A new window on cancer therapy? Targeting the nucleolus and ribosome biogenesis using the small molecule inhibitor of polymerase I transcription, CX-5461

2015 ◽  
Vol 4 (2) ◽  
pp. 61-65
Author(s):  
Simon J Harrison ◽  
Amee George ◽  
Ross Hannan
Keyword(s):  
Cancer Therapy ◽  
Small Molecule ◽  
Ribosome Biogenesis ◽  
Small Molecule Inhibitor ◽  
Molecule Inhibitor ◽  
Polymerase I

scholarly journals Discovery of fruquintinib, a potent and highly selective small molecule inhibitor of VEGFR 1, 2, 3 tyrosine kinases for cancer therapy

2014 ◽  
Vol 15 (12) ◽  
pp. 1635-1645 ◽  
Author(s):  
Qiaoling Sun ◽  
Jinghong Zhou ◽  
Zheng Zhang ◽  
Mingchuan Guo ◽  
Junqing Liang ◽  
...  
Keyword(s):  
Cancer Therapy ◽  
Small Molecule ◽  
Tyrosine Kinases ◽  
Small Molecule Inhibitor ◽  
Molecule Inhibitor

scholarly journals Diverse Landscape Of Dermatologic Toxicities From Small Molecule Inhibitor Cancer Therapy

2021 ◽  
Author(s):  
Riyad N. H. Seervai ◽  
Woo Cheal Cho ◽  
Emily Y. Chu ◽  
Mario L. Marques‐Piubelli ◽  
Debora A. Ledesma ◽  
...  
Keyword(s):  
Cancer Therapy ◽  
Small Molecule ◽  
Small Molecule Inhibitor ◽  
Molecule Inhibitor

Abstract 797: Discovery of a highly selective and potent small molecule inhibitor against c-MET for cancer therapy

2015 ◽  
Author(s):  
Rudi Bao ◽  
Zhongzong Pan ◽  
Zhiming Zhao ◽  
Hongping Yu ◽  
Yaochang Xu
Keyword(s):  
Cancer Therapy ◽  
Small Molecule ◽  
Small Molecule Inhibitor ◽  
Molecule Inhibitor

Abstract 1729: Discovery of a synthetic small molecule inhibitor of HSP90 for cancer therapy

2015 ◽  
Author(s):  
Rudi Bao ◽  
Zhongzong Pan ◽  
Zhiming Zhao ◽  
Hongping Yu ◽  
Yaochang Xu
Keyword(s):  
Cancer Therapy ◽  
Small Molecule ◽  
Small Molecule Inhibitor ◽  
Molecule Inhibitor ◽  
Synthetic Small Molecule

scholarly journals Targeting DDX 3 with a small molecule inhibitor for lung cancer therapy

2015 ◽  
Vol 7 (5) ◽  
pp. 648-669 ◽  
Author(s):  
Guus M Bol ◽  
Farhad Vesuna ◽  
Min Xie ◽  
Jing Zeng ◽  
Khaled Aziz ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Cancer Therapy ◽  
Small Molecule ◽  
Small Molecule Inhibitor ◽  
Molecule Inhibitor ◽  
Lung Cancer Therapy

scholarly journals Development of Oxadiazole-Based ODZ10117 as a Small-Molecule Inhibitor of STAT3 for Targeted Cancer Therapy

2019 ◽  
Vol 8 (11) ◽  
pp. 1847 ◽  
Author(s):  
Kim ◽  
Lee ◽  
Song ◽  
Park ◽  
Gadhe ◽  
...  
Keyword(s):  
Cancer Therapy ◽  
Small Molecule ◽  
Nuclear Translocation ◽  
Small Molecule Inhibitor ◽  
Sh2 Domain ◽  
Migration And Invasion ◽  
Targeted Cancer Therapy ◽  
In Vivo Models ◽  
Molecule Inhibitor

Persistently activated STAT3 is a promising target for a new class of anticancer drug development and cancer therapy, as it is associated with tumor initiation, progression, malignancy, drug resistance, cancer stem cell properties, and recurrence. Here, we discovered 3-(2,4-dichloro-phenoxymethyl)-5-trichloromethyl-[1,2,4]oxadiazole (ODZ10117) as a small-molecule inhibitor of STAT3 to be used in STAT3-targeted cancer therapy. ODZ10117 targeted the SH2 domain of STAT3 regardless of other STAT family proteins and upstream regulators of STAT3, leading to inhibition of the tyrosine phosphorylation, dimerization, nuclear translocation, and transcriptional activity of STAT3. The inhibitory effect of ODZ10117 on STAT3 was stronger than the known STAT3 inhibitors such as S3I-201, STA-21, and nifuroxazide. ODZ10117 suppressed the migration and invasion, induced apoptosis, reduced tumor growth and lung metastasis, and extended the survival rate in both in vitro and in vivo models of breast cancer. Overall, we demonstrated that ODZ10117 is a novel STAT3 inhibitor and may be a promising agent for the development of anticancer drugs.

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