ChemBioChem

Cover image for Vol. 14 Issue 10

July 8, 2013

Volume 14, Issue 10

Pages 1149–1270

  1. Cover Pictures

    1. Top of page
    2. Cover Pictures
    3. Graphical Abstract
    4. Corrigendum
    5. News
    6. Review
    7. Highlight
    8. Communications
    9. Full Papers
    1. You have free access to this content
      Cover Picture: The TEAD4–YAP/TAZ Protein–Protein Interaction: Expected Similarities and Unexpected Differences (ChemBioChem 10/2013) (page 1149)

      Jean Christophe Hau, Dr. Dirk Erdmann, Yannick Mesrouze, Dr. Pascal Furet, Patrizia Fontana, Catherine Zimmermann, Dr. Tobias Schmelzle, Dr. Francesco Hofmann and Dr. Patrick Chène

      Version of Record online: 1 JUL 2013 | DOI: 10.1002/cbic.201390033

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      The cover picture shows a schematic view of the interaction between the YAP and TAZ co-activators with a TEAD transcription factor. TEAD transcription factors are key elements of the Hippo pathway, which is deregulated in various types of cancers. YAP and TAZ share a high sequence homology and bind with similar affinity at the same site on the TEAD surface. However, this apparent similarity conceals differences in the ways in which both co-activators interact with TEAD. On p. 1218 ff., P. Chène et al. depict the similarities and differences of the TEAD4–YAP/TAZ protein–protein interaction.

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      Inside Cover: 1-Arylsulfonyl-5-(N-hydroxyacrylamide)indolines Histone Deacetylase Inhibitors Are Potent Cytokine Release Suppressors (ChemBioChem 10/2013) (page 1150)

      Dr. Hsueh-Yun Lee, Dr. Chia-Ron Yang, Dr. Mei-Jung Lai, Han-Li Huang, Yi-Ling Hsieh, Yi-Min Liu, Dr. Teng-Kuang Yeh, Yu-Hsuan Li, Samir Mehndiratta, Dr. Che-Ming Teng and Dr. Jing-Ping Liou

      Version of Record online: 1 JUL 2013 | DOI: 10.1002/cbic.201390034

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      The inside cover picture shows a SAR study of synthetic N-hydroxyacrylamides, described by J.-P. Liou et al. on p. 1248 ff., that identified 3-[1- (4-methoxybenzenesulfonyl)-2,3-dihydro-1H-indol-5-yl]-N-hydroxyacrylamide as a potent HDAC inhibitor. This compound not only suppresses the production of lipopolysaccharide-induced cytokines but also markedly reduces carrageenan-induced inflammation in rat.

  2. Graphical Abstract

    1. Top of page
    2. Cover Pictures
    3. Graphical Abstract
    4. Corrigendum
    5. News
    6. Review
    7. Highlight
    8. Communications
    9. Full Papers
  3. Corrigendum

    1. Top of page
    2. Cover Pictures
    3. Graphical Abstract
    4. Corrigendum
    5. News
    6. Review
    7. Highlight
    8. Communications
    9. Full Papers
    1. You have free access to this content
      Corrigendum: Exploring the Pharmacology and Action Spectra of Photochromic Open-Channel Blockers (page 1157)

      Timm Fehrentz, Christian A. Kuttruff, Florian M. E. Huber, Dr. Michael A. Kienzler, Dr. Peter Mayer and Prof. Dr. Dirk Trauner

      Version of Record online: 1 JUL 2013 | DOI: 10.1002/cbic.201300343

      This article corrects:

      Exploring the Pharmacology and Action Spectra of Photochromic Open-Channel Blockers

      Vol. 13, Issue 12, 1746–1749, Version of Record online: 13 JUL 2012

  4. News

    1. Top of page
    2. Cover Pictures
    3. Graphical Abstract
    4. Corrigendum
    5. News
    6. Review
    7. Highlight
    8. Communications
    9. Full Papers
  5. Review

