Targeting BET bromodomain proteins in cancer: The example of lymphomas

F Spriano, A Stathis, F Bertoni - Pharmacology & therapeutics, 2020 - Elsevier
Abstract The Bromo-and Extra-Terminal domain (BET) family proteins act as “readers” of
acetylated histones and they are important transcription regulators. BRD2, BRD3, BRD4 and …

Small-molecule inhibitors of breast cancer-related targets: Potential therapeutic agents for breast cancer

T Liu, S Song, X Wang, J Hao - European Journal of Medicinal Chemistry, 2021 - Elsevier
Despite dramatic advances in cancer research and therapy, breast cancer remains a tricky
health problem and represents a top biomedical research priority. Nowadays, breast cancer …

Brain co‐delivery of first‐line chemotherapy drug and epigenetic bromodomain inhibitor for multidimensional enhanced synergistic glioblastoma therapy

Y Liu, W Wang, D Zhang, Y Sun, F Li, M Zheng… - …, 2022 - Wiley Online Library
Glioblastoma (GBM) is a central nervous system tumor with poor prognosis due to the rapid
development of resistance to mono chemotherapy and poor brain targeted delivery …

Reprogramming transcription factors Oct4 and Sox2 induce a BRD-dependent immunosuppressive transcriptome in GBM-propagating cells

T Ma, C Hu, B Lal, W Zhou, Y Ma, M Ying, P Prinos… - Cancer research, 2021 - AACR
A subset of stem-like cells in glioblastoma (GBM; GSC) underlies tumor propagation,
therapeutic resistance, and tumor recurrence. Immune evasion is critical for GSCs to carry …

[HTML][HTML] Targeting PD-1/PD-L1 in cancer immunotherapy: an effective strategy for treatment of triple-negative breast cancer (TNBC) patients

S Kumar, M Chatterjee, P Ghosh, KK Ganguly, M Basu… - Genes & …, 2023 - Elsevier
Maintaining the balance between eliciting immune responses against foreign proteins and
tolerating self-proteins is crucial for maintenance of homeostasis. The functions of …

Targeting non-canonical activation of GLI1 by the SOX2-BRD4 transcriptional complex improves the efficacy of HEDGEHOG pathway inhibition in melanoma

S Pietrobono, E Gaudio, S Gagliardi, M Zitani… - Oncogene, 2021 - nature.com
Despite the development of new targeted and immune therapies, the prognosis of metastatic
melanoma remains bleak. Therefore, it is critical to better understand the mechanisms …

[HTML][HTML] BRD4 inhibition suppresses PD-L1 expression in triple-negative breast cancer

X Jing, S Shao, Y Zhang, A Luo, L Zhao, L Zhang… - Experimental cell …, 2020 - Elsevier
Abstract Programmed death-ligand 1 (PD-L1) expression on the surface of tumour cells can
cause tumour immune evasion. Benefits of combining anti-PD-L1 therapy with nab …

[HTML][HTML] Carbon nanotubes (CNT)-loaded ginsenosides Rb3 suppresses the PD-1/PD-L1 pathway in triple-negative breast cancer

X Luo, H Wang, D Ji - Aging (Albany NY), 2021 - ncbi.nlm.nih.gov
Carbon nanotubes (CNTs), as advanced nanotechnology with specific properties and
structures, have presented practical drug delivery properties. Ginsenoside Rg3 is a …

An optimized BRD4 inhibitor effectively eliminates NF-κB-driven triple-negative breast cancer cells

GJ Yang, YQ Song, W Wang, QB Han, DL Ma… - Bioorganic …, 2021 - Elsevier
Acetylation of NF-κB's RelA subunit at lysine-310 (AcLys310) helps to maintain constitutive
NF-κB activity in cancers such as triple-negative breast cancer (TNBC). Bromodomain …

PD-L1 small-molecule modulators: A new hope in epigenetic-based multidrug cancer therapy?

C Zwergel, R Fioravanti, A Mai - Drug Discovery Today, 2023 - Elsevier
Highlights•Short digest on the latest updates regarding immunotherapy with a focus on PD-
L1.•Summary of the recent advances in the field of small molecule PD-L1 …