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Your search keyword '"Ardayfio, Ophelia"' showing total 6 results
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6 results on '"Ardayfio, Ophelia"'

2. Selective inhibition of Ezh2 by a small molecule inhibitor blocks tumor cells proliferation

Author

Qi, Wei, Chan, HoMan, Tenga, Lin, Li, Ling, Chuai, Shannon, Zhang, Ruipeng, Zeng, Jue, Li, Min, Fan, Hong, Lin, Ying, Gu, Justin, Ardayfio, Ophelia, Zhang, Ji-Hu, Yan, Xiaoxia, Fang, Jialuo, Mi, Yuan, Zhang, Man, Zhou, Tao, Feng, Grace, Chen, Zijun, Li, Guobin, Yang, Teddy, Zhao, Kehao, Liu, Xianghui, Yu, Zhengtian, Lu, Chris X., Atadja, Peter, and Li, En

Published
2012

3. Identification of Orally Available Naphthyridine Protein Kinase D Inhibitors

Author

Meredith, Erik L., Ardayfio, Ophelia, Beattie, Kimberly, Dobler, Markus R., Enyedy, Istvan, Gaul, Christoph, Hosagrahara, Vinayak, Jewell, Charles, Koch, Keith, Lee, Wendy, Lehmann, HansJoerg, McKinsey, Timothy A., Miranda, Karl, Pagratis, Nikos, Pancost, Margaret, Patnaik, Anup, Phan, Dillon, Plato, Craig, Qian, Ming, Rajaraman, Vasumathy, Rao, Chang, Rozhitskaya, Olga, Ruppen, Thomas, Shi, Jie, Siska, Sarah J., Springer, Clayton, van Eis, Maurice, Vega, Richard B., von Matt, Anette, Yang, Lihua, Yoon, Taeyoung, Zhang, Ji-Hu, Zhu, Na, and Monovich, Lauren G.

Abstract

A novel 2,6-naphthyridine was identified by high throughput screen (HTS) as a dual protein kinase C/D (PKC/PKD) inhibitor. PKD inhibition in the heart was proposed as a potential antihypertrophic mechanism with application as a heart failure therapy. As PKC was previously identified as the immediate upstream activator of PKD, PKD vs PKC selectivity was essential to understand the effect of PKD inhibition in models of cardiac hypertrophy and heart failure. The present study describes the modification of the HTS hit to a series of prototype pan-PKD inhibitors with routine 1000-fold PKD vs PKC selectivity. Example compounds inhibited PKD activity in vitro, in cells, and in vivo following oral administration. Their effects on heart morphology and function are discussed herein.

Published
2024
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4. Discovery and Molecular Basis of a Diverse Set of Polycomb Repressive Complex 2 Inhibitors Recognition by EED

Author

Li, Ling, primary, Zhang, Hailong, additional, Zhang, Man, additional, Zhao, Mengxi, additional, Feng, Lijian, additional, Luo, Xiao, additional, Gao, Zhenting, additional, Huang, Ying, additional, Ardayfio, Ophelia, additional, Zhang, Ji-Hu, additional, Lin, Ying, additional, Fan, Hong, additional, Mi, Yuan, additional, Li, Guobin, additional, Liu, Lei, additional, Feng, Leying, additional, Luo, Fangjun, additional, Teng, Lin, additional, Qi, Wei, additional, Ottl, Johannes, additional, Lingel, Andreas, additional, Bussiere, Dirksen E., additional, Yu, Zhengtian, additional, Atadja, Peter, additional, Lu, Chris, additional, Li, En, additional, Gu, Justin, additional, and Zhao, Kehao, additional

Published
2017
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5. Identification of Orally Available Naphthyridine Protein Kinase D Inhibitors

Author

Meredith, Erik L., primary, Ardayfio, Ophelia, additional, Beattie, Kimberly, additional, Dobler, Markus R., additional, Enyedy, Istvan, additional, Gaul, Christoph, additional, Hosagrahara, Vinayak, additional, Jewell, Charles, additional, Koch, Keith, additional, Lee, Wendy, additional, Lehmann, HansJoerg, additional, McKinsey, Timothy A., additional, Miranda, Karl, additional, Pagratis, Nikos, additional, Pancost, Margaret, additional, Patnaik, Anup, additional, Phan, Dillon, additional, Plato, Craig, additional, Qian, Ming, additional, Rajaraman, Vasumathy, additional, Rao, Chang, additional, Rozhitskaya, Olga, additional, Ruppen, Thomas, additional, Shi, Jie, additional, Siska, Sarah J., additional, Springer, Clayton, additional, van Eis, Maurice, additional, Vega, Richard B., additional, von Matt, Anette, additional, Yang, Lihua, additional, Yoon, Taeyoung, additional, Zhang, Ji-Hu, additional, Zhu, Na, additional, and Monovich, Lauren G., additional

Published
2010
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6. Selective inhibition of Ezh2 by a small molecule inhibitor blocks tumor cells proliferation.

Author

Wei Qi, Chan, HoMan, Lin Teng, Ling Li, Chuai, Shannon, Ruipeng Zhang, Jue Zeng, Min Li, Hong Fan, Ying Lin, Gu, Justin, Ardayfio, Ophelia, Ji-Hu Zhang, Xiaoxia Yan, Jialuo Fang, Yuan Mi, Man Zhang, Tao Zhou, Feng, Grace, and Zijun Chen

Subjects
CONTACT inhibition, CANCER cells, CELL proliferation, GENE expression, GENETIC mutation, HISTONES
Abstract

Ezh2 (Enhancer of zeste homolog 2) protein is the enzymatic component of the Polycomb repressive complex 2 (PRC2), which represses gene expression by methylating lysine 27 of histone H3 (H3K27) and regulates cell proliferation and differentiation during embryonic development. Recently, hot-spot mutations of Ezh2 were identified in diffused large B-cell lymphomas and follicular lymphomas. To investigate if tumor growth is dependent on the enzymatic activity of Ezh2, we developed a potent and selective small molecule inhibitor, EI1, which inhibits the enzymatic activity of Ezh2 through direct binding to the enzyme and competing with the methyl group donor S-Adenosyl methionine. EI1-treated cells exhibit genome-wide loss of H3K27 methylation and activation of PRC2 target genes. Furthermore, inhibition of Ezh2 by EI1 in diffused large B-cell lymphomas cells carrying the Y641 mutations results in decreased proliferation, cell cycle arrest, and apoptosis. These results provide strong validation of Ezh2 as a potential therapeutic target for the treatment of cancer. [ABSTRACT FROM AUTHOR]

Published
2012
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