    1. Top of page
    2. Cover Pictures
    3. Graphical Abstract
    4. Corrigendum
    5. News
    6. Review
    7. Highlight
    8. Communications
    9. Full Papers
    1. Chemical Tools for Studying the Biological Function of Glycolipids (pages 1164–1184)

      Dr. Bridget L. Stocker and Dr. Mattie S. M. Timmer

      Version of Record online: 18 JUN 2013 | DOI: 10.1002/cbic.201300064

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      Comprehensive toolkit: The vital roles played by glycolipids in many biological systems have led synthetic chemists to develop unique chemical tools that can be used to help to understand glycolipids' activities. We highlight approaches that have been made in the development of glycolipid probes, including both recent and historical examples of a variety of probe types.

  6. Highlight

    1. Top of page
    2. Cover Pictures
    3. Graphical Abstract
    4. Corrigendum
    5. News
    6. Review
    7. Highlight
    8. Communications
    9. Full Papers
    1. A Rotaxane Turing Machine for Peptides (pages 1185–1187)

      Claire Margaret Wilson, Dr. Andrea Gualandi and Prof. Pier Giorgio Cozzi

      Version of Record online: 3 JUN 2013 | DOI: 10.1002/cbic.201300248

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      A ringing belt: An artificial molecular machine was invented to build up a programmable peptidic sequence. By molecular movements, the rotaxane-based machine progressively introduces amino acids to form a short peptide chain. The journey towards an artificial ribosome is still quite long, but a conceivable future can be envisaged.

  7. Communications

    1. Top of page
    2. Cover Pictures
    3. Graphical Abstract
    4. Corrigendum
    5. News
    6. Review
    7. Highlight
    8. Communications
    9. Full Papers
    1. PR Toxin Biosynthesis in Penicillium roqueforti (pages 1189–1193)

      Dr. Nelson L. Brock and Dr. Jeroen S. Dickschat

      Version of Record online: 18 JUN 2013 | DOI: 10.1002/cbic.201300254

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      Complex bouquet: A recently developed method for trace analyses combining the advantages of GC-MS and 13C NMR spectroscopy was applied to investigate the volatiles of Penicillium roqueforti. Besides the main compound, aristolochene, several side products of aristolochene synthase and downstream oxidation products en route to PR toxin were identified, giving insight into the biosynthetic pathway.

    2. In Vivo Evidence for a Prodrug Activation Mechanism during Colibactin Maturation (pages 1194–1197)

      Dr. Xiaoying Bian, Dr. Jun Fu, Dr. Alberto Plaza, Dr. Jennifer Herrmann, Dr. Dominik Pistorius, Prof. Dr. A. Francis Stewart, Dr. Youming Zhang and Prof. Dr. Rolf Müller

      Version of Record online: 6 JUN 2013 | DOI: 10.1002/cbic.201300208

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      Releasing the cytopath: We have identified an N-myristoyl-D-asparagine (1) as the free N-terminal prodrug scaffold in cytopathogenic Escherichia coli strains expressing the colibactin gene cluster. Colibactin is released in vivo upon cleavage of precolibactin. We provide for the first time in vivo evidence of the prodrug-like release mechanism of colibactin.

    3. A Single PLP-Dependent Enzyme PctV Catalyzes the Transformation of 3-Dehydroshikimate into 3-Aminobenzoate in the Biosynthesis of Pactamycin (pages 1198–1203)

      Akane Hirayama, Prof. Dr. Tadashi Eguchi and Prof. Dr. Fumitaka Kudo

      Version of Record online: 6 JUN 2013 | DOI: 10.1002/cbic.201300153

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      Natural amino donation: A PLP-dependent aminotransferase PctV, encoded in the pactamycin biosynthetic gene cluster, was found to catalyze the formation of 3-aminobenzoate from 3-dehydroshikimate with L-glutamate as the amino donor. The PctV reaction comprises a transamination and two dehydration reactions. This is the first report of a simple 3-ABA synthase in nature.

