Small molecule signaling in Caenorhabditis elegans.


:Whereas the C. elegans genome was sequenced many years ago, the role of small molecule signals in its biology is still poorly understood. A recent publication reports the identification of two steroidal signaling molecules that regulate C. elegans reproductive development and dauer diapause via the nuclear receptor DAF-12. The two compounds, named dafachronic acids, represent the first endogenous ligands identified for any of the 284 nuclear receptors in C. elegans.


ACS Chem Biol


ACS chemical biology


Schroeder FC




Has Abstract


2006-05-23 00:00:00












  • Impaired transport of nucleotides in a mitochondrial carrier explains severe human genetic diseases.

    abstract::The mitochondrial ADP/ATP carrier (AAC) is a prominent actor in the energetic regulation of the cell, importing ADP into the mitochondria and exporting ATP toward the cytoplasm. Severe genetic diseases have been ascribed to specific mutations in this membrane protein. How minute, well-localized modifications of the tr...

    journal_title:ACS chemical biology

    pub_type: 杂志文章


    authors: Ravaud S,Bidon-Chanal A,Blesneac I,Machillot P,Juillan-Binard C,Dehez F,Chipot C,Pebay-Peyroula E

    更新日期:2012-07-20 00:00:00

  • A chemical biological strategy to facilitate diabetic wound healing.

    abstract::A complication of diabetes is the inability of wounds to heal in diabetic patients. Diabetic wounds are refractory to healing due to the involvement of activated matrix metalloproteinases (MMPs), which remodel the tissue resulting in apoptosis. There are no readily available methods that identify active unregulated MM...

    journal_title:ACS chemical biology

    pub_type: 杂志文章


    authors: Gooyit M,Peng Z,Wolter WR,Pi H,Ding D,Hesek D,Lee M,Boggess B,Champion MM,Suckow MA,Mobashery S,Chang M

    更新日期:2014-01-17 00:00:00

  • Revisiting the role of glycosylation in the structure of human IgG Fc.

    abstract::Binding of the Fc domain of Immunoglobulin G (IgG) to Fcγ receptors on leukocytes can initiate a series of signaling events resulting in antibody-dependent cell-mediated cytotoxicity (ADCC) and other important immune responses. Fc domains lacking glycosylation at N297 have greatly diminished Fcγ receptor binding and l...

    journal_title:ACS chemical biology

    pub_type: 杂志文章


    authors: Borrok MJ,Jung ST,Kang TH,Monzingo AF,Georgiou G

    更新日期:2012-09-21 00:00:00

  • Enzymatic Plasticity Inspired by the Diterpene Cyclase CotB2.

    abstract::Enzymatic plasticity, as a modern term referring to the functional conversion of an enzyme, is significant for enzymatic activity redesign. The bacterial diterpene cyclase CotB2 is a typical plastic enzyme by which its native form precisely conducts a chemical reaction while its mutants diversify the catalytic functio...

    journal_title:ACS chemical biology

    pub_type: 杂志文章


    authors: Tang X,Zhang F,Zeng T,Li W,Yin S,Wu R

    更新日期:2020-10-16 00:00:00

  • A Hydrogel-Microsphere Drug Delivery System That Supports Once-Monthly Administration of a GLP-1 Receptor Agonist.

    abstract::We have developed a chemically controlled very long-acting delivery system to support once-monthly administration of a peptidic GLP-1R agonist. Initially, the prototypical GLP-1R agonist exenatide was covalently attached to hydrogel microspheres by a self-cleaving β-eliminative linker; after subcutaneous injection in ...

    journal_title:ACS chemical biology

    pub_type: 杂志文章


    authors: Schneider EL,Hearn BR,Pfaff SJ,Reid R,Parkes DG,Vrang N,Ashley GW,Santi DV

    更新日期:2017-08-18 00:00:00

  • Biochemical and biophysical analysis of a chiral PqsD inhibitor revealing tight-binding behavior and enantiomers with contrary thermodynamic signatures.

    abstract::Antivirulence strategies addressing bacterial pathogenicity without exhibiting growth inhibition effects represent a novel approach to overcome today's crisis in antibiotic development. In recent studies, we examined various inhibitors of PqsD, an enzyme involved in formation of Pseudomonas aeruginosa cell-to-cell sig...

