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Journal Cover Cell Chemical Biology
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   Hybrid Journal Hybrid journal (It can contain Open Access articles)
   ISSN (Online) 2451-9456
   Published by Elsevier Homepage  [3177 journals]
  • A Master Switch in Thiopeptide Biosynthesis
    • Authors: Claudia Roessler; Hans-Dieter Arndt
      Pages: 121 - 123
      Abstract: Although considerable knowledge of the biosynthetic machinery of thiopeptide antibiotics has been accumulated, the regulation of their production remains unclear. In this issue of Cell Chemical Biology, Li et al. (2018) have now characterized a key transcription factor and suggest its feedback regulation by biosynthesis intermediates and the final product.
      Citation: Cell Chemical Biology 25, 2 (2018)
      PubDate: 2018-02-15
      DOI: 10.1016/j.chembiol.2018.01.017
      Issue No: Vol. 25, No. 2 (2018)
  • Insights into an Ancient Atypical Kinase Essential for Biosynthesis of
           Coenzyme Q
    • Authors: Catherine F. Clarke
      Pages: 123 - 125
      Abstract: COQ8 proteins are homologs of atypical protein kinases required for the biosynthesis of coenzyme Q (CoQ). In this issue of Cell Chemical Biology, Reidenbach et al. (2018) show that COQ8 has an ATPase activity, required for CoQ biosynthesis, that is strongly activated by cardiolipin and small molecule mimics of early CoQ intermediates.
      Citation: Cell Chemical Biology 25, 2 (2018)
      PubDate: 2018-02-15
      DOI: 10.1016/j.chembiol.2018.02.001
      Issue No: Vol. 25, No. 2 (2018)
  • Screening Drugs for Kidney Disease: Targeting the Podocyte
    • Authors: Joshua S. Bryer; Katalin Susztak
      Pages: 126 - 127
      Abstract: Podocytes cover the kidney glomerular basement membrane and present the final barrier in the renal filtration system. Podocyte loss, observed in most kidney diseases, correlates with kidney function decline. In this issue of Cell Chemical Biology, Seiber et al. (2018), using a high-throughput chemical screen, identified the compound CDG-0876, which improved podocyte survival.
      Citation: Cell Chemical Biology 25, 2 (2018)
      PubDate: 2018-02-15
      DOI: 10.1016/j.chembiol.2018.01.018
      Issue No: Vol. 25, No. 2 (2018)
  • Unmasking Fucosylation: from Cell Adhesion to Immune System Regulation and
    • Authors: Jun Li; Hui-Chen Hsu, John D. Mountz, John G. Allen
      Abstract: Fucose occurs very specifically in cell-surface glycan and may be thought of as a privileged sugar residue in glycobiology. Fucose is necessary for many critical cell adhesion and signaling events. Genetic modulation or modulation by fucose-specific reagents has revealed exciting new biology and opened new opportunities for the treatment of human diseases. In this review, Li et al. describe the tools used to discover new fucose biology, its impact on living systems, and initial clinical trial results.
      Citation: Cell Chemical Biology (2018)
      PubDate: 2018-03-08
      DOI: 10.1016/j.chembiol.2018.02.005
  • The Dolphin Proline-Rich Antimicrobial Peptide Tur1A Inhibits Protein
           Synthesis by Targeting the Bacterial Ribosome
    • Authors: Mario Mardirossian; Natacha Pérébaskine, Monica Benincasa, Stefano Gambato, Sven Hofmann, Paul Huter, Claudia Müller, Kai Hilpert, C. Axel Innis, Alessandro Tossi, Daniel N. Wilson
      Abstract: Proline-rich antimicrobial peptides (PrAMPs) are antibacterial components of the immune system of some animals. Mardirossian et al. identified two PrAMPs in the artiodactyl Tursiops truncatus (bottlenose dolphin), Tur1A and Tur1B. Tur1A was shown to inhibit bacterial protein synthesis by binding to the ribosome.
      Citation: Cell Chemical Biology (2018)
      PubDate: 2018-03-08
      DOI: 10.1016/j.chembiol.2018.02.004
  • A Split-Luciferase-Based Trimer Formation Assay as a High-throughput
           Screening Platform for Therapeutics in Alport Syndrome
    • Authors: Kohei Omachi; Misato Kamura, Keisuke Teramoto, Haruka Kojima, Tsubasa Yokota, Shota Kaseda, Jun Kuwazuru, Ryosuke Fukuda, Kosuke Koyama, Shingo Matsuyama, Keishi Motomura, Tsuyoshi Shuto, Mary Ann Suico, Hirofumi Kai
      Abstract: Omachi et al. showed that the type IV collagen α345(IV) trimer is a therapeutic target for the hereditary kidney disease, Alport syndrome. They established an HTS-applicable α345(IV) trimer assay and showed that chemical chaperones rescued trimer formation of mutant α5(IV).
