[HTML][HTML] PLK1 inhibition-based combination therapies for cancer management

S Su, G Chhabra, CK Singh, MA Ndiaye, N Ahmad - Translational oncology, 2022 - Elsevier
Polo-like kinase I (PLK1), a cell cycle regulating kinase, has been shown to have oncogenic
function in several cancers. Although PLK1 inhibitors, such as BI2536, BI6727 (volasertib) …

Small molecules targeting HATs, HDACs, and BRDs in cancer therapy

D Wu, Y Qiu, Y Jiao, Z Qiu, D Liu - Frontiers in oncology, 2020 - frontiersin.org
Evidence for research over the past decade shows that epigenetic regulation mechanisms
run through the development and prognosis of tumors. Therefore, small molecular …

Medulloblastoma targeted therapy: From signaling pathways heterogeneity and current treatment dilemma to the recent advances in development of therapeutic …

Q Wang, X Xin, Q Dai, M Sun, J Chen… - Pharmacology & …, 2023 - Elsevier
Medulloblastoma (MB) is a major pediatric malignant brain tumor that arises in the
cerebellum. MB tumors exhibit highly heterogeneous driven by diverse genetic alterations …

[HTML][HTML] PLK1 inhibition sensitizes breast cancer cells to radiation via suppressing autophagy

B Wang, X Huang, H Liang, H Yang, Z Guo, M Ai… - International Journal of …, 2021 - Elsevier
Purpose Polo-like kinase 1 (PLK1) is a protein kinase that is overexpressed in breast cancer
and may represent an attractive target for breast cancer treatment. However, few studies …

Super-enhancers and the super-enhancer reader BRD4: tumorigenic factors and therapeutic targets

H Qian, M Zhu, X Tan, Y Zhang, X Liu, L Yang - Cell Death Discovery, 2023 - nature.com
Transcriptional super-enhancers and the BET bromodomain protein BRD4 are emerging as
critical drivers of tumorigenesis and therapeutic targets. Characterized by substantial …

Targeting epigenetic regulation for cancer therapy using small molecule inhibitors

A Kumar, L Emdad, PB Fisher, SK Das - Advances in Cancer Research, 2023 - Elsevier
Cancer cells display pervasive changes in DNA methylation, disrupted patterns of histone
posttranslational modification, chromatin composition or organization and regulatory …

Super-enhancers: a new frontier for glioma treatment

M Cheng, ZW Zhang, XH Ji, Y Xu, E Bian… - Biochimica et Biophysica …, 2020 - Elsevier
Glioma is the most common primary malignant tumor in the human brain. Although there are
a variety of treatments, such as surgery, radiation and chemotherapy, glioma is still an …

Novel Aminopyrimidine-2, 4-diones, 2-Thiopyrimidine-4-ones, and 6-Arylpteridines as Dual-Target Inhibitors of BRD4/PLK1: Design, Synthesis, Cytotoxicity, and …

S El-Kalyoubi, SA El-Sebaey, SM Elfeky… - Pharmaceuticals, 2023 - mdpi.com
Structural-based drug design and solvent-free synthesis were combined to obtain three
novel series of 5-arylethylidene-aminopyrimidine-2, 4-diones (4, 5a–c, 6a, b), 5 …

Time series modeling of cell cycle exit identifies Brd4 dependent regulation of cerebellar neurogenesis

C Penas, ME Maloof, V Stathias, J Long, SK Tan… - Nature …, 2019 - nature.com
Cerebellar neuronal progenitors undergo a series of divisions before irreversibly exiting the
cell cycle and differentiating into neurons. Dysfunction of this process underlies many …

Recent progress in agents targeting polo-like kinases: Promising therapeutic strategies

Z Zhang, X Xing, P Guan, S Song, G You, C Xia… - European Journal of …, 2021 - Elsevier
Polo-like kinases (PLKs) play important roles in regulating multiple aspects of cell cycle and
cell proliferation. In many cancer types, PLK family members are often dysregulated, which …