Nature Chemical Biology

Patch-clamp fluorometry measurements of cAMP binding and channel opening combined with global kinetic fitting revealed that ligand binding to the tetrameric hyperpolarization-activated cyclic nucleotide–gated channel is favored at the second and fourth binding events.

Categories: Journals

Glycobiology: Enzyme deficiencies deciphered

Wed, 01/18/2012 - 00:00

Glycobiology: Enzyme deficiencies deciphered

Nature Chemical Biology 8, 137 (2012). doi:10.1038/nchembio.778

Author: Lena Kjellén

Mucopolysaccharidoses are inherited disorders in which inactivation of lysosomal enzymes results in accumulation of glycosaminoglycans within cells, causing tissue and organ dysfunction. A method to determine the unique end structures of the accumulated glycosaminoglycans offers a new way for diagnosis.

Categories: Journals

Signaling: An oxysterol ligand for Smoothened

Wed, 01/18/2012 - 00:00

Signaling: An oxysterol ligand for Smoothened

Nature Chemical Biology 8, 139 (2012). doi:10.1038/nchembio.774

Authors: Hayley J Sharpe & Frederic J de Sauvage

20(S)-hydroxycholesterol, a naturally occurring oxysterol, activates the Hedgehog signaling pathway by directly binding an allosteric site on Smoothened.

Categories: Journals

Disease-specific non–reducing end carbohydrate biomarkers for mucopolysaccharidoses

Sun, 01/08/2012 - 00:00

Disease-specific non–reducing end carbohydrate biomarkers for mucopolysaccharidoses

Nature Chemical Biology 8, 197 (2012). doi:10.1038/nchembio.766

Authors: Roger Lawrence, Jillian R Brown, Kanar Al-Mafraji, William C Lamanna, James R Beitel, Geert-Jan Boons, Jeffrey D Esko & Brett E Crawford

Categories: Journals

Timing facilitated site transfer of an enzyme on DNA

Sun, 01/08/2012 - 00:00

Timing facilitated site transfer of an enzyme on DNA

Nature Chemical Biology 8, 205 (2012). doi:10.1038/nchembio.764

Authors: Joseph D Schonhoft & James T Stivers

Categories: Journals

Oxysterols are allosteric activators of the oncoprotein Smoothened

Sun, 01/08/2012 - 00:00

Oxysterols are allosteric activators of the oncoprotein Smoothened

Nature Chemical Biology 8, 211 (2012). doi:10.1038/nchembio.765

Authors: Sigrid Nachtergaele, Laurel K Mydock, Kathiresan Krishnan, Jayan Rammohan, Paul H Schlesinger, Douglas F Covey & Rajat Rohatgi

Categories: Journals

Skepinone-L is a selective p38 mitogen-activated protein kinase inhibitor

Sun, 12/25/2011 - 00:00

Skepinone-L is a selective p38 mitogen-activated protein kinase inhibitor

Nature Chemical Biology 8, 141 (2012). doi:10.1038/nchembio.761

Authors: Solveigh C Koeberle, Johannes Romir, Stefan Fischer, Andreas Koeberle, Verena Schattel, Wolfgang Albrecht, Christian Grütter, Oliver Werz, Daniel Rauh, Thilo Stehle & Stefan A Laufer

Until now, a lack of inhibitors with high potency and selectivity in vivo has hampered investigation of the p38 mitogen-activated protein kinase (MAPK) signaling pathway. We describe the design of skepinone-L, which is, to our knowledge, the first ATP-competitive p38 MAPK inhibitor with excellent in vivo efficacy and selectivity. Therefore, skepinone-L is a valuable probe for chemical biology research, and it may foster the development of a unique class of kinase inhibitors.