      Citation: Cell Chemical Biology (2018)
      PubDate: 2018-03-08
      DOI: 10.1016/j.chembiol.2018.02.003
  • Snapshots of C-S Cleavage in Egt2 Reveals Substrate Specificity and
           Reaction Mechanism
    • Authors: Seema Irani; Nathchar Naowarojna, Yang Tang, Karan R. Kathuria, Shu Wang, Anxhela Dhembi, Norman Lee, Wupeng Yan, Huijue Lyu, Catherine E. Costello, Pinghua Liu, Yan Jessie Zhang
      Abstract: Irani et al. have determined the structure of Egt2, a C-S lyase at the final step in the ergothioneine biosynthesis pathways. Using X-ray crystallography and various biochemical studies, the reaction mechanism was delineated.
      Citation: Cell Chemical Biology (2018)
      PubDate: 2018-03-01
      DOI: 10.1016/j.chembiol.2018.02.002
  • Novel RNA-Affinity Proteogenomics Dissects Tumor Heterogeneity for
           Revealing Personalized Markers in Precision Prognosis of Cancer
    • Authors: Li Wang; John A. Wrobel, Ling Xie, DongXu Li, Giada Zurlo, Huali Shen, Pengyuan Yang, Zefeng Wang, Yibing Peng, Harsha P. Gunawardena, Qing Zhang, Xian Chen
      Abstract: The interpatient tumor-phenotypic heterogeneity hinders discovery of biomarkers for individualized prognosis. Wang and colleagues introduce an alternative splicing activity-based proteogenomic method that dissects tumor heterogeneity for de novo discovery of individualized prognostic biomarkers. The resulting biomarkers distinguish high-risk patient subpopulations from other patients within each single breast cancer subtype.
      Citation: Cell Chemical Biology (2018)
      PubDate: 2018-03-01
      DOI: 10.1016/j.chembiol.2018.01.016
  • Repurposing High-Throughput Image Assays Enables Biological Activity
           Prediction for Drug Discovery
    • Authors: Jaak Simm; Günter Klambauer, Adam Arany, Marvin Steijaert, Jörg Kurt Wegner, Emmanuel Gustin, Vladimir Chupakhin, Yolanda T. Chong, Jorge Vialard, Peter Buijnsters, Ingrid Velter, Alexander Vapirev, Shantanu Singh, Anne E. Carpenter, Roel Wuyts, Sepp Hochreiter, Yves Moreau, Hugo Ceulemans
      Abstract: Simm et al. demonstrate a computational method to predict the activities of compounds in hundreds of biological assays from a single image-based screen of half a million compounds. The resulting models boosted the identification and diversity of hit compounds for two projects, encouraging further research in this field.
      Citation: Cell Chemical Biology (2018)
      PubDate: 2018-03-01
      DOI: 10.1016/j.chembiol.2018.01.015
  • MUB40 Binds to Lactoferrin and Stands as a Specific Neutrophil Marker
    • Authors: Mark C. Anderson; Thibault Chaze, Yves-Marie Coïc, Louise Injarabian, Friederike Jonsson, Naelle Lombion, Dorothée Selimoglu-Buet, Judith Souphron, Caroline Ridley, Pascale Vonaesch, Bruno Baron, Ellen T. Arena, Jean-Yves Tinevez, Giulia Nigro, Katharina Nothelfer, Eric Solary, Valérie Lapierre, Thierry Lazure, Mariette Matondo, David Thornton, Philippe J. Sansonetti, Françoise Baleux, Benoit S. Marteyn
      Abstract: MUB40 is a universal and specific marker of mammalian neutrophils. MUB40 interacts with lactoferrin, stored in specific (β1), tertiary (β2), and secretome (γ) granules secreted upon stimulation. Neutrophil detection in inflamed or infected tissues is facilitated by MUB40 peptides conjugated to fluorophores. Neutrophilic inflammation detection may be envisaged by combining MUB40 with non-invasive imaging.
      Citation: Cell Chemical Biology (2018)
      PubDate: 2018-02-22
      DOI: 10.1016/j.chembiol.2018.01.014
  • SRPKIN-1: A Covalent SRPK1/2 Inhibitor that Potently Converts VEGF from
           Pro-angiogenic to Anti-angiogenic Isoform
    • Authors: John M. Hatcher; Guowei Wu, Chuyue Zeng, Jie Zhu, Fan Meng, Sherrina Patel, Wenqiu Wang, Scott B. Ficarro, Alan L. Leggett, Chelsea E. Powell, Jarrod A. Marto, Kang Zhang, Jacky Chi Ki Ngo, Xiang-Dong Fu, Tinghu Zhang, Nathanael S. Gray
      Abstract: Hatcher et al. report the first irreversible SRPK1/2 inhibitor SRPKIN-1, which inhibits phosphorylation of serine/arginine (SR)-rich splicing factors protein and induces a VEGF alternative splicing isoform switch, leading to anti-angiogenesis in a wet CNV mouse model.
