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 …
some fields such as pharmaceutical chemistry and synthetic chemistry. Especially in the …
[HTML][HTML] Keep calm and carry on with extra centrosomes
Simple Summary Precise chromosome segregation during mitosis is a vital event
orchestrated by formation of bipolar spindle poles. Supernumerary centrosomes, caused by …
orchestrated by formation of bipolar spindle poles. Supernumerary centrosomes, caused by …
[PDF][PDF] CRISPR activation screening in a mouse model for drivers of hepatocellular carcinoma growth and metastasis
Hepatocellular carcinoma (HCC) remains a major cause of cancer-related mortality
worldwide. Here we described a genome-wide screen by CRISPR activation (CRISPRa) …
worldwide. Here we described a genome-wide screen by CRISPR activation (CRISPRa) …
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 …
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
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 …
types. Although studies have shown that overexpression of PLK4 promotes CA, the effect of …
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 …
cell proliferation. In many cancer types, PLK family members are often dysregulated, which …
Structure-based discovery of 1-(3-fluoro-5-(5-(3-(methylsulfonyl) phenyl)-1H-pyrazolo [3, 4-b] pyridin-3-yl) phenyl)-3-(pyrimidin-5-yl) urea as a potent and selective …
Y Sun, L Wang, Y Sun, J Wang, Y Xue, T Wu… - European Journal of …, 2022 - Elsevier
Abstract Polo-like kinase 4 (PLK4) is a serine/threonine protein kinase involved in regulating
cell mitosis and centriole duplication, and has emerged as a therapeutic target for treating …
cell mitosis and centriole duplication, and has emerged as a therapeutic target for treating …
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 …
proposed as a therapeutic target for multiple cancers, especially TRIM37-amplified breast …
Design, synthesis, and biological evaluation of novel pyrazolo [3, 4-d] pyrimidine derivatives as potent PLK4 inhibitors for the treatment of TRIM37-amplified breast …
Y Sun, Y Sun, L Wang, T Wu, W Yin, J Wang… - European Journal of …, 2022 - Elsevier
Serine/threonine-protein kinase polo-like kinase 4 (PLK4) is a mitosis-associated protein
kinase that plays a vital role in the duplication of centrioles in dividing cells and is …
kinase that plays a vital role in the duplication of centrioles in dividing cells and is …
Radiotherapy and radiosensitization in breast cancer: Molecular targets and clinical applications
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 …
where local control of the primary or metastatic disease may be achieved by surgical …