Target validation: Switching domains

August 18th, 2016 by Alessio Ciulli

Nature Chemical Biology 12, 659 (2016). doi:10.1038/nchembio.2154

Author: Alessio Ciulli

Chemical probes and drugs often bind to functional domains on disease-relevant proteins. A study suggests a chemical genetic approach to establish on-target effects by swapping the targeted domain, affording resistance to pharmacological inhibition while retaining functionality.

Chemical synthesis: Linking up lysines

August 18th, 2016 by Caitlin Deane

Nature Chemical Biology 12, 657 (2016). doi:10.1038/nchembio.2163

Author: Caitlin Deane

Discovery of allosteric modulators for GABAA receptors by ligand-directed chemistry

August 15th, 2016 by Kei Yamaura

Nature Chemical Biology 12, 822 (2016). doi:10.1038/nchembio.2150

Authors: Kei Yamaura, Shigeki Kiyonaka, Tomohiro Numata, Ryuji Inoue & Itaru Hamachi

  • Posted in Nat Chem Biol, Publications
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TALE proteins search DNA using a rotationally decoupled mechanism

August 15th, 2016 by Luke Cuculis

Nature Chemical Biology 12, 831 (2016). doi:10.1038/nchembio.2152

Authors: Luke Cuculis, Zhanar Abil, Huimin Zhao & Charles M Schroeder

Structural basis of laminin binding to the LARGE glycans on dystroglycan

August 15th, 2016 by David C Briggs

Nature Chemical Biology 12, 810 (2016). doi:10.1038/nchembio.2146

Authors: David C Briggs, Takako Yoshida-Moriguchi, Tianqing Zheng, David Venzke, Mary E Anderson, Andrea Strazzulli, Marco Moracci, Liping Yu, Erhard Hohenester & Kevin P Campbell

  • Posted in Nat Chem Biol, Publications
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Cellularly active N-hydroxyurea FEN1 inhibitors block substrate entry to the active site

August 15th, 2016 by Jack C Exell

Nature Chemical Biology 12, 815 (2016). doi:10.1038/nchembio.2148

Authors: Jack C Exell, Mark J Thompson, L David Finger, Steven J Shaw, Judit Debreczeni, Thomas A Ward, Claire McWhirter, Catrine L B Siöberg, Daniel Martinez Molina, W Mark Abbott, Clifford D Jones, J Willem M Nissink, Stephen T Durant & Jane A Grasby

  • Posted in Nat Chem Biol, Publications
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Inhibiting androgen receptor nuclear entry in castration-resistant prostate cancer

August 8th, 2016 by Julie A Pollock

Nature Chemical Biology 12, 795 (2016). doi:10.1038/nchembio.2131

Authors: Julie A Pollock, Suzanne E Wardell, Alexander A Parent, David B Stagg, Stephanie J Ellison, Holly M Alley, Christina A Chao, Scott A Lawrence, James P Stice, Ivan Spasojevic, Jennifer G Baker, Sung Hoon Kim, Donald P McDonnell, John A Katzenellenbogen & John D Norris

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A hybrid polyketide–nonribosomal peptide in nematodes that promotes larval survival

August 8th, 2016 by Qingyao Shou

Nature Chemical Biology 12, 770 (2016). doi:10.1038/nchembio.2144

Authors: Qingyao Shou, Likui Feng, Yaoling Long, Jungsoo Han, Joshawna K Nunnery, David H Powell & Rebecca A Butcher

Polyketides and nonribosomal peptides are two important types of natural products that are produced by many species of bacteria and fungi but are exceedingly rare in metazoans. Here, we elucidate the structure of a hybrid polyketide–nonribosomal peptide from Caenorhabditis elegans that is produced in the canal-associated neurons (CANs) and promotes survival during starvation-induced larval arrest. Our results uncover a novel mechanism by which animals respond to nutrient fluctuations to extend survival.

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FRET binding antenna reports spatiotemporal dynamics of GDI–Cdc42 GTPase interactions

August 8th, 2016 by Louis Hodgson

Nature Chemical Biology 12, 802 (2016). doi:10.1038/nchembio.2145

Authors: Louis Hodgson, Désirée Spiering, Mohsen Sabouri-Ghomi, Onur Dagliyan, Céline DerMardirossian, Gaudenz Danuser & Klaus M Hahn

  • Posted in Nat Chem Biol, Publications
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Metabolic plasticity underpins innate and acquired resistance to LDHA inhibition

August 1st, 2016 by Aaron Boudreau

Nature Chemical Biology 12, 779 (2016). doi:10.1038/nchembio.2143

Authors: Aaron Boudreau, Hans E Purkey, Anna Hitz, Kirk Robarge, David Peterson, Sharada Labadie, Mandy Kwong, Rebecca Hong, Min Gao, Christopher Del Nagro, Raju Pusapati, Shuguang Ma, Laurent Salphati, Jodie Pang, Aihe Zhou, Tommy Lai, Yingjie Li, Zhongguo Chen, Binqing Wei, Ivana Yen, Steve Sideris, Mark McCleland, Ron Firestein, Laura Corson, Alex Vanderbilt, Simon Williams, Anneleen Daemen, Marcia Belvin, Charles Eigenbrot, Peter K Jackson, Shiva Malek, Georgia Hatzivassiliou, Deepak Sampath, Marie Evangelista & Thomas O'Brien

  • Posted in Nat Chem Biol, Publications
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