      Citation: Cell Chemical Biology (2018)
      PubDate: 2018-02-22
      DOI: 10.1016/j.chembiol.2018.01.013
  • Identification of the Nicotinamide Salvage Pathway as a New Toxification
           Route for Antimetabolites
    • Authors: Daniela Buonvicino; Francesca Mazzola, Federica Zamporlini, Francesco Resta, Giuseppe Ranieri, Emidio Camaioni, Mirko Muzzi, Riccardo Zecchi, Giuseppe Pieraccini, Christian Dölle, Massimo Calamante, Gianluca Bartolucci, Mathias Ziegler, Barbara Stecca, Nadia Raffaelli, Alberto Chiarugi
      Abstract: Synthesis and consumption of the pyridine nucleotide NAD are increased in cancer cells and contribute to cell proliferation and neoplastic transformation. Buonvicino et al. identified Vacor as a new structure interfering with NAD metabolome which may lead to the development of new antineoplastic molecules.
      Citation: Cell Chemical Biology (2018)
      PubDate: 2018-02-22
      DOI: 10.1016/j.chembiol.2018.01.012
  • N-Acetyl Cysteine Functions as a Fast-Acting Antioxidant by Triggering
           Intracellular H2S and Sulfane Sulfur Production
    • Authors: Daria Ezeriņa; Yoko Takano, Kenjiro Hanaoka, Yasuteru Urano, Tobias P. Dick
      Abstract: N-Acetyl cysteine (NAC), by itself a poor scavenger of oxidants, is converted inside cells to yield sulfane sulfur species, which are very potent scavengers of oxidants. This conversion may account for many of the antioxidative effects provided by NAC which have hitherto remained unexplained.
      Citation: Cell Chemical Biology (2018)
      PubDate: 2018-02-08
      DOI: 10.1016/j.chembiol.2018.01.011
  • Engineered Glycocalyx Regulates Stem Cell Proliferation in Murine Crypt
    • Authors: Sara H. Rouhanifard; Aime Lopez Aguilar, Lu Meng, Kelley W. Moremen, Peng Wu
      Abstract: Rouhanifard et al. present a method for glycan engineering in a crypt organoid system and apply it to assess functions of N-acetyllactosamine (LacNAc) in stem cell biology. Results suggest that Paneth cells express high levels of LacNAc, and that blocking access to it leads to hyperproliferation of neighboring Lgr5+ stem cells.
      Citation: Cell Chemical Biology (2018)
      PubDate: 2018-02-08
      DOI: 10.1016/j.chembiol.2018.01.010
  • Structural Basis for Inhibitor-Induced Hydrogen Peroxide Production by
           Kynurenine 3-Monooxygenase
    • Authors: Hyun Tae Kim; Byeong Kwan Na, Jiwoung Chung, Sulhee Kim, Sool Ki Kwon, Hyunju Cha, Jonghyeon Son, Joong Myung Cho, Kwang Yeon Hwang
      Abstract: KMO inhibitors have been developed for the treatment of neurodegenerative disorders, but the mechanisms of flavin reduction and H2O2 production by KMO inhibitors are unknown. Kim et al. propose the triggering mechanism of flavin reduction and reveal the cause of H2O2 production by the inhibitors in KMO.
      Citation: Cell Chemical Biology (2018)
      PubDate: 2018-02-08
      DOI: 10.1016/j.chembiol.2018.01.008
  • Rox, a Rifamycin Resistance Enzyme with an Unprecedented Mechanism of
    • Authors: Kalinka Koteva; Georgina Cox, Jayne K. Kelso, Matthew D. Surette, Haley L. Zubyk, Linda Ejim, Peter Stogios, Alexei Savchenko, Dan Sørensen, Gerard D. Wright
      Abstract: The ROX family of monooxygenases mediates resistance to rifamycin antibiotics. Koteva, Cox, Kelso et al. report the structural and biochemical characterization of these enzymes, revealing that monooxygenation causes linearization of the antibiotic. This results in an altered conformation that inhibits the ability of the antibiotic to bind to its target, RNA polymerase.
      Citation: Cell Chemical Biology (2018)
      PubDate: 2018-02-01
      DOI: 10.1016/j.chembiol.2018.01.009
  • Switch of Mitochondrial Superoxide Dismutase into a Prooxidant Peroxidase
           in Manganese-Deficient Cells and Mice
    • Authors: Douglas Ganini; Janine H. Santos, Marcelo G. Bonini, Ronald P. Mason
      Abstract: Ganini et al. demonstrate that incorporation of iron over manganese by the mitochondrial superoxide dismutase (SOD2) generates a prooxidant peroxidase in mitochondria of human cells and mice. They show that FeSOD2 formation leads to mitochondrial dysfunction and oxidative stress.
