Location matters: site of conjugation modulates stability and pharmacokinetics of antibody drug conjugates.

  title={Location matters: site of conjugation modulates stability and pharmacokinetics of antibody drug conjugates.},
  author={Pavel Strop and S Liu and Magdalena Dorywalska and Kathy Delaria and Russell G Dushin and Thomas-Toan Tran and W B Ho and Santiago Esteban Farias and Meritxell Galindo Casas and Yasmina Noubia Abdiche and Dahui Zhou and Ramalakshmi Y Chandrasekaran and Caroline Samain and Carole Loo and Andrea Rossi and Mathias Rickert and Stellanie Krimm and Teresa W T Wong and Sherman Michael Chin and Jessica J. Yu and Jeanette Dilley and Javier Chaparro-Riggers and Gary F Filzen and Christopher J. O'Donnell and Fang Wang and Jeremy S. Myers and Jaume Pons and David L. Shelton and Arvind Rajpal},
  journal={Chemistry & biology},
  volume={20 2},
Antibody drug conjugates (ADCs) are a therapeutic class offering promise for cancer therapy. The attachment of cytotoxic drugs to antibodies can result in an effective therapy with better safety potential than nontargeted cytotoxics. To understand the role of conjugation site, we developed an enzymatic method for site-specific antibody drug conjugation using microbial transglutaminase. This allowed us to attach diverse compounds at multiple positions and investigate how the site influences… CONTINUE READING

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