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      Production of Propane and Other Short-Chain Alkanes by Structure-Based Engineering of Ligand Specificity in Aldehyde-Deformylating Oxygenase (pages 1204–1208)

      Dr. Basile Khara, Navya Menon, Dr. Colin Levy, Dr. David Mansell, Debasis Das, Prof. E. Neil G. Marsh, Prof. David Leys and Prof. Nigel S. Scrutton

      Version of Record online: 11 JUN 2013 | DOI: 10.1002/cbic.201300307

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      Biocatalytic propane production: structure-based engineering of aldehyde-deformylating oxygenase improves specificity for short- and medium-chain-length aldehydes and enhances the propane generation in whole-cell biotransformations. This presents new opportunities for developing biocatalytic modules for the production of volatile “drop-in” biofuels.

    5. Optimization of a Small Laccase by Active-Site Redesign (pages 1209–1211)

      Dr. Miguel D. Toscano, Dr. Leonardo De Maria, Dr. Sune Lobedanz and Dr. Lars H. Østergaard

      Version of Record online: 14 JUN 2013 | DOI: 10.1002/cbic.201300256

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      Small but faster: A small laccase from Streptomyces coelicolor (SLAC) has been engineered by structure-based design and site-directed mutagenesis to improve the activity on commercially relevant substrates. The variants generated showed up to 40-fold increased efficiency on 2,6-dimethoxyphenol and the ability to use mediators with considerably higher redox potentials (methylsyringate and TEMPO).

    6. Probing the Dimerization Interface of Leishmania infantum Trypanothione Reductase with Site-Directed Mutagenesis and Short Peptides (pages 1212–1217)

      Miguel A. Toro, Pedro A. Sánchez-Murcia, Dr. David Moreno, Marta Ruiz-Santaquiteria, Prof. Dr. Juan Fernando Alzate, Dr. Ana Negri, Prof. Dr. María-José Camarasa, Prof. Dr. Federico Gago, Dr. Sonsoles Velázquez and Prof. Dr. Antonio Jiménez-Ruiz

      Version of Record online: 6 JUN 2013 | DOI: 10.1002/cbic.201200744

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      Binding at the interface: We tested the inhibitory activity of a set of peptide sequences derived from an α-helix of the dimeric trypanothione reductase from Leishmania infantum. Replacement of a glutamic acid residue with a lysine promoted monomer dissociation and enzyme inhibition.

  8. Full Papers

    1. Top of page
    2. Cover Pictures
    3. Graphical Abstract
    4. Corrigendum
    5. News
    6. Review
    7. Highlight
    8. Communications
    9. Full Papers
    1. The TEAD4–YAP/TAZ Protein–Protein Interaction: Expected Similarities and Unexpected Differences (pages 1218–1225)

      Jean Christophe Hau, Dr. Dirk Erdmann, Yannick Mesrouze, Dr. Pascal Furet, Patrizia Fontana, Catherine Zimmermann, Dr. Tobias Schmelzle, Dr. Francesco Hofmann and Dr. Patrick Chène

      Version of Record online: 18 JUN 2013 | DOI: 10.1002/cbic.201300163

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      Hippo pathway functionality: YAP and TAZ are two homologous cofactors that bind with similar affinities to the same binding site on the surface of the TEAD transcription factor, and this might be important for Hippo pathway functionality. However, there are several molecular differences between the binding of YAP and TAZ to TEAD.

    2. Optimizing the Kinetics and Thermodynamics of DNA i-Motif Folding (pages 1226–1230)

      Dr. Anna Lena Lieblein, Dr. Boris Fürtig and Prof. Dr. Harald Schwalbe

      Version of Record online: 21 JUN 2013 | DOI: 10.1002/cbic.201300284

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      Strategic balance of power: Based on strategic loop design of i-motif-forming DNA sequences, it is possible to shift the conformational equilibrium between two competing structures and to change the kinetics and the folding pathway. These optimized sequences can serve as building blocks for applications such as nanomaterials and pH sensors.