      Citation: Cell Chemical Biology (2018)
      PubDate: 2018-02-01
      DOI: 10.1016/j.chembiol.2018.01.007
  • CD1b Tetramers Identify T Cells that Recognize Natural and Synthetic
           Diacylated Sulfoglycolipids from Mycobacterium tuberculosis
    • Authors: Charlotte A. James; Krystle K.Q. Yu, Martine Gilleron, Jacques Prandi, Vijayendar R. Yedulla, Zuzanna Z. Moleda, Eleonora Diamanti, Momin Khan, Varinder K. Aggarwal, Josephine F. Reijneveld, Peter Reinink, Stefanie Lenz, Ryan O. Emerson, Thomas J. Scriba, Michael N.T. Souter, Dale I. Godfrey, Daniel G. Pellicci, D. Branch Moody, Adriaan J. Minnaard, Chetan Seshadri, Ildiko Van Rhijn
      Abstract: Sulfoglycolipids (SGLs) are uniquely synthesized by Mycobacterium tuberculosis (Mtb) and recognized by human T cells. James, Yu et al. describe a new hybrid synthesis for key antigenic determinants of SGLs and the development of SGL-specific tetramers that can now be applied to large-scale translational studies.
      Citation: Cell Chemical Biology (2018)
      PubDate: 2018-02-01
      DOI: 10.1016/j.chembiol.2018.01.006
  • Directed Evolution to Engineer Monobody for FRET Biosensor Assembly and
           Imaging at Live-Cell Surface
    • Authors: Praopim Limsakul; Qin Peng, Yiqian Wu, Molly E. Allen, Jing Liang, Albert G. Remacle, Tyler Lopez, Xin Ge, Brian K. Kay, Huimin Zhao, Alex Y. Strongin, Xiang-Lei Yang, Shaoying Lu, Yingxiao Wang
      Abstract: Limsakul et al. demonstrate that directed evolution and sequence-function analysis are promising tools for engineering molecular binders and hybrid FRET biosensors, which reveal new distinct subcellular features of MT1-MMP molecular regulations at the extracellular surface of live cells.
      Citation: Cell Chemical Biology (2018)
      PubDate: 2018-01-30
      DOI: 10.1016/j.chembiol.2018.01.002
  • Novel Structural Mechanism of Allosteric Regulation of Aspartic Peptidases
           via an Evolutionarily Conserved Exosite
    • Authors: Iva Hánová; Jiří Brynda, Radka Houštecká, Nawsad Alam, Daniel Sojka, Petr Kopáček, Lucie Marešová, Jiří Vondrášek, Martin Horn, Ora Schueler-Furman, Michael Mareš
      Abstract: Aspartic peptidases (APs) are critically involved in numerous pathologies; however, little is known about their physiological regulation. Hánová et al. discovered the first selective endogenous inhibitor of APs in higher organisms. It is generated by autoproteolysis and acts through a unique structural mechanism.
      Citation: Cell Chemical Biology (2018)
      PubDate: 2018-01-30
      DOI: 10.1016/j.chembiol.2018.01.001
  • Dynarrestin, a Novel Inhibitor of Cytoplasmic Dynein
    • Authors: Susanne Höing; Ting-Yu Yeh, Matthias Baumann, Nancy E. Martinez, Peter Habenberger, Lea Kremer, Hannes C.A. Drexler, Philipp Küchler, Peter Reinhardt, Axel Choidas, Mia-Lisa Zischinsky, Gunther Zischinsky, Swaran Nandini, Aaron P. Ledray, Stephanie A. Ketcham, Lydia Reinhardt, Masin Abo-Rady, Michael Glatza, Stephen J. King, Peter Nussbaumer, Slava Ziegler, Bert Klebl, Trina A. Schroer, Hans R. Schöler, Herbert Waldmann, Jared Sterneckert
      Abstract: Höing, Yeh et al. identify dynarrestin, a novel inhibitor of the Hedgehog-signaling pathway. Dynarrestin specifically inhibits dynein in a reversible and novel manner.
      Citation: Cell Chemical Biology (2018)
      PubDate: 2018-01-30
      DOI: 10.1016/j.chembiol.2017.12.014
  • Inhibition of Dpp8/9 Activates the Nlrp1b Inflammasome
    • Authors: Marian C. Okondo; Sahana D. Rao, Cornelius Y. Taabazuing, Ashley J. Chui, Sarah E. Poplawski, Darren C. Johnson, Daniel A. Bachovchin
      Abstract: Dpp8/9 inhibitors induce an inflammatory form of cell death called pyroptosis in monocytes and macrophages. Here, Okondo et al. show that Dpp8/9 inhibition activates the inflammasome sensor protein Nlrp1b, which in turn activates pro-caspase-1 to mediate pyroptosis. This work reveals a previously unrecognized mechanism for stimulating the innate immune system.
