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Novel α-glucosidase inhibitors identified using multiple cyclic peptide combinatorial libraries

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Summary

Twenty-six cyclic synthetic peptide combinatorial libraries (disulfides and lactams) of varying size and composition, representing 6.8 × 103 to 4.7 × 107 individual peptides, were synthesized along with their respective linear analogs. One of the hexapeptide lactam libraries (cyclo[xXxXxN]) was found to have significant α-glucosidase inhibitory activity. This library was carried through an iterative process of synthesis and screening, during which all of the five mixture positions (x and X) were successively defined. As the result of this process, potent and selective a-glucosidase inhibitors were identified.

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Authors and Affiliations

  1. Torrey Pines Institute for Molecular Studies, 3550 General Atomics Court, 92121, San Diego, CA, USA

    Jutta Eichler, Adam W. Lucka, Clemencia Pinilla & Richard A. Houghten

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  1. Jutta Eichler
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  2. Adam W. Lucka
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  3. Clemencia Pinilla
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  4. Richard A. Houghten
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Eichler, J., Lucka, A.W., Pinilla, C. et al. Novel α-glucosidase inhibitors identified using multiple cyclic peptide combinatorial libraries. Mol Divers 1, 233–240 (1996). https://doi.org/10.1007/BF01715527

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  • DOI: https://doi.org/10.1007/BF01715527

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