The DOI matches its Crossref record; 3 of the 3 references it cites were found in a registry or an index.
A peptomimetic inhibitor of BCL6 with potent antilymphoma effects in vitro and in vivo
Open accessAbstract
The BCL6 transcriptional repressor is the most commonly involved oncogene in diffuse large B-cell lymphomas (DLBCLs). BCL6 lymphomagenic activity is dependent on its ability to recruit corepressor proteins to a unique binding site on its N-terminal BTB domain. A recombinant peptide fragment of the SMRT (silencing mediator for retinoid and thyroid hormone receptor) corepressor that blocks this site can inhibit BCL6 biologic functions. Shortening and conversion of this peptide to D-amino acid and retro configuration as well as the addition of a fusogenic motif yielded a far more potent and stable BCL6 inhibitor that still retained the specificity of the original SMRT fragment. Like the L-peptide, retroinverso BCL6 peptide inhibitor (RI-BPI) selectively killed BCR rather than OxPhos-type DLBCL cells. The RI-BPI could recapitulate the failure to form germinal centers seen in BCL6 null mice yet was nontoxic and nonimmunogenic even when administered for up to 52 weeks. RI-BPI showed superior duration of tissue penetration and could accordingly powerfully suppress the growth of human DLBCLs xenografts in a dose-dependent manner. Finally, RI-BPI could kill primary human DLBCL cells but had no effect on normal lymphoid tissue or other tumors.
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Wadia, J. S., Stan, R. V., & Dowdy, S. F. (2004) · Nature Medicine · doi:10.1038/nm996 · Cited by 1,647
Self-citationCattoretti, G., Pasqualucci, L., Ballon, G., Tam, W., Nandula, S. V., Shen, Q., Mo, T., Murty, V. V., & Dalla-Favera, R. (2005) · Cancer Cell · doi:10.1016/j.ccr.2005.03.037 · Cited by 383
Ranuncolo, S. M., Polo, J. M., Dierov, J., Singer, M., Kuo, T., Greally, J., Green, R., Carroll, M., & Melnick, A. (2007) · Nature Immunology · doi:10.1038/ni1478 · Cited by 278
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Cited by
A Small-Molecule Inhibitor of BCL6 Kills DLBCL Cells In Vitro and In Vivo
Cerchietti, L. C., Ghetu, A. F., Zhu, X., Da Silva, G. F., Zhong, S., Matthews, M., Bunting, K. L., Polo, J. M., Farès, C., Arrowsmith, C. H., et al. (2010) · Cancer Cell · doi:10.1016/j.ccr.2009.12.050 · Cited by 288
Self-citationBreaking bad in the germinal center: how deregulation of BCL6 contributes to lymphomagenesis
Hatzi, K., & Melnick, A. (2014) · Trends in Molecular Medicine · doi:10.1016/j.molmed.2014.03.001 · Cited by 183
Self-citationGerminal center‐derived lymphomas: The darkest side of humoral immunity
Mlynarczyk, C., Fontán, L., & Melnick, A. (2019) · Immunological Reviews · doi:10.1111/imr.12755 · Cited by 179
Self-citationRationally designed BCL6 inhibitors target activated B cell diffuse large B cell lymphoma
Cardenas, M. G., Yu, W., Beguelin, W., Teater, M. R., Geng, H., Goldstein, R. L., Oswald, E., Hatzi, K., Yang, S.-N., Cohen, J., et al. (2016) · Journal of Clinical Investigation · doi:10.1172/jci85795 · Cited by 176
Self-citationMcCoull, W., Cheung, T., Anderson, E., Barton, P., Burgess, J., Byth, K., Cao, Q., Castaldi, M. P., Chen, H., Chiarparin, E., et al. (2018) · ACS Chemical Biology · doi:10.1021/acschembio.8b00698 · Cited by 139
Metadata
- Authors
- Cerchietti, L. C., Yang, S. N., Shaknovich, R., Hatzi, K., Polo, J. M., Chadburn, A., Dowdy, S. F., & Melnick, A.
- Venue
- Blood
- Publisher
- American Society of Hematology
- Published
- 2009-04-09
- Volume
- 113
- Issue
- 15
- Pages
- 3397-3405
- ISSN
- 0006-4971 (ISSN-L)
- 1528-0020
- OpenAlex
- W2017580443
- Cited by
- 183
- References
- 3
- FWCI
- 6.53
- Type
- journal article
- Language
- en
- Open access
- bronze
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- Cerchietti, L. C., Yang, S. N., Shaknovich, R., Hatzi, K., Polo, J. M., Chadburn, A., Dowdy, S. F., & Melnick, A. (2009). A peptomimetic inhibitor of BCL6 with potent antilymphoma effects in vitro and in vivo. Blood. https://doi.org/10.1182/blood-2008-07-168773
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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