      Citation: Cell Chemical Biology (2018)
      PubDate: 2018-01-30
      DOI: 10.1016/j.chembiol.2017.12.013
  • Structure, Function, and Biosynthetic Origin of Octapeptin Antibiotics
           Active against Extensively Drug-Resistant Gram-Negative Bacteria
    • Authors: Tony Velkov; Alejandra Gallardo-Godoy, James D. Swarbrick, Mark. A.T. Blaskovich, Alysha G. Elliott, Meiling Han, Philip E. Thompson, Kade D. Roberts, Johnny X. Huang, Bernd Becker, Mark S. Butler, Lawrence H. Lash, Sónia Troeira Henriques, Roger L. Nation, Sivashangarie Sivanesan, Marc-Antoine Sani, Frances Separovic, Haydyn Mertens, Dieter Bulach, Torsten Seemann, Jeremy Owen, Jian Li, Matthew A. Cooper
      Abstract: Octapeptins are colistin-like lipopeptide antibiotics with activity against multi- and extensively drug-resistant (MDR and XDR) Gram-negative bacteria. We describe the design, synthesis, and early preclinical evaluation of a novel series of octapeptins with superior activity and pharmacokinetics.
      Citation: Cell Chemical Biology (2018)
      PubDate: 2018-01-25
      DOI: 10.1016/j.chembiol.2018.01.005
  • Lipids Shape the Electron Acceptor-Binding Site of the Peripheral Membrane
           Protein Dihydroorotate Dehydrogenase
    • Authors: Joana Costeira-Paulo; Joseph Gault, Gergana Popova, Marcus J.G.W. Ladds, Ingeborg M.M. van Leeuwen, Médoune Sarr, Anders Olsson, David P. Lane, Sonia Laín, Erik G. Marklund, Michael Landreh
      Abstract: The combination of mass spectrometry and molecular dynamics simulations provides insights into the relationship between lipid and substrate binding to the peripheral membrane protein dehydroorotate dehydrogenase, revealing ligand-induced stabilization of the flexible membrane-binding region.
      Citation: Cell Chemical Biology (2018)
      PubDate: 2018-01-18
      DOI: 10.1016/j.chembiol.2017.12.012
  • Lipoprotein Signal Peptidase Inhibitors with Antibiotic Properties
           Identified through Design of a Robust In┬áVitro HT Platform
    • Authors: Seiya Kitamura; Anna Owensby, Daniel Wall, Dennis W. Wolan
      Abstract: Kitamura et al. developed an FRET-based assay to measure the proteolysis of peptide substrates by E. coli lipoprotein signal peptidase (Lsp). After identifying inhibitors with a high-throughput screen, the authors iteratively optimized lead candidates to generate compounds with IC50 values as low as 99 nM, which prevented bacterial growth.
      Citation: Cell Chemical Biology (2018)
      PubDate: 2018-01-11
      DOI: 10.1016/j.chembiol.2017.12.011
  • Metabolomics Reveals that Dietary Xenoestrogens Alter Cellular Metabolism
           Induced by Palbociclib/Letrozole Combination Cancer Therapy
    • Authors: Benedikt Warth; Philipp Raffeiner, Ana Granados, Tao Huan, Mingliang Fang, Erica M. Forsberg, H. Paul Benton, Laura Goetz, Caroline H. Johnson, Gary Siuzdak
      Abstract: Warth et al. used innovative global metabolomics and pathway prediction technology to describe the metabolic effects of the combined palbociclib/letrozole breast cancer therapy. Moreover, the role of dietary xenoestrogens on this treatment was examined by metabolite data, proliferation experiments, and functional assays.
      Citation: Cell Chemical Biology (2018)
      PubDate: 2018-01-11
      DOI: 10.1016/j.chembiol.2017.12.010
  • Robust Prediction of Resistance to Trimethoprim in Staphylococcus aureus
    • Authors: Philip W. Fowler; Kevin Cole, N. Claire Gordon, Angela M. Kearns, Martin J. Llewelyn, Tim E.A. Peto, Derrick W. Crook, A. Sarah Walker
      Abstract: Fowler et al. demonstrate how alchemical free energy calculations not only can classify whether mutations in Staphylococcus aureus dihydrofolate reductase confer resistance to trimethoprim, an antibiotic, or not, but also that the method is quantitatively accurate.
      Citation: Cell Chemical Biology (2018)
      PubDate: 2018-01-04
      DOI: 10.1016/j.chembiol.2017.12.009
  • ROS-Mediated 15-Hydroxyprostaglandin Dehydrogenase Degradation via
           Cysteine Oxidation Promotes NAD+-Mediated Epithelial-Mesenchymal
    • Authors: Weixuan Wang; Yadong Hu, Xiaofei Wang, Qingtao Wang, Haiteng Deng
      Abstract: Wang et al. showed that decreased NAD promoted EMT via ROS-mediated 15-PGDH degradation. Proteasome- and autophagy-mediated 15-PGDH degradation depends on oxidation of the Cys44 residue to sulfonic acid in 15-PGDH. Supplementation of NAD precursors upregulates 15-PGDH expression.
