A 7-methoxybicoumarin derivative selectively inhibits BRD4 BD2 for anti-melanoma therapy

Editorial: Epigenetics of the immune component of inflammation

“…Mounting evidence revealed that epigenetic modifications (DNA/RNA modifications, non-coding RNAs, and post-translational modifications) are linked with the genesis of inflammation via modulating a variety of immune components such as cytokines, transcription factors, complements, pattern recognition receptors, and other inflammation-related genes. The epigenetic genes are constitutively activated or deactivated in multiple immune-or nonimmune cells under inflammatory conditions and contribute to a variety of inflammatory diseases, such as rheumatoid arthritis (RA) [Yang et al, as well as diabetes (3), Ding et al], and cancers (4,5), etc. Inflammation often hijacks various epigenetic mechanisms to promote occurrence and development of these diseases (6,7).…”

“…The epigenetic genes are constitutively activated or deactivated in multiple immune- or non-immune cells under inflammatory conditions and contribute to a variety of inflammatory diseases, such as rheumatoid arthritis (RA) [ Yang et al. , as well as diabetes ( 3 ), Ding et al ], and cancers ( 4 , 5 ), etc. Inflammation often hijacks various epigenetic mechanisms to promote occurrence and development of these diseases ( 6 , 7 ).…”

“…In turn, epigenetic modifications also mediate pathologic development of inflammation by regulating immune components in inflammatory microenvironments ( 8 , 9 ). Numerous preclinical and clinical studies showed that epigenetic modulators, including KDM5 inhibitors ( 10 ), LSD1 inhibitors ( 11 ), HDAC inhibitors ( 12 ), EZH2 inhibitors ( 13 , 14 ), and BET inhibitors ( 4 , 5 , 15 ) exhibit anti–inflammatory activities in vitro and in vivo . Therefore, exploring the roles of epigenetics of immune components in inflammation not only helps us to understand the progress of inflammatory diseases, but also contributes to developing novel strategies for diagnosis and treatment of these diseases.…”

The binding mechanism of NHWD-870 to bromodomain-containing protein 4 based on molecular dynamics simulations and free energy calculation

“…BET inhibitors have shown high efficacy in preclinical models and positive results in clinical trials of haematological malignancies, including acute lymphoblastic leukaemia, multiple myeloma, acute myeloid leukaemia, and non-Hodgkin's lymphoma. 11,14–19 Currently, there are more than 40 BET inhibitors with available preclinical data or entering early clinical development. Despite this, to the best of our knowledge, there has yet to be a BET inhibitor approved by the Food and Drug Administration (FDA).…”

MG53 inhibits cellular proliferation and tumor progression in colorectal carcinoma

“…However, in the case of cancer cells, ABCB1 expression leads to a reduced cell concentration of the substrate chemotherapeutic drug, thus causing MDR 17 , 18 . Some of the most common substrate chemotherapeutic drugs of ABCB1 include paclitaxel, etoposide, vincristine, colchicine, and doxorubicin 19 , 20 . Many studies have been conducted to develop novel inhibitors as modulators of ABC transporter mediated MDR and as potential anti-cancer drugs 21 , 22 .…”