The drugable proteome is limited by the number of functional binding sites that can bind small molecules and respond with a therapeutic effect. Orthosteric and allosteric modulators of enzyme function or receptor signaling are well-established mechanisms of drug action. Drugs that promote novel protein-protein interactions and induce protein degradation promise to dramatically expand opportunities for therapeutic intervention. This approach is more difficult for rational design due to the extensive contact surfaces that must be perturbed antagonistically. Here, I will highlight recent applications of computational methods in the design and optimization of targeted protein degraders.

Design and optimization of targeted protein degraders: Leveraging computational tools

2019 Fall National Meeting

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