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  • Title: Synthesis and biological evaluation of boron peptide analogues of Belactosin C as proteasome inhibitors.
    Author: Nakamura H, Watanabe M, Ban HS, Nabeyama W, Asai A.
    Journal: Bioorg Med Chem Lett; 2009 Jun 15; 19(12):3220-4. PubMed ID: 19428245.
    Abstract:
    A series of boron peptides 11, 13, 15 and 17 were designed and synthesized as proteasome inhibitors based on the structure of Belactosin C. Matteson homologation was a key step in the synthesis of the boron peptides. Compounds 11a and 13 showed significant inhibition of 20S proteasome chymotrypsin-like (beta5) activity (IC(50)=0.28 and 0.51 microM, respectively). Furthermore, like PS-341, compound 11a increased the G2/M cell distribution. A biparametric cytofluorimetric analysis with FITC-labeled annexin V and propidium iodide showed induction of apoptosis by compound 11a at >1 microM concentrations of compound.
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