An overview of spirooxindole as a promising scaffold for novel drug discovery

LM Zhou, RY Qu, GF Yang - Expert Opinion on Drug Discovery, 2020 - Taylor & Francis
Introduction: Spirooxindole, a unique and versatile scaffold, has been widely studied in
some fields such as pharmaceutical chemistry and synthetic chemistry. Especially in the …

Keep calm and carry on with extra centrosomes

BM Kalkan, SC Ozcan, NJ Quintyne, SL Reed, C Acilan - Cancers, 2022 - mdpi.com
Simple Summary Precise chromosome segregation during mitosis is a vital event
orchestrated by formation of bipolar spindle poles. Supernumerary centrosomes, caused by …

Discovery of the First Potent, Selective, and In Vivo Efficacious Polo-like Kinase 4 Proteolysis Targeting Chimera Degrader for the Treatment of TRIM37-Amplified …

Y Sun, Y Xue, P Sun, S Mu, H Liu, Y Sun… - Journal of Medicinal …, 2023 - ACS Publications
Polo-like kinase 4 (PLK4) is a master regulator of centriole replication and has been
proposed as a therapeutic target for multiple cancers, especially TRIM37-amplified breast …

CRISPR activation screening in a mouse model for drivers of hepatocellular carcinoma growth and metastasis

B Zhang, Z Ren, H Zheng, M Lin, G Chen, OJ Luo… - Iscience, 2023 - cell.com
Hepatocellular carcinoma (HCC) remains a major cause of cancer-related mortality
worldwide. Here we described a genome-wide screen by CRISPR activation (CRISPRa) …

Fraxetin down-regulates polo-like kinase 4 (PLK4) to inhibit proliferation, migration and invasion of prostate cancer cells through the phosphatidylinositol 3-kinase …

Z Ma, Y Sun, W Peng - Bioengineered, 2022 - Taylor & Francis
Fraxetin, a natural product isolated from herb Cortex Fraxini, has been demonstrated to
exhibit anti-cancer effects on various cancers. The aim of this work is to investigate the anti …

[HTML][HTML] Centrosomal-associated proteins: potential therapeutic targets for solid tumors?

Y Luan, M Li, Y Zhao, Q Li, J Wen, S Gao… - Biomedicine & …, 2021 - Elsevier
The centrosome is a special organelle in human cells and an organizing unit for
microtubules and signaling molecules. In addition, the centrosome is tightly restricted during …

PLK4 initiates crosstalk between cell cycle, cell proliferation and macrophages infiltration in gliomas

X Zhang, Z Li, C Wei, L Luo, S Li, J Zhou… - Frontiers in …, 2022 - frontiersin.org
Tumor immune microenvironment plays an important role in tumorigenesis and metastasis.
Polo-like kinases 4 (PLK4) is a crucial regulatory factor in the process of cell cycle, and its …

Radiotherapy and radiosensitization in breast cancer: Molecular targets and clinical applications

V Bhat, S Pellizzari, AL Allan, E Wong, M Lock… - Critical Reviews in …, 2022 - Elsevier
Relatively poor survival outcomes are observed in advanced or metastatic breast cancer,
where local control of the primary or metastatic disease may be achieved by surgical …

Novel indazole derivatives as potent apoptotic antiproliferative agents by multi-targeted mechanism: Synthesis and biological evaluation

FOA Frejat, H Zhai, Y Cao, L Wang, YA Mostafa… - Bioorganic …, 2022 - Elsevier
Indazole is a significant class of heterocyclic compounds with a wide range of biological
activity. We display here the synthesis and biological evaluation of a novel series of indazole …

Hypoxia drives centrosome amplification in cancer cells via HIF1α-dependent induction of polo-like kinase 4

K Mittal, J Kaur, S Sharma, N Sharma, G Wei… - Molecular Cancer …, 2022 - AACR
Centrosome amplification (CA) has been implicated in the progression of various cancer
types. Although studies have shown that overexpression of PLK4 promotes CA, the effect of …