A water-mediated allosteric network governs activation of Aurora kinase A

February 6th, 2017 by Soreen Cyphers

Nature Chemical Biology 13, 402 (2017). doi:10.1038/nchembio.2296

Authors: Soreen Cyphers, Emily F Ruff, Julie M Behr, John D Chodera & Nicholas M Levinson

  • Posted in Nat Chem Biol, Publications
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In vitro reconstitution demonstrates the cell wall ligase activity of LCP proteins

February 6th, 2017 by Kaitlin Schaefer

Nature Chemical Biology 13, 396 (2017). doi:10.1038/nchembio.2302

Authors: Kaitlin Schaefer, Leigh M Matano, Yuan Qiao, Daniel Kahne & Suzanne Walker

  • Posted in Nat Chem Biol, Publications
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Call for Papers: 254th ACS Meeting August 20-24, 2017 in Washington DC

February 2nd, 2017 by pthomas2

Abstract deadline Monday March 20, 2017. In addition to poster sessions, there will be oral sessions for contributed papers from Graduate students and postdocs, Early Career Investigators and Mid-Career Investigators. Speakers for these symposia will be selected from the submitted abstracts. If your abstract is not chosen for an oral presentation, it will be moved to a poster session. Click here to submit abstract.

  • Posted in DBC News
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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.

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

  • Posted in Nat Chem Biol, Publications
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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

  • Posted in Nat Chem Biol, Publications
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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

  • Posted in Nat Chem Biol, Publications
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Structural Basis for the Lesion-scanning Mechanism of the Bacterial MutY DNA Glycosylase [Enzymology]

January 27th, 2017 by Lan Wang, Srinivas Chakravarthy, Gregory L Verdine

The highly mutagenic A:oxoG (8-oxoguanine) base-pair is generated mainly by misreplication of the C:oxoG base-pair, the oxidation product of the C:G base-pair. A:oxoG base-pair is particularly insidious because neither base in it carries faithful information to direct the repair of the other. The bacterial MutY (MUTYH in humans) adenine DNA glycosylase is able to initiate the repair of A:oxoG by selectively cleaving the A base from the A:oxoG base-pair. The difference between faithful repair and wreaking mutagenic havoc on the genome lies in the accurate discrimination between two structurally similar base-pairs: A:oxoG and A:T. Here we present two crystal structures of the MutY N-terminal domain in complex with either undamaged DNA or DNA containing an intrahelical lesion. These structures have captured for the first time, a DNA glycosylase scanning the genome for a damaged base in the very first stage of lesion-recognition and the base-extrusion pathway. The mode of interaction observed here has suggested a common lesion-scanning mechanism across the entire helix-hairpin-helix superfamily to which MutY belongs. In addition, small-angle X-ray scattering (SAXS) studies together with accompanying biochemical assays have suggested a possible role played by the C-terminal oxoG-recognition domain of MutY in lesion-scanning.

Cyclotide Structure and Function: The Role of Membrane Binding and Permeation

January 27th, 2017 by Sónia Troeira Henriques and David J. Craik

TOC Graphic

Biochemistry
DOI: 10.1021/acs.biochem.6b01212

Draft Program for ACS 253rd National Meeting

January 24th, 2017 by pthomas2

The draft program for the 253rd ACS National Meeting to be held in San Francisco, CA from April 2-6 can be found here: Download Program.