Concepedia

Achieving <i>In Vivo</i> Target Depletion through the Discovery and Optimization of Benzimidazolone BCL6 Degraders

Benjamin R. Bellenie, Kwai-Ming J. Cheung, Ana Varela, Olivier A. Pierrat, Gavin W. Collie, Gary Box, Michael D. Bright, Sharon Gowan, Angela Hayes, Matthew J. Rodrigues,

Journal of Medicinal Chemistry · 2020 · 73 citations · 13 references

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Abstract

]imidazol-2-one (CCT369260), which reduces BCL6 levels in a lymphoma xenograft mouse model following oral dosing.

References

13

Catalytic in vivo protein knockdown by small-molecule PROTACs

Daniel P. Bondeson, Alina Mares, Ian E. Smith et al. · Nature Chemical Biology · 2015 · 1.3K citations · Full text

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Specific peptide interference reveals BCL6 transcriptional and oncogenic mechanisms in B-cell lymphoma cells

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A Small-Molecule Inhibitor of BCL6 Kills DLBCL Cells In Vitro and In Vivo

Leandro Cerchietti, Alexandru F. Ghetu, Xiao Zhu et al. · Cancer Cell · 2010 · 286 citations · Full text

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Chemically Induced Degradation of the Oncogenic Transcription Factor BCL6

Nina Kerres, Steffen Steurer, Stefanie Schlager et al. · Cell Reports · 2017 · 206 citations · Full text

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Small‐Molecule‐Mediated Degradation of the Androgen Receptor through Hydrophobic Tagging

Jeffrey L. Gustafson, Taavi K. Neklesa, Carly S. Cox et al. · Angewandte Chemie International Edition · 2015 · 195 citations

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