Site-selective labeling of a lysine residue in human serum albumin.

  title={Site-selective labeling of a lysine residue in human serum albumin.},
  author={Shigehiro Asano and James T. Patterson and Thomas Gaj and Carlos F. Barbas},
  journal={Angewandte Chemie},
  volume={53 44},
Conjugation to human serum albumin (HSA) has emerged as a powerful approach for extending the in vivo half-life of many small molecule and peptide/protein drugs. Current HSA conjugation strategies, however, can often yield heterogeneous mixtures with inadequate pharmacokinetics, low efficacies, and variable safety profiles. Here, we designed and synthesized analogues of TAK-242, a small molecule inhibitor of Toll-like receptor 4, that primarily reacted with a single lysine residue of HSA. These… CONTINUE READING


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Site-specific labeling of recombinant HSA at Lys64 and Cys34. Conjugation reactions

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