    journal_title:ACS chemical biology

    pub_type: 杂志文章


    authors: Storz MP,Brengel C,Weidel E,Hoffmann M,Hollemeyer K,Steinbach A,Müller R,Empting M,Hartmann RW

    更新日期:2013-12-20 00:00:00

  • Cholesterol, it's not just for heart disease anymore.

    abstract::Recent studies have shown that cholesterol plays a significant role in the ability of Toxin A from Clostridium difficile to enter eukaryotic cells. The translocation process is one of three major steps during intoxication that could be targeted for intervention against the severe antibiotic-associated diarrhea caused ...

    journal_title:ACS chemical biology

    pub_type: 杂志文章


    authors: Kerzmann A,Feig AL

    更新日期:2006-04-25 00:00:00

  • mRNA display selection of a high-affinity, modification-specific phospho-IkappaBalpha-binding fibronectin.

    abstract::The complexity of the human proteome is greatly expanded by post-translational modifications. New tools capable of recognizing these modifications in a sequence-specific fashion provide a route to purify these modified proteins, to alter protein trafficking, and to visualize signal transduction in real time. Here, we ...

    journal_title:ACS chemical biology

    pub_type: 杂志文章


    authors: Olson CA,Liao HI,Sun R,Roberts RW

    更新日期:2008-08-15 00:00:00

  • Enzymatic synthesis of polybrominated dioxins from the marine environment.

    abstract::Polyhalogenated dibenzo-p-dioxins are arguably among the most toxic molecules known to man. In addition to anthropogenic sources, marine invertebrates also harbor polybrominated dibenzo-p-dioxins of as yet unknown biogenic origin. Here, we report that the bmp gene locus in marine bacteria, a recently characterized sou...

    journal_title:ACS chemical biology

    pub_type: 信件


    authors: Agarwal V,Moore BS

    更新日期:2014-09-19 00:00:00

  • Validating Signal Transducer and Activator of Transcription (STAT) Protein-Inhibitor Interactions Using Biochemical and Cellular Thermal Shift Assays.

    abstract::Signal transducer and activator of transcription (STAT) proteins have important biological functions; however, deregulation of STAT signaling is a driving force behind the onset and progression of inflammatory diseases and cancer. While their biological roles suggest that STAT proteins would be valuable targets for de...

    journal_title:ACS chemical biology

    pub_type: 杂志文章


    authors: Attarha S,Reithmeier A,Busker S,Desroses M,Page BDG

    更新日期:2020-07-17 00:00:00

  • Use of calculated cation-pi binding energies to predict relative strengths of nicotinic acetylcholine receptor agonists.

    abstract::Agonists and antagonists of the nicotinic acetylcholine receptor (nAChR) are used to treat nicotine addiction, neuromuscular disorders, and neurological diseases. In designing small molecule therapeutics with the nAChR as a target, it is useful to identify chemical parameters that correlate with ability to activate th...

    journal_title:ACS chemical biology

    pub_type: 杂志文章


    authors: Tantama M,Licht S

    更新日期:2008-11-21 00:00:00

  • Precursor-Guided Mining of Marine Sponge Metabolomes Lends Insight into Biosynthesis of Pyrrole-Imidazole Alkaloids.

    abstract::Pyrrole-imidazole alkaloids are natural products isolated from marine sponges, holobiont metazoans that are associated with symbiotic microbiomes. Pyrrole-imidazole alkaloids have attracted attention due to their chemical complexity and their favorable pharmacological properties. However, insights into how these molec...

    journal_title:ACS chemical biology

    pub_type: 杂志文章


    authors: Mohanty I,Moore SG,Yi D,Biggs JS,Gaul DA,Garg N,Agarwal V

    更新日期:2020-08-21 00:00:00

  • Progressive Stereo Locking (PSL): A Residual Dipolar Coupling Based Force Field Method for Determining the Relative Configuration of Natural Products and Other Small Molecules.

    abstract::Establishing the relative configuration of a bioactive natural product represents the most challenging part in determining its structure. Residual dipolar couplings (RDCs) are sensitive probes of the relative spatial orientation of internuclear vectors. We adapted a force field structure calculation methodology to all...

