Developing Spindlin1 small-molecule inhibitors by using protein microarrays

May 15th, 2017 by Narkhyun Bae

Nature Chemical Biology 13, 750 (2017). doi:10.1038/nchembio.2377

Authors: Narkhyun Bae, Monica Viviano, Xiaonan Su, Jie Lv, Donghang Cheng, Cari Sagum, Sabrina Castellano, Xue Bai, Claire Johnson, Mahmoud Ibrahim Khalil, Jianjun Shen, Kaifu Chen, Haitao Li, Gianluca Sbardella & Mark T Bedford

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A conserved threonine prevents self-intoxication of enoyl-thioester reductases

May 15th, 2017 by Raoul G Rosenthal

Nature Chemical Biology 13, 745 (2017). doi:10.1038/nchembio.2375

Authors: Raoul G Rosenthal, Bastian Vögeli, Tristan Wagner, Seigo Shima & Tobias J Erb

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Plasticity, dynamics, and inhibition of emerging tetracycline resistance enzymes

May 8th, 2017 by Jooyoung Park

Nature Chemical Biology 13, 730 (2017). doi:10.1038/nchembio.2376

Authors: Jooyoung Park, Andrew J Gasparrini, Margaret R Reck, Chanez T Symister, Jennifer L Elliott, Joseph P Vogel, Timothy A Wencewicz, Gautam Dantas & Niraj H Tolia

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Antibiotic resistance: Blocking tetracycline destruction

May 8th, 2017 by Sonja Petkovic

Nature Chemical Biology 13, 694 (2017). doi:10.1038/nchembio.2396

Authors: Sonja Petkovic & Winfried Hinrichs

Enzymology and structural and functional characterization of some FAD-dependent monooxygenases provide insights into degradation of tetracycline antibiotics, but also show unexpected features of substrate recognition, reaction mechanism, and competitive inhibition.

Membrane curvature regulates ligand-specific membrane sorting of GPCRs in living cells

May 8th, 2017 by Kadla R Rosholm

Nature Chemical Biology 13, 724 (2017). doi:10.1038/nchembio.2372

Authors: Kadla R Rosholm, Natascha Leijnse, Anna Mantsiou, Vadym Tkach, Søren L Pedersen, Volker F Wirth, Lene B Oddershede, Knud J Jensen, Karen L Martinez, Nikos S Hatzakis, Poul Martin Bendix, Andrew Callan-Jones & Dimitrios Stamou

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Computational design of ligand-binding membrane receptors with high selectivity

May 1st, 2017 by Xiang Feng

Nature Chemical Biology 13, 715 (2017). doi:10.1038/nchembio.2371

Authors: Xiang Feng, Joaquin Ambia, Kuang-Yui M Chen, Melvin Young & Patrick Barth

  • Posted in Nat Chem Biol, Publications
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Thiolutin is a zinc chelator that inhibits the Rpn11 and other JAMM metalloproteases

May 1st, 2017 by Linda Lauinger

Nature Chemical Biology 13, 709 (2017). doi:10.1038/nchembio.2370

Authors: Linda Lauinger, Jing Li, Anton Shostak, Ibrahim Avi Cemel, Nati Ha, Yaru Zhang, Philipp E Merkl, Simon Obermeyer, Nicolas Stankovic-Valentin, Tobias Schafmeier, Walter J Wever, Albert A Bowers, Kyle P Carter, Amy E Palmer, Herbert Tschochner, Frauke Melchior, Raymond J Deshaies, Michael Brunner & Axel Diernfellner

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Selective degradation of splicing factor CAPERα by anticancer sulfonamides

April 24th, 2017 by Taisuke Uehara

Nature Chemical Biology 13, 675 (2017). doi:10.1038/nchembio.2363

Authors: Taisuke Uehara, Yukinori Minoshima, Koji Sagane, Naoko Hata Sugi, Kaoru Ogawa Mitsuhashi, Noboru Yamamoto, Hiroshi Kamiyama, Kentaro Takahashi, Yoshihiko Kotake, Mai Uesugi, Akira Yokoi, Atsushi Inoue, Taku Yoshida, Miyuki Mabuchi, Akito Tanaka & Takashi Owa

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Immunology: Mind the immuno-connection gap

April 24th, 2017 by Wolfgang Link

Nature Chemical Biology 13, 572 (2017). doi:10.1038/nchembio.2373

Author: Wolfgang Link

Biologic drugs that modulate the immune system have revolutionized the therapeutic landscape for several selected cancer types. A new study reports an image-based assay system to monitor cell–cell interactions, identifying small-molecule compounds with immunomodulatory capacity.

Protein degradation: DCAFinating splicing

April 24th, 2017 by Georg E Winter

Nature Chemical Biology 13, 575 (2017). doi:10.1038/nchembio.2378

Author: Georg E Winter

Chemical control of protein homeostasis and induction of protein destabilization are emerging therapeutic strategies. Two recent studies identify a set of sulfonamides that can modulate the CRL4DCAF15 E3 ligase complex to target the splicing factor RBM39 for proteasomal degradation.