scholarly journals Identification and Assessments of Novel and Potent Small-Molecule Inhibitors of EED–EZH2 Interaction of Polycomb Repressive Complex 2 by Computational Methods and Biological Evaluations

2020 ◽  
Vol 68 (1) ◽  
pp. 58-63 ◽  
Author(s):  
Kongkai Zhu ◽  
Daohai Du ◽  
Rui Yang ◽  
Hongrui Tao ◽  
Hua Zhang
Keyword(s):  
Computational Methods ◽  
Small Molecule ◽  
Small Molecule Inhibitors ◽  
Polycomb Repressive Complex ◽  
Polycomb Repressive Complex 2

Small Molecule Approaches for Targeting the Polycomb Repressive Complex 2 (PRC2) in Cancer

2020 ◽  
Vol 63 (24) ◽  
pp. 15344-15370
Author(s):  
M. Cynthia Martin ◽  
Guihua Zeng ◽  
Jindan Yu ◽  
Gary E. Schiltz
Keyword(s):  
Small Molecule ◽  
Polycomb Repressive Complex ◽  
Polycomb Repressive Complex 2

scholarly journals Identification of Novel Potential VEGFR-2 Inhibitors Using a Combination of Computational Methods for Drug Discovery

Life ◽  
2021 ◽  
Vol 11 (10) ◽  
pp. 1070
Author(s):  
Mohammad M. Al-Sanea ◽  
Garri Chilingaryan ◽  
Narek Abelyan ◽  
Arsen Sargsyan ◽  
Sargis Hovhannisyan ◽  
...  
Keyword(s):  
Drug Discovery ◽  
Computational Methods ◽  
Small Molecule ◽  
Small Molecule Inhibitors ◽  
Acquired Resistance ◽  
Growth Factor Receptor ◽  
Clinical Effects ◽  
Wide Range ◽  
Critical Issues ◽  
Endothelial Growth Factor

The vascular endothelial growth factor receptor 2 (VEGFR-2) is largely recognized as a potent therapeutic molecular target for the development of angiogenesis-related tumor treatment. Tumor growth, metastasis and multidrug resistance highly depends on the angiogenesis and drug discovery of the potential small molecules targeting VEGFR-2, with the potential anti-angiogenic activity being of high interest to anti-cancer research. Multiple small molecule inhibitors of the VEGFR-2 are approved for the treatment of different type of cancers, with one of the most recent, tivozanib, being approved by the FDA for the treatment of relapsed or refractory advanced renal cell carcinoma (RCC). However, the endogenous and acquired resistance of the protein, toxicity of compounds and wide range of side effects still remain critical issues, which lead to the short-term clinical effects and failure of antiangiogenic drugs. We applied a combination of computational methods and approaches for drug design and discovery with the goal of finding novel, potential and small molecule inhibitors of VEGFR2, as alternatives to the known inhibitors’ chemical scaffolds and components. From studying several of these compounds, the derivatives of pyrido[1,2-a]pyrimidin-4-one and isoindoline-1,3-dione in particular were identified.

scholarly journals Small-molecule inhibitors targeting Polycomb repressive complex 1 RING domain

2021 ◽  
Author(s):  
Shirish Shukla ◽  
Weijiang Ying ◽  
Felicia Gray ◽  
Yiwu Yao ◽  
Miranda L. Simes ◽  
...  
Keyword(s):  
Small Molecule ◽  
Small Molecule Inhibitors ◽  
Ring Domain ◽  
Polycomb Repressive Complex ◽  
Polycomb Repressive Complex 1
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