Categories: Journals

Primary amines protect against retinal degeneration in mouse models of retinopathies

Sun, 12/25/2011 - 00:00

Primary amines protect against retinal degeneration in mouse models of retinopathies

Nature Chemical Biology 8, 170 (2012). doi:10.1038/nchembio.759

Authors: Akiko Maeda, Marcin Golczak, Yu Chen, Kiichiro Okano, Hideo Kohno, Satomi Shiose, Kaede Ishikawa, William Harte, Grazyna Palczewska, Tadao Maeda & Krzysztof Palczewski

Categories: Journals

Natural product–inspired cascade synthesis yields modulators of centrosome integrity

Sun, 12/25/2011 - 00:00

Natural product–inspired cascade synthesis yields modulators of centrosome integrity

Nature Chemical Biology 8, 179 (2012). doi:10.1038/nchembio.758

Authors: Heiko Dückert, Verena Pries, Vivek Khedkar, Sascha Menninger, Hanna Bruss, Alexander W Bird, Zoltan Maliga, Andreas Brockmeyer, Petra Janning, Anthony Hyman, Stefan Grimme, Markus Schürmann, Hans Preut, Katja Hübel, Slava Ziegler, Kamal Kumar & Herbert Waldmann

Categories: Journals

Small-molecule proteostasis regulators for protein conformational diseases

Sun, 12/25/2011 - 00:00

Small-molecule proteostasis regulators for protein conformational diseases

Nature Chemical Biology 8, 185 (2012). doi:10.1038/nchembio.763

Authors: Barbara Calamini, Maria Catarina Silva, Franck Madoux, Darren M Hutt, Shilpi Khanna, Monica A Chalfant, S Adrian Saldanha, Peter Hodder, Bradley D Tait, Dan Garza, William E Balch & Richard I Morimoto

Categories: Journals

Chemical informatics and target identification in a zebrafish phenotypic screen

Sun, 12/18/2011 - 00:00

Chemical informatics and target identification in a zebrafish phenotypic screen

Nature Chemical Biology 8, 144 (2012). doi:10.1038/nchembio.732

Authors: Christian Laggner, David Kokel, Vincent Setola, Alexandra Tolia, Henry Lin, John J Irwin, Michael J Keiser, Chung Yan J Cheung, Daniel L Minor, Bryan L Roth, Randall T Peterson & Brian K Shoichet

Target identification is a core challenge in chemical genetics. Here we use chemical similarity to computationally predict the targets of 586 compounds that were active in a zebrafish behavioral assay. Among 20 predictions tested, 11 compounds had activities ranging from 1 nM to 10,000 nM on the predicted targets. The roles of two of these targets were tested in the original zebrafish phenotype. Prediction of targets from chemotype is rapid and may be generally applicable.

Categories: Journals

Knot formation in newly translated proteins is spontaneous and accelerated by chaperonins

Sun, 12/18/2011 - 00:00

Knot formation in newly translated proteins is spontaneous and accelerated by chaperonins

Nature Chemical Biology 8, 147 (2012). doi:10.1038/nchembio.742

Authors: Anna L Mallam & Sophie E Jackson

Categories: Journals

Protein-protein interactions: In the TANK

Enzyme engineering: Just a jump to the left

Methods: Zebrafish click

Allostery: A systematic search

Metabolism: Closing the loop

Translation: Ribosome 3.0

Molecular switches: The pore of the matter

Chemical genetics: Bumping into AMPK substrates

Ion channels: Cooperativity in twin gatings

Glycobiology: Enzyme deficiencies deciphered

Signaling: An oxysterol ligand for Smoothened

Disease-specific non–reducing end carbohydrate biomarkers for mucopolysaccharidoses

Timing facilitated site transfer of an enzyme on DNA

Oxysterols are allosteric activators of the oncoprotein Smoothened

Skepinone-L is a selective p38 mitogen-activated protein kinase inhibitor

Primary amines protect against retinal degeneration in mouse models of retinopathies

Natural product–inspired cascade synthesis yields modulators of centrosome integrity

Small-molecule proteostasis regulators for protein conformational diseases

Chemical informatics and target identification in a zebrafish phenotypic screen

Knot formation in newly translated proteins is spontaneous and accelerated by chaperonins

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