Discovery of pyrrolopyrimidinone inhibitors of the BCL6-SMRT corepressor interaction.
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TL;DR
A rational, structure-based drug design approach was able to use a rational, structure-based drug design approach to identify and advance a novel series of pyrrolopyrimidinone BCL6 BTB inhibitors.
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A rational, structure-based drug design approach was able to use a rational, structure-based drug design approach to identify and advance a novel series of pyrrolopyrimidinone BCL6 BTB inhibitors.
APA
Iain D. G. Watson, Justin A. Morin, et al. (2026). Discovery of pyrrolopyrimidinone inhibitors of the BCL6-SMRT corepressor interaction.. Bioorganic & medicinal chemistry, 135, 118575. https://doi.org/10.1016/j.bmc.2026.118575
MLA
Iain D. G. Watson, et al.. "Discovery of pyrrolopyrimidinone inhibitors of the BCL6-SMRT corepressor interaction.." Bioorganic & medicinal chemistry, vol. 135, 2026, pp. 118575.
PMID
41621194 ↗
Abstract 한글 요약
B-cell lymphoma 6 (BCL6) is a transcriptional repressor protein central to the development and maintenance of germinal centers (GCs) during the humoral immune response. BCL6 is often deregulated in diffuse large B-cell lymphoma (DLBCL), a type of non-Hodgkin's lymphoma, and inhibition of the protein-protein interaction between BCL6 and corepressors has been implicated as a therapeutic strategy. Based on a previously identified small molecule binding site on the BCL6 BTB domain, we carried out a virtual screen and identified a set of high micromolar screening hits. One series was advanced to a low micromolar confirmed hit via iterative rounds of compound optimization guided by structure activity relationships and co-crystal structures. Overall, we were able to use a rational, structure-based drug design approach to identify and advance a novel series of pyrrolopyrimidinone BCL6 BTB inhibitors.
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