    3. Development of Colorimetric HTS Assay of Cytochrome P450 for ortho-Specific Hydroxylation, and Engineering of CYP102D1 with Enhanced Catalytic Activity and Regioselectivity (pages 1231–1238)

      Dr. Kwon-Young Choi, Eun-Ok Jung, Prof. Dr. Hyungdon Yun, Prof. Dr. Yung-Hun Yang, Prof. Dr. Romas J. Kazlauskas and Prof. Dr. Byung-Gee Kim

      Version of Record online: 18 JUN 2013 | DOI: 10.1002/cbic.201300212

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      High-speed activity: A general HTS assay method for ortho-specific hydroxylation by P450 enzymes is presented. In order to screen for P450 variants with higher hydroxylation activities, an indirect HTS assay method to sense aldehyde molecules generated from O-dealkylation reaction of chemically permethylated substrate was developed.

    4. New Insights into the Pharmacological Chaperone Activity of C2-Substituted Glucoimidazoles for the Treatment of Gaucher Disease (pages 1239–1247)

      Zhonghua Li, Dr. Tiehai Li, Shaoxing Dai, Xiaoli Xie, Xiaofeng Ma, Dr. Wei Zhao, Weimin Zhang, Dr. Jing Li and Prof. Peng George Wang

      Version of Record online: 14 JUN 2013 | DOI: 10.1002/cbic.201300197

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      A new chaperone for Gaucher: We synthesized and evaluated series of C2-substituted GIZs as GCase chaperones for Gaucher disease therapy. Interestingly, compound 11 (shown in red), which has good membrane permeability, low-toxicity, and glycosidase selectivity, promoted the stabilization of mutant GCase and targeting of ER-retained mutant GCase to lysosomes.

    5. 1-Arylsulfonyl-5-(N-hydroxyacrylamide)indolines Histone Deacetylase Inhibitors Are Potent Cytokine Release Suppressors (pages 1248–1254)

      Dr. Hsueh-Yun Lee, Dr. Chia-Ron Yang, Dr. Mei-Jung Lai, Han-Li Huang, Yi-Ling Hsieh, Yi-Min Liu, Dr. Teng-Kuang Yeh, Yu-Hsuan Li, Samir Mehndiratta, Dr. Che-Ming Teng and Dr. Jing-Ping Liou

      Version of Record online: 20 JUN 2013 | DOI: 10.1002/cbic.201300201

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      HDAC inhibitors suppress cytokine in vitro and in vivo: A panel of HDAC inhibitors was developed and evaluated for anti-inflammatory activity, which has not been well studied previously. Compound 1 was more potent than SAHA in vitro and in vivo. Our results suggest that 1 is a novel agent for the treatment of inflammation-associated diseases.

    6. Dual Activators of Protein Kinase R (PKR) and Protein Kinase R-Like Kinase (PERK) Identify Common and Divergent Catalytic Targets (pages 1255–1262)

      Huijun Bai, Dr. Ting Chen, Dr. Jie Ming, Prof. Hong Sun, Peng Cao, Dr. Dahlene N. Fusco, Prof. Raymond T. Chung, Prof. Michael Chorev, Prof. Qi Jin and Prof. Bertal H. Aktas

      Version of Record online: 19 JUN 2013 | DOI: 10.1002/cbic.201300177

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      The jobs of the PERK? DHBDC, a dual activator of two eIF2α kinases, PKR and PERK, has been identified by chemical genetics approaches. DHBDC induces eIF2α phosphorylation and its downstream effectors by activating PKR and PERK, and activates the NF-κB pathway exclusively through PERK.

    7. Fluorescent THF-Based Fructose Analogue Exhibits Fructose-Dependent Uptake (pages 1263–1270)

      Dr. Marina Tanasova, Matthew Plutschack, Megan E. Muroski, Prof. Shana J. Sturla, Prof. Geoffrey F. Strouse and Prof. D. Tyler McQuade

      Version of Record online: 19 JUN 2013 | DOI: 10.1002/cbic.201300164

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      Differentiating cancer cells: To answer the controversial question, “What role does fructose play in human health?”, the mechanism of fructose transport must be understood. One path to this understanding is the creation of specific probes. This work describes the synthesis and use of a 2,5-anhydro-D-mannitol-based fluorescent probe to target the fructose-specific transporters.

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