Search Results - "O’Yang, Counde"

RO1138452 and RO3244794: characterization of structurally distinct, potent and selective IP (prostacyclin) receptor antagonists by Bley, Keith R, Bhattacharya, Anindya, Daniels, Don V, Gever, Joel, Jahangir, Alam, O'Yang, Counde, Smith, Steven, Srinivasan, Dinesh, Ford, Anthony P D W, Jett, Mary‐Frances

“…Prostacyclin (PGI2) possesses various physiological functions, including modulation of nociception, inflammation and cardiovascular activity. Elucidation of…”
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An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED by Qi, Wei, Zhao, Kehao, Gu, Justin, Huang, Ying, Wang, Youzhen, Zhang, Hailong, Zhang, Man, Zhang, Jeff, Yu, Zhengtian, Li, Ling, Teng, Lin, Chuai, Shannon, Zhang, Chao, Zhao, Mengxi, Chan, HoMan, Chen, Zijun, Fang, Douglas, Fei, Qi, Feng, Leying, Feng, Lijian, Gao, Yuan, Ge, Hui, Ge, Xinjian, Li, Guobin, Lingel, Andreas, Lin, Ying, Liu, Yueqin, Luo, Fangjun, Shi, Minlong, Wang, Long, Wang, Zhaofu, Yu, Yanyan, Zeng, Jue, Zeng, Chenhui, Zhang, Lijun, Zhang, Qiong, Zhou, Shaolian, Oyang, Counde, Atadja, Peter, Li, En

“…H3K27me3 binding to the EED pocket of the Polycomb repressive complex 2 (PRC2) is required to activate PRC2. An allosteric small-molecule inhibitor of PRC2 was…”
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Convenient Method for the 3-Functionalization of Isoindazoles by Bunnell, Aaron, O'Yang, Counde, Petrica, Andra, Soth, Michael J.

“…The C-3 position of isoindazoles is readily functionalized by metalation with lithium diisopropylamide followed by reaction with a variety of electrophiles…”
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Discovery of Small-Molecule Antagonists of the H3K9me3 Binding to UHRF1 Tandem Tudor Domain by Senisterra, Guillermo, Zhu, Hugh Y, Luo, Xiao, Zhang, Hailong, Xun, Guoliang, Lu, Chunliang, Xiao, Wen, Hajian, Taraneh, Loppnau, Peter, Chau, Irene, Li, Fengling, Allali-Hassani, Abdellah, Atadja, Peter, Oyang, Counde, Li, En, Brown, Peter J, Arrowsmith, Cheryl H, Zhao, Kehao, Yu, Zhengtian, Vedadi, Masoud

“…Ubiquitin-like with PHD and RING finger domains 1 (UHRF1) is a multidomain protein that plays a critical role in maintaining DNA methylation patterns through…”
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Synthesis and Biological Evaluation of Ketorolac Analogs by J. Lopez, Francisco, Jett, Mary-Frances, M. Muchowski, Joseph, Nitzan, Dov, O'Yang, Counde

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Synthesis of 10,10-difluorothromboxane A2, a potent and chemically stable thromboxane agonist by Fried, Josef, John, Varghese, Szwedo, Mitchell J, Chen, Chien Kuang, O'Yang, Counde, Morinelli, Thomas A, Okwu, Anselm K, Halushka, Perry V

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Discovery of First-in-Class, Potent, and Orally Bioavailable Embryonic Ectoderm Development (EED) Inhibitor with Robust Anticancer Efficacy by Huang, Ying, Zhang, Jeff, Yu, Zhengtian, Zhang, Hailong, Wang, Youzhen, Lingel, Andreas, Qi, Wei, Gu, Justin, Zhao, Kehao, Shultz, Michael D, Wang, Long, Fu, Xingnian, Sun, Yongfeng, Zhang, Qiong, Jiang, Xiangqing, Zhang, Jiangwei, Zhang, Chunye, Li, Ling, Zeng, Jue, Feng, Lijian, Zhang, Chao, Liu, Yueqin, Zhang, Man, Zhang, Lijun, Zhao, Mengxi, Gao, Zhenting, Liu, Xianghui, Fang, Douglas, Guo, Haibing, Mi, Yuan, Gabriel, Tobias, Dillon, Michael P, Atadja, Peter, Oyang, Counde

“…Overexpression and somatic heterozygous mutations of EZH2, the catalytic subunit of polycomb repressive complex 2 (PRC2), are associated with several tumor…”
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Discovery of the Clinical Candidate MAK683: An EED-Directed, Allosteric, and Selective PRC2 Inhibitor for the Treatment of Advanced Malignancies by Huang, Ying, Sendzik, Martin, Zhang, Jeff, Gao, Zhenting, Sun, Yongfeng, Wang, Long, Gu, Justin, Zhao, Kehao, Yu, Zhengtian, Zhang, Lijun, Zhang, Qiong, Blanz, Joachim, Chen, Zijun, Dubost, Valérie, Fang, Douglas, Feng, Lijian, Fu, Xingnian, Kiffe, Michael, Li, Ling, Luo, Fangjun, Luo, Xiao, Mi, Yuan, Mistry, Prakash, Pearson, David, Piaia, Alessandro, Scheufler, Clemens, Terranova, Remi, Weiss, Andreas, Zeng, Jue, Zhang, Hailong, Zhang, Jiangwei, Zhao, Mengxi, Dillon, Michael P, Jeay, Sebastien, Qi, Wei, Moggs, Jonathan, Pissot-Soldermann, Carole, Li, En, Atadja, Peter, Lingel, Andreas, Oyang, Counde