      Citation: Cell Chemical Biology (2018)
      PubDate: 2018-01-04
      DOI: 10.1016/j.chembiol.2017.12.008
  • Target Identification and Mechanism of Action of Picolinamide and
           Benzamide Chemotypes with Antifungal Properties
    • Authors: Verena Pries; Christina Nöcker, Danish Khan, Philipp Johnen, Zebin Hong, Ashutosh Tripathi, Anna-Lena Keller, Michael Fitz, Francesca Perruccio, Ireos Filipuzzi, Sasikala Thavam, Thomas Aust, Ralph Riedl, Slava Ziegler, Fulvia Bono, Gabriel Schaaf, Vytas A. Bankaitis, Herbert Waldmann, Dominic Hoepfner
      Abstract: Rising mortality rates and a limited armamentarium ask for novel, effective antifungal agents. Pries et al. have identified benzamide- and picolinamide-derived compounds that target the fungal lipid-transfer protein Sec14. Intersecting structure-activity relationship data, high-resolution genetics data and the first Sec14p crystal structure in complex with an inhibitor, pave the way for rational evaluation of this compound/target pair for its antifungal potential.
      Citation: Cell Chemical Biology (2018)
      PubDate: 2018-01-04
      DOI: 10.1016/j.chembiol.2017.12.007
  • The Elements of Translational Chemical Biology
    • Authors: Robert A. Copeland; P. Ann Boriack-Sjodin
      Pages: 128 - 134
      Abstract: A causal relationship between target activity modulation by small molecules and phenotypic consequence is the cornerstone of chemical biology and drug discovery. Here Copeland and Boriack-Sjodin articulate elements of translational chemical biology, as guideposts for the appropriate use of chemical probes in cellular studies.
      Citation: Cell Chemical Biology 25, 2 (2018)
      PubDate: 2017-12-07
      DOI: 10.1016/j.chembiol.2017.11.003
      Issue No: Vol. 25, No. 2 (2017)
  • Overcoming Resistance to the THZ Series of Covalent Transcriptional CDK
    • Authors: Yang Gao; Tinghu Zhang, Hideki Terai, Scott B. Ficarro, Nicholas Kwiatkowski, Ming-Feng Hao, Bandana Sharma, Camilla L. Christensen, Edmond Chipumuro, Kwok-kin Wong, Jarrod A. Marto, Peter S. Hammerman, Nathanael S. Gray, Rani E. George
      Pages: 135 - 142.e5
      Abstract: Gao et al. report ABC transporter upregulation as a major mechanism of acquired resistance to the THZ series of covalent CDK7/12/13 inhibitors and describe the generation of E9, which escapes drug efflux and whose target selectivity was confirmed by the acquisition of a CDK12-binding site mutation in E9-resistant cells.
      Citation: Cell Chemical Biology 25, 2 (2018)
      PubDate: 2017-12-21
      DOI: 10.1016/j.chembiol.2017.11.007
      Issue No: Vol. 25, No. 2 (2017)
  • NosP-Regulated Nosiheptide Production Responds to Both Peptidyl and
           Small-Molecule Ligands Derived from the Precursor Peptide
    • Authors: Jingjing Li; Yue Li, Guoqing Niu, Heng Guo, Yanping Qiu, Zhi Lin, Wen Liu, Huarong Tan
      Pages: 143 - 153.e4
      Abstract: Li. et al. describe a complex regulation of nosiheptide biosynthesis mediated by NosP via LP-containing precursor, intermediate, and end product. These findings expand our current knowledge regarding versatile roles of LP in RiPP production.
      Citation: Cell Chemical Biology 25, 2 (2018)
      PubDate: 2017-11-30
      Issue No: Vol. 25, No. 2 (2017)
  • Conserved Lipid and Small-Molecule Modulation of COQ8 Reveals Regulation
           of the Ancient Kinase-like UbiB Family
    • Authors: Andrew G. Reidenbach; Zachary A. Kemmerer, Deniz Aydin, Adam Jochem, Molly T. McDevitt, Paul D. Hutchins, Jaime L. Stark, Jonathan A. Stefely, Thiru Reddy, Alex S. Hebert, Emily M. Wilkerson, Isabel E. Johnson, Craig A. Bingman, John L. Markley, Joshua J. Coon, Matteo Dal Peraro, David J. Pagliarini
      Pages: 154 - 165.e11
      Abstract: Reidenbach et al. discover small-molecule and lipid ligands for the atypical kinase-like protein COQ8 that enhance its ATPase activity. They develop an analog-sensitive version of COQ8 that can be covalently inhibited, enabling acute inhibition of COQ8 ATPase activity in vitro and coenzyme Q biosynthesis in vivo.
