Issue 10, 2022

Degrader-antibody conjugates

Abstract

Degrader-antibody conjugates (DACs) are novel entities that combine a proteolysis targeting chimera (PROTAC) payload with a monoclonal antibody via some type of chemical linker. This review provides a current summary of the DAC field. Many general aspects associated with the creation and biological performance of traditional cytotoxic antibody-drug conjugates (ADCs) are initially presented. These characteristics are subsequently compared and contrasted with related parameters that impact DAC generation and biological activity. Several examples of DACs assembled from both the scientific and the patent literature are utilized to highlight differing strategies for DAC creation, and specific challenges associated with DAC construction are documented. Collectively, the assembled examples demonstrate that biologically-active DACs can be successfully prepared using a variety of PROTAC payloads which employ diverse E3 ligases to degrade multiple protein targets.

Graphical abstract: Degrader-antibody conjugates

Article information

Article type
Tutorial Review
Submitted
16 feb 2022
First published
04 mei 2022

Chem. Soc. Rev., 2022,51, 3886-3897

Degrader-antibody conjugates

P. S. Dragovich, Chem. Soc. Rev., 2022, 51, 3886 DOI: 10.1039/D2CS00141A

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