    journal_title:ACS chemical biology

    pub_type: 杂志文章


    authors: Cornilescu G,Ramos Alvarenga RF,Wyche TP,Bugni TS,Gil RR,Cornilescu CC,Westler WM,Markley JL,Schwieters CD

    更新日期:2017-08-18 00:00:00

  • Cruentaren A binds F1F0 ATP synthase to modulate the Hsp90 protein folding machinery.

    abstract::The molecular chaperone Hsp90 requires the assistance of immunophilins, co-chaperones, and partner proteins for the conformational maturation of client proteins. Hsp90 inhibition represents a promising anticancer strategy due to the dependence of numerous oncogenic signaling pathways upon Hsp90 function. Historically,...

    journal_title:ACS chemical biology

    pub_type: 杂志文章


    authors: Hall JA,Kusuma BR,Brandt GE,Blagg BS

    更新日期:2014-04-18 00:00:00

  • Mechanistic Insights into Taxadiene Epoxidation by Taxadiene-5α-Hydroxylase.

    abstract::The anticancer molecule taxol (Paclitaxel) stands as one of the most medically and economically important natural products. However, despite decades of extensive study, its biosynthesis remains poorly understood. Unpredictable behavior of the first oxygenation enzyme, taxadiene-5α-hydroxylase, which produces a range o...

    journal_title:ACS chemical biology

    pub_type: 杂志文章


    authors: Edgar S,Zhou K,Qiao K,King JR,Simpson JH,Stephanopoulos G

    更新日期:2016-02-19 00:00:00

  • Identification of a Novel Mycobacterial Arabinosyltransferase Activity Which Adds an Arabinosyl Residue to α-d-Mannosyl Residues.

    abstract::The arabinosyltransferases responsible for the biosynthesis of the arabinan domains of two abundant heteropolysaccharides of the cell envelope of all mycobacterial species, lipoarabinomannan and arabinogalactan, are validated drug targets. Using a cell envelope preparation from Mycobacterium smegmatis as the enzyme so...

    journal_title:ACS chemical biology

    pub_type: 杂志文章


    authors: Angala SK,McNeil MR,Zou L,Liav A,Zhang J,Lowary TL,Jackson M

    更新日期:2016-06-17 00:00:00

  • Competitive binding of a benzimidazole to the histone-binding pocket of the Pygo PHD finger.

    abstract::The Pygo-BCL9 complex is a chromatin reader, facilitating β-catenin-mediated oncogenesis, and is thus emerging as a potential therapeutic target for cancer. Its function relies on two ligand-binding surfaces of Pygo's PHD finger that anchor the histone H3 tail methylated at lysine 4 (H3K4me) with assistance from the B...

    journal_title:ACS chemical biology

    pub_type: 杂志文章


    authors: Miller TC,Rutherford TJ,Birchall K,Chugh J,Fiedler M,Bienz M

    更新日期:2014-12-19 00:00:00

  • Structural Analysis of the Tobramycin and Gentamicin Clinical Resistome Reveals Limitations for Next-generation Aminoglycoside Design.

    abstract::Widespread use and misuse of antibiotics has allowed for the selection of resistant bacteria capable of avoiding the effects of antibiotics. The primary mechanism for resistance to aminoglycosides, a broad-spectrum class of antibiotics, is through covalent enzymatic modification of the drug, waning their bactericidal ...

    journal_title:ACS chemical biology

    pub_type: 杂志文章


    authors: Bassenden AV,Rodionov D,Shi K,Berghuis AM

    更新日期:2016-05-20 00:00:00

  • Cytochrome c Reduction by H2S Potentiates Sulfide Signaling.

    abstract::Hydrogen sulfide (H2S) is an endogenously produced gas that is toxic at high concentrations. It is eliminated by a dedicated mitochondrial sulfide oxidation pathway, which connects to the electron transfer chain at the level of complex III. Direct reduction of cytochrome c (Cyt C) by H2S has been reported previously b...

    journal_title:ACS chemical biology

    pub_type: 杂志文章


    authors: Vitvitsky V,Miljkovic JL,Bostelaar T,Adhikari B,Yadav PK,Steiger AK,Torregrossa R,Pluth MD,Whiteman M,Banerjee R,Filipovic MR

    更新日期:2