. These compounds are the first proteasome inhibitors have demonstrated high selectivity for the chymotrypsin-like activity of the 20S proteasome.