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A small-molecule degrades a cancer-promoting

Nov 27, 2020 · Scientists from Heidelberg and USA have now deciphered another mechanism whereby a small molecule can degrade a cancer protein. This drug binds to the lymphoma-driving protein BCL6, and induces BCL6 self-polymerization, which then attracts the cell's disposal system, leading to BCL6 degradation and the death of the cancer cell. Gluing Proteins for Targeted Degradation:Cancer CellJan 11, 2021 · Given the novel degradation mechanism triggered by the polymerization of BCL6, one could ask whether it can be applied more broadly to induce degradation of other proteins. Growing evidence indicates that small molecules can induce hetero-dimerization, homo-dimerization, and further polymerization of proteins (Stanton et al., 2018

Protein degradation profile reveals dynamic nature of 20S

Abstract. Small molecules have been discovered to stimulate the 20S core particle (CP) of the proteasome to degrade proteins. However, the impact a 20S CP stimulator can have on the regulation of protein levels has not been fully characterized. Previous studies have focused on using one kind of stimulator to enhance the degradation of specific 20S CP substrates. Small molecule probes for targeting autophagy Nature May 25, 2021 · Autophagy is an essential catabolic cellular degradation process. It is responsible for the degradation of damaged or otherwise dispensable proteins, as well as aggregates 1 and droplets 2, bySmall-molecule-induced polymerization triggers degradation Here we report an alternative mechanism of targeted protein degradation, in which a small molecule induces the highly specific, reversible polymerization of a target protein, followed by its sequestration into cellular foci and subsequent degradation. BI-3802 is a small molecule that binds to the Broad-complex, Tramtrack and Bric-à-brac (BTB) domain of the oncogenic transcription factor B cell lymphoma 6 (BCL6) and leads to the proteasomal degradation