| Literature DB >> 33844535 |
Yong Ai1, Lucia Hwang1, Alexander D MacKerell1, Ari Melnick2,3, Fengtian Xue1.
Abstract
B-cell lymphoma 6 (BCL6) is a master regulator of germinal center formation that produce antibody-secreting plasma cells and memory B-cells for sustained immune responses. The BTB domain of BCL6 (BCL6BTB) forms a homodimer that mediates transcriptional repression by recruiting its corepressor proteins to form a biologically functional transcriptional complex. The protein-protein interaction (PPI) between the BCL6BTB and its corepressors has emerged as a therapeutic target for the treatment of DLBCL and a number of other human cancers. This Perspective provides an overview of recent advances in the development of BCL6BTB inhibitors from reversible inhibitors, irreversible inhibitors, to BCL6 degraders. Inhibitor design and medicinal chemistry strategies for the development of novel compounds will be provided. The binding mode of new inhibitors to BCL6BTB are highlighted. Also, the in vitro and in vivo assays used for the evaluation of new compounds will be discussed.Entities:
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Year: 2021 PMID： 33844535 PMCID： PMC8168288 DOI： 10.1021/acs.jmedchem.0c01686
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446