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TARGETED PROTEIN DEGRADATION: FROM CHEMICAL BIOLOGY TO DRUG DISCOVERY

September 24, 2019 | (8:30 AM)
USA (United States of America)
The majority of disease-causing proteins are not amenable to modulation by conventional pharmacological methods. In recent years an alternative therapeutic strategy known as targeted protein degradation has emerged with the potential to inhibit these “undruggable” proteins. This method utilizes chimeric, tripartite molecules that bind to the protein of interest, thereby promoting its polyubiquitination and subsequent proteosomal degradation. These chimeras can be designed to target a wide range of proteins, and offer the advantage of completely ablating both catalytic and scaffolding functions. Moreover, recent data indicates that these molecules can be developed into effective oral agents, making them therapeutically viable.