HTS-compatible FRET-based conformational sensors clarify membrane receptor activation

January 30th, 2017 by Pauline Scholler

Nature Chemical Biology 13, 372 (2017). doi:10.1038/nchembio.2286

Authors: Pauline Scholler, David Moreno-Delgado, Nathalie Lecat-Guillet, Etienne Doumazane, Carine Monnier, Fabienne Charrier-Savournin, Ludovic Fabre, Cédric Chouvet, Stéphanie Soldevila, Laurent Lamarque, Geoffrey Donsimoni, Thomas Roux, Jurriaan M Zwier, Eric Trinquet, Philippe Rondard & Jean-Philippe Pin

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The EED protein–protein interaction inhibitor A-395 inactivates the PRC2 complex

January 30th, 2017 by Yupeng He

Nature Chemical Biology 13, 389 (2017). doi:10.1038/nchembio.2306

Authors: Yupeng He, Sujatha Selvaraju, Michael L Curtin, Clarissa G Jakob, Haizhong Zhu, Kenneth M Comess, Bailin Shaw, Juliana The, Evelyne Lima-Fernandes, Magdalena M Szewczyk, Dong Cheng, Kelly L Klinge, Huan-Qiu Li, Marina Pliushchev, Mikkel A Algire, David Maag, Jun Guo, Justin Dietrich, Sanjay C Panchal, Andrew M Petros, Ramzi F Sweis, Maricel Torrent, Lance J Bigelow, Guillermo Senisterra, Fengling Li, Steven Kennedy, Qin Wu, Donald J Osterling, David J Lindley, Wenqing Gao, Scott Galasinski, Dalia Barsyte-Lovejoy, Masoud Vedadi, Fritz G Buchanan, Cheryl H Arrowsmith, Gary G Chiang, Chaohong Sun & William N Pappano

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An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED

January 30th, 2017 by Wei Qi

Nature Chemical Biology 13, 381 (2017). doi:10.1038/nchembio.2304

Authors: Wei Qi, Kehao Zhao, Justin Gu, Ying Huang, Youzhen Wang, Hailong Zhang, Man Zhang, Jeff Zhang, Zhengtian Yu, Ling Li, Lin Teng, Shannon Chuai, Chao Zhang, Mengxi Zhao, HoMan Chan, Zijun Chen, Douglas Fang, Qi Fei, Leying Feng, Lijian Feng, Yuan Gao, Hui Ge, Xinjian Ge, Guobin Li, Andreas Lingel, Ying Lin, Yueqin Liu, Fangjun Luo, Minlong Shi, Long Wang, Zhaofu Wang, Yanyan Yu, Jue Zeng, Chenhui Zeng, Lijun Zhang, Qiong Zhang, Shaolian Zhou, Counde Oyang, Peter Atadja & En Li

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Chromatin biology: Breaking into the PRC2 cage

January 30th, 2017 by Daniel Holoch

Nature Chemical Biology 13, 345 (2017). doi:10.1038/nchembio.2313

Authors: Daniel Holoch & Raphaël Margueron

New small-molecule inhibitors of the histone methyltransferase PRC2 interfere with the allosteric activation of enzymatic activity. These compounds are effective against PRC2-dependent tumors that are resistant to catalytic inhibitors and provide important new tools for altering chromatin regulation.

Akt3 is a privileged first responder in isozyme-specific electrophile response

January 23rd, 2017 by Marcus J C Long

Nature Chemical Biology 13, 333 (2017). doi:10.1038/nchembio.2284

Authors: Marcus J C Long, Saba Parvez, Yi Zhao, Sanjna L Surya, Yiran Wang, Sheng Zhang & Yimon Aye

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Enzyme-catalyzed cationic epoxide rearrangements in quinolone alkaloid biosynthesis

January 23rd, 2017 by Yi Zou

Nature Chemical Biology 13, 325 (2017). doi:10.1038/nchembio.2283

Authors: Yi Zou, Marc Garcia-Borràs, Mancheng C Tang, Yuichiro Hirayama, Dehai H Li, Li Li, Kenji Watanabe, K N Houk & Yi Tang

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Redox regulation: Taking AKTion on HNEs

January 23rd, 2017 by Eranthie Weerapana

Nature Chemical Biology 13, 244 (2017). doi:10.1038/nchembio.2311

Author: Eranthie Weerapana

Differential redox regulation of kinase isoforms serves to provide intricate control of cellular signaling events. In a new study, a single isoform of Akt, Akt3, is shown to be preferentially modified by lipid-derived electrophiles to modulate downstream signaling events in mammalian cells and zebrafish.

The SUV4-20 inhibitor A-196 verifies a role for epigenetics in genomic integrity

January 23rd, 2017 by Kenneth D Bromberg

Nature Chemical Biology 13, 317 (2017). doi:10.1038/nchembio.2282

Authors: Kenneth D Bromberg, Taylor R H Mitchell, Anup K Upadhyay, Clarissa G Jakob, Manisha A Jhala, Kenneth M Comess, Loren M Lasko, Conglei Li, Creighton T Tuzon, Yujia Dai, Fengling Li, Mohammad S Eram, Alexander Nuber, Niru B Soni, Vlasios Manaves, Mikkel A Algire, Ramzi F Sweis, Maricel Torrent, Gunnar Schotta, Chaohong Sun, Michael R Michaelides, Alex R Shoemaker, Cheryl H Arrowsmith, Peter J Brown, Vijayaratnam Santhakumar, Alberto Martin, Judd C Rice, Gary G Chiang, Masoud Vedadi, Dalia Barsyte-Lovejoy & William N Pappano

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Susan Lindquist (1949–2016)

January 19th, 2017 by Tricia R Serio

Nature Chemical Biology 13, 127 (2017). doi:10.1038/nchembio.2305

Author: Tricia R Serio

Susan Lindquist passed away on 27 October 2016, far too early for those who marveled at her brilliance through her many contributions to science, for all who knew her directly, and especially for her former trainees.

RNA modification: Reading Sex-lethal

January 19th, 2017 by Grant Miura

Nature Chemical Biology 13, 129 (2017). doi:10.1038/nchembio.2291

Author: Grant Miura