2-(3-4-dihydroxyphenyl)-7-8-dihydroxy-1-benzopyran-4-one and Neoplasms

2-(3-4-dihydroxyphenyl)-7-8-dihydroxy-1-benzopyran-4-one has been researched along with Neoplasms* in 1 studies

Other Studies

1 other study(ies) available for 2-(3-4-dihydroxyphenyl)-7-8-dihydroxy-1-benzopyran-4-one and Neoplasms

ArticleYear
Targeting Bromodomain-Selective Inhibitors of BET Proteins in Drug Discovery and Development.
    Journal of medicinal chemistry, 2022, 04-14, Volume: 65, Issue:7

    Blocking the interactions between bromodomain and extraterminal (BET) proteins and acetylated lysines of histones by small molecules has important implications for the treatment of cancers and other diseases. Many pan-BET inhibitors have shown satisfactory results in clinical trials, but their potential for poor tolerability and toxicity persist. However, recently reported studies illustrate that some BET bromodomain (BET-BD1 or BET-BD2)-selective inhibitors have advantage over pan-inhibitors, including reduced toxicity concerns. Furthermore, some selective BET inhibitors have similar or even better therapeutic efficacy in inflammatory diseases or cancers. Therefore, the development of selective BET inhibitors has become a hot spot for medicinal chemists. Here, we summarize the known selective BET-BD1 and BET-BD2 inhibitors and review the methods for enhancing the selectivity and potency of these inhibitors based on their different modes of interactions with BET-BD1 or BET-BD2. Finally, we discuss prospective strategies that selectively target the bromodomains of BET proteins.

    Topics: Drug Discovery; Histones; Humans; Neoplasms; Prospective Studies; Protein Domains; Transcription Factors

2022