      Citation: Cell Chemical Biology 25, 2 (2018)
      PubDate: 2017-11-30
      DOI: 10.1016/j.chembiol.2017.11.001
      Issue No: Vol. 25, No. 2 (2017)
  • Site-Specific Installation of Succinyl Lysine Analog into Histones Reveals
           the Effect of H2BK34 Succinylation on Nucleosome Dynamics
    • Authors: Yihang Jing; Zheng Liu, Gaofei Tian, Xiucong Bao, Toyotaka Ishibashi, Xiang David Li
      Pages: 166 - 174.e7
      Abstract: Jing and Liu et al. have developed a chemical approach to site-specifically introduce a succinyl lysine analog, Kcsucc, into histones. The further biochemical, biophysical and cell biology studies revealed that succinylation at histone H2B Lys34 (H2BK34succ) significantly influences nucleosome and chromatin dynamics.
      Citation: Cell Chemical Biology 25, 2 (2018)
      PubDate: 2017-12-14
      DOI: 10.1016/j.chembiol.2017.11.005
      Issue No: Vol. 25, No. 2 (2017)
  • GDC-0879, a BRAFV600E Inhibitor, Protects Kidney Podocytes from Death
    • Authors: Jonas Sieber; Nicolas Wieder, Abbe Clark, Manuel Reitberger, Sofia Matan, Jeannine Schoenfelder, Jianming Zhang, Anna Mandinova, Joshua Adam Bittker, Juan Gutierrez, Ozan Aygün, Namrata Udeshi, Steven Carr, Peter Mundel, Andreas Werner Jehle, Anna Greka
      Pages: 175 - 184.e4
      Abstract: Sieber et al. implement a high-throughput screening assay of podocyte viability and find that the BRAF inhibitor GDC-0879 protects podocytes by restoring MAPK signaling, offering a novel repurposing strategy for targeted kidney therapeutics.
      Citation: Cell Chemical Biology 25, 2 (2018)
      PubDate: 2017-12-14
      DOI: 10.1016/j.chembiol.2017.11.006
      Issue No: Vol. 25, No. 2 (2017)
  • Specific Inhibition of the Bifunctional Farnesyl/Geranylgeranyl
           Diphosphate Synthase in Malaria Parasites via a New Small-Molecule Binding
    • Authors: Jolyn E. Gisselberg; Zachary Herrera, Lindsey M. Orchard, Manuel Llinás, Ellen Yeh
      Pages: 185 - 193.e5
      Abstract: Gisselberg et al. identified a non-bisphosphonate inhibitor of the bifunctional FPPS/GGPPS in malaria parasites. Using this inhibitor they uncover a new, highly selective small-molecule binding site in this validated antimalarial drug target, overcoming previous limitations to developing malaria-specific FPPS/GGPPS inhibitors.
      Citation: Cell Chemical Biology 25, 2 (2018)
      PubDate: 2017-12-21
      DOI: 10.1016/j.chembiol.2017.11.010
      Issue No: Vol. 25, No. 2 (2017)
  • Objective, Quantitative, Data-Driven Assessment of Chemical Probes
    • Authors: Albert A. Antolin; Joseph E. Tym, Angeliki Komianou, Ian Collins, Paul Workman, Bissan Al-Lazikani
      Pages: 194 - 205.e5
      Abstract: Chemical probe selection remains largely subjective, not utilizing extensive medicinal chemistry data, causing widespread use of flawed probes. Antolin et al. describe the Probe Miner resource, empowering objective, quantitative, data-driven assessment of chemical probes based on regularly updated large-scale data.
      Citation: Cell Chemical Biology 25, 2 (2018)
      PubDate: 2017-12-14
      DOI: 10.1016/j.chembiol.2017.11.004
      Issue No: Vol. 25, No. 2 (2017)
  • Quantitative, Wide-Spectrum Kinase Profiling in Live Cells for Assessing
           the Effect of Cellular ATP on Target Engagement
    • Authors: James D. Vasta; Cesear R. Corona, Jennifer Wilkinson, Chad A. Zimprich, James R. Hartnett, Morgan R. Ingold, Kristopher Zimmerman, Thomas Machleidt, Thomas A. Kirkland, Kristin G. Huwiler, Rachel Friedman Ohana, Michael Slater, Paul Otto, Mei Cong, Carrow I. Wells, Benedict-Tilman Berger, Thomas Hanke, Carina Glas, Ke Ding, David H. Drewry, Kilian V.M. Huber, Timothy M. Willson, Stefan Knapp, Susanne Müller, Poncho L. Meisenheimer, Frank Fan, Keith V. Wood, Matthew B. Robers
      Pages: 206 - 214.e11
      Abstract: Vasta et al. describe a broad-spectrum approach (BRET) to quantitatively measure target engagement for kinases inside live cells. Compared with biochemical measurements, the analysis revealed an improved intracellular selectivity profile for clinically relevant kinase inhibitors. This serves as a mechanistic tool to determine the effect of cellular ATP on engagement potency.
