Proteolysis targeting chimera (PROTAC™) molecules can reduce intracellular levels of a targeted pathogenic protein by making use of a cell’s own protein disposal machinery. These heterobifunctional molecules, composed of two ligands linked through a chemical bridge, are designed to recruit an E3 ubiquitin ligase complex to a targeted protein to induce its degradation through exploitation of the ubiquitin-proteasome pathway. As a platform for drug discovery, the PROTAC™ modality is a small-molecule protein knockdown approach that results in drastically different pharmacodynamics in comparison to traditional occupancy-driven small-molecule inhibition of protein activity or gene-based medicines. This presentation will focus on the inroads that Arvinas has made to develop, understand, and advance this technology into the clinic.<br/>

PROTAC™ targeted protein degraders: Exciting modality for drug discovery

2019 Fall National Meeting

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