One-bead-one-compound combinatorial peptidomimetic libraries, in conjunction with a high-stringency screening method, are a powerful tool for screening peptide and peptidomimetic ligands for target proteins. Picomolar-affinity peptidomimetics for the integrin α4β1 have now been developed and have been successfully used to image α4β1-expressing tumors in living mice.
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Chen, X., Gambhir, S. Significance of one-bead-one-compound combinational chemistry. Nat Chem Biol 2, 351–352 (2006). https://doi.org/10.1038/nchembio0706-351
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DOI: https://doi.org/10.1038/nchembio0706-351