“…Polycomb Repressive Complex 2 (PRC2) plays an important role in transcriptional regulation during animal development and in cell differentiation, and…”
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Preclinical pharmacokinetics and metabolism of MAK683, a clinical stage selective oral embryonic ectoderm development (EED) inhibitor for cancer treatment by Zhang, Ji Yue (Jeff), Zhang, Jiangwei, Kiffe, Michael, Walles, Markus, Jin, Yi, Blanz, Joachim, Dayer, Jerôme, Sanchez, Arevalo, Zhang, Chunye, Zhang, Lijun, Huang, Ying, Oyang, Counde

“…MAK683 (N-((5-fluoro-2,3-dihydrobenzofuran-4-yl)methyl)-8-(2-methylpyridin-3-yl)-[1,2,4]triazolo[4,3-c]pyrimidin-5-amine) is a potent and orally bioavailable…”
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Quantitative Profiling of Combinational K27/K36 Modifications on Histone H3 Variants in Mouse Organs by Yu, Yanyan, Chen, Jiajia, Gao, Yuan, Gao, Jun, Liao, Rijing, Wang, Yi, Oyang, Counde, Li, En, Zeng, Chenhui, Zhou, Shaolian, Yang, Pengyuan, Jin, Hong, Yi, Wei

“…The coexisting post-translational modifications (PTMs) on histone H3 N-terminal tails were known to crosstalk between each other, indicating their…”
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Absolute Quantification of Histone PTM Marks by MRM-Based LC-MS/MS by Gao, Jun, Liao, Rijing, Yu, Yanyan, Zhai, Huili, Wang, Yingqi, Sack, Ragna, Peters, Antoine H. F. M, Chen, Jiajia, Wu, Haiping, Huang, Zheng, Hu, Min, Qi, Wei, Lu, Chris, Atadja, Peter, Oyang, Counde, Li, En, Yi, Wei, Zhou, Shaolian

“…The N-terminal tails of core histones harbor the sites of numerous post-translational modifications (PTMs) with important roles in the regulation of chromatin…”
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Characterization of the analgesic and anti-inflammatory activities of ketorolac and its enantiomers in the rat by Jett, M F, Ramesha, C S, Brown, C D, Chiu, S, Emmett, C, Voronin, T, Sun, T, O'Yang, C, Hunter, J C, Eglen, R M, Johnson, R M

“…The marked analgesic efficacy of ketorolac in humans, relative to other nonsteroidal anti-inflammatory drugs (NSAIDs), has lead to speculation as to whether…”
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Abstract 2461: Discovery of an orally available and liver-targeted ALPK1 agonist for cancer immunotherapy by Wang, Yupeng, Du, Nana, Dong, Xiaona, Sun, Xuebing, Hong, Yuan, Yang, Xiaolong, Ji, Zhijiang, Wang, Qianyu, Lv, Yun, Shi, Zhichen, Gao, Yajuan, Hou, Xiaofu, Zhang, Yaxin, Wang, Juan, Mao, Rui, Liu, Yinxin, Li, Liang, Ding, Jingjin, Wang, Hexiang, Hu, Nan, O’Yang, Counde, Li, Zhihong, Bley, Keith, Shao, Feng

“…Boosting anti-tumor immune responses can be achieved by activating the innate immune system. Despite the ongoing development of numerous STING and TLR agonists…”
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Abstract LB-288: An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED by Qi, Wei, Zhao, Kehao, Gu, Justin, Huang, Ying, Wang, Youzhen, Zhang, Hailong, Zhang, Man, Zhang, Jeff, Yu, Zhengtian, Li, Ling, Teng, Lin, Chuai, Shannon, Zhang, Chao, Zhao, Mengxi, Chan, HoMan, Chen, Zijun, Fang, Douglas, Qi, Fei, Feng, Leying, Feng, Lijian, Gao, Yuan, Ge, Hui, Ge, Xinjian, Lingel, Andreas, Li, Guobin, Lin, Ying, Liu, Yueqin, Luo, Fangjun, Shi, Minlong, Wang, Long, Wang, Zhaofu, Yu, Yanyan, Zeng, Jue, Zeng, Chenhui, Zhang, Lijun, Zhang, Qiong, Zhou, Shaolian, Oyang, Counde, Atadja, Peter, Li, En

“…Polycomb repressive complex 2 (PRC2) consists of three core subunits, EZH2, EED and SUZ12 and plays pivotal roles in transcriptional regulation through its…”
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Stability of prostacyclin analogues: an unusual lack of reactivity in acid-catalyzed alkene hydration by MAGILL, A, O'YANG, C, POWELL, M. F

“…Prostacyclin analogue 5 undergoes specific acid-catalyzed hydration (kH+ = 1.9 x 10(-7)M-1 sec-1 at 25 degrees C) and a pH-independent oxidation reaction (k0 =…”
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