Click and Pick: Identification of Sialoside Analogues for Siglec-Based Cell Targeting

Authors

  • Cory D. Rillahan,

    1. Department of Chemical Physiology, The Scripps Research Institute, 10550 N. Torrey Pines Road, La Jolla, CA 92037 (USA)
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  • Dr. Erik Schwartz,

    1. Department of Chemistry, The Scripps Research Institute, 10550 N. Torrey Pines Road, La Jolla, CA 92037 (USA)
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  • Ryan McBride,

    1. Department of Chemical Physiology, The Scripps Research Institute, 10550 N. Torrey Pines Road, La Jolla, CA 92037 (USA)
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  • Prof. Valery V. Fokin,

    1. Department of Chemistry, The Scripps Research Institute, 10550 N. Torrey Pines Road, La Jolla, CA 92037 (USA)
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  • Prof. James C. Paulson

    Corresponding author
    1. Department of Chemical Physiology, The Scripps Research Institute, 10550 N. Torrey Pines Road, La Jolla, CA 92037 (USA)
    • Department of Chemical Physiology, The Scripps Research Institute, 10550 N. Torrey Pines Road, La Jolla, CA 92037 (USA)
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  • We would like to thank Prof. K. Barry Sharpless, Prof. Ola Blixt, and Prof. Jason Hein, for encouragement and help at early stages of this project as well as Dr. Norihito Kawasaki for advice and assistance in preparation of human white blood cells. This work was supported by the NIH (T32AI007606 to C.D.R., R01AI050143 and P01L107151 to J.C.P., and GM087620 to V.V.F.), a Schering-Plough Research Institute postdoctoral fellowship (E.S.), and a Rubicon fellowship from the Netherlands Organization for Scientific Research (E.S.).

Abstract

original image

Click ‘n’ chips: Azide and alkyne-bearing sialic acids (purple diamond; see picture) were subjected to high-throughput click chemistry to generate a library of sialic acid analogues. Microarray printing of the library and screening with the siglec family of sialic-acid-binding proteins, led to the identification of high-affinity ligands for siglec-9 and siglec-10.

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