      Citation: Cell Chemical Biology 25, 2 (2018)
      PubDate: 2017-11-22
      Issue No: Vol. 25, No. 2 (2017)
  • PhoDAGs Enable Optical Control of Diacylglycerol-Sensitive Transient
           Receptor Potential Channels
    • Authors: Trese Leinders-Zufall; Ursula Storch, Katherin Bleymehl, Michael Mederos y Schnitzler, James A. Frank, David B. Konrad, Dirk Trauner, Thomas Gudermann, Frank Zufall
      Pages: 215 - 223.e3
      Abstract: Diacylglycerol-sensitive TRP channels play important roles in health and disease, but their activation mechanisms are not well understood. Leinders-Zufall et al. develop an optical toolkit that enables monitoring of the effects of these channels with unprecedented speed and precision.
      Citation: Cell Chemical Biology 25, 2 (2018)
      PubDate: 2017-12-21
      DOI: 10.1016/j.chembiol.2017.11.008
      Issue No: Vol. 25, No. 2 (2017)
  • Drug Target Commons: A Community Effort to Build a Consensus Knowledge
           Base for Drug-Target Interactions
    • Authors: Jing Tang; Zia-ur-Rehman Tanoli, Balaguru Ravikumar, Zaid Alam, Anni Rebane, Markus Vähä-Koskela, Gopal Peddinti, Arjan J. van Adrichem, Janica Wakkinen, Alok Jaiswal, Ella Karjalainen, Prson Gautam, Liye He, Elina Parri, Suleiman Khan, Abhishekh Gupta, Mehreen Ali, Laxman Yetukuri, Anna-Lena Gustavsson, Brinton Seashore-Ludlow, Anne Hersey, Andrew R. Leach, John P. Overington, Gretchen Repasky, Krister Wennerberg, Tero Aittokallio
      Pages: 224 - 229.e2
      Abstract: Tang et al. launches a novel crowd-sourcing effort to standardize the collection, management, curation, and annotation of the notoriously heterogeneous compound-target bioactivity measurements. The web-based community platform aims to provide the most comprehensive, reproducible, and sustainable bioactivity knowledge base for the end users.
      Citation: Cell Chemical Biology 25, 2 (2018)
      PubDate: 2017-12-21
      DOI: 10.1016/j.chembiol.2017.11.009
      Issue No: Vol. 25, No. 2 (2017)
  • Acid-Tolerant Monomeric GFP from Olindias formosa
    • Authors: Hajime Shinoda; Yuanqing Ma, Ryosuke Nakashima, Keisuke Sakurai, Tomoki Matsuda, Takeharu Nagai
      Abstract: Shinoda et al. describe the cloning, engineering, and characterization of a monomeric GFP “Gamillus” from Olindias formosa. Gamillus has superior acid tolerance (pKa = 3.4) to reported other monomeric GFPs, and a unique trans chromophore configuration contributed to the acid tolerance. They demonstrate the usefulness for imaging in an acidic cellular environment, e.g., lysosomes.
      Citation: Cell Chemical Biology (2017)
      PubDate: 2017-12-28
      DOI: 10.1016/j.chembiol.2017.12.005
  • A Decade of Click Chemistry in Protein Palmitoylation: Impact on Discovery
           and New Biology
    • Authors: Xinxin Gao; Rami N. Hannoush
      Abstract: Gao and Hannoush provide a comprehensive summary of the biological advancements that were enabled by the use of clickable fatty acid probes. The authors also provide an outlook on future research explorations in the field of protein palmitoylation that could be enabled through the use of click-chemistry-based technologies.
      Citation: Cell Chemical Biology (2017)
      PubDate: 2017-12-28
      DOI: 10.1016/j.chembiol.2017.12.002
  • Identification of New Activators of Mitochondrial Fusion Reveals a Link
           between Mitochondrial Morphology and Pyrimidine Metabolism
    • Authors: Laia Miret-Casals; David Sebastián, José Brea, Eva M. Rico-Leo, Manuel Palacín, Pedro M. Fernández-Salguero, M. Isabel Loza, Fernando Albericio, Antonio Zorzano
      Abstract: Miret-Casals et al. identify leflunomide as an activator of MFN1/2 expression and demonstrate a connection between pyrimidine metabolism and mitochondrial fusion. This connection provides new avenues toward the treatment of diseases linked to mitochondrial dysfunction.
      Citation: Cell Chemical Biology (2017)
      PubDate: 2017-12-28
      DOI: 10.1016/j.chembiol.2017.12.001
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