Preparation and Assessment of Self-Immolative Linkers for Therapeutic Bioconjugates with Amino- and Hydroxyl-Containing Cargoes

Bioconjug Chem. 2019 May 15;30(5):1489-1499. doi: 10.1021/acs.bioconjchem.9b00214. Epub 2019 May 3.

Abstract

A series of self-immolative linkers containing a thiol-reactive group at one end and a hydroxyl- or amine-reactive group at the other were prepared. The utility of these reagents for preparations of bioconjugates was explored by reacting the linkers with appropriately functionalized model drugs and peptides. Degradation studies of a series of conjugates with different linkers reveal that the structure of the linkers has a significant impact on their stability.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amines / chemistry
  • Peptides / chemistry
  • Pharmaceutical Preparations / chemistry
  • Sulfhydryl Compounds / chemistry*

Substances

  • Amines
  • Peptides
  • Pharmaceutical Preparations
  • Sulfhydryl Compounds