From PROTACs to DACs: How targeted protein degraders are breaking rules and boundaries in drug design

From PROTACs to DACs: How targeted protein degraders are breaking rules and boundaries in drug design

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Overview

Approximately 80% of proteins lack enzymatic activity or an obvious active site for traditional small molecule drugs to block. This thwarts the development of therapies for diseases associated with these proteins.

To take on these “undruggable” proteins, researchers are developing complex drug structures like proteolysis-targeting chimeras (PROTACs) and other chimeric targeted protein degraders that challenge the traditional rules of drug design. Due to their structural complexity, collaborations are essential to accelerate the development of targeted protein degraders to meet critical unmet needs.

Key Objectives:

How PROTACs and other chimeric targeted protein degraders challenge the traditional rules of drug design.
How collaborative efforts are stimulating advances and knowledge-sharing in degrader discovery and development.
Other targeted protein degrader-based drugs showing promise include lysosome-targeting chimeras (LYTACs), autophagy-targeting chimeras (AUTACs), and degrader-antibody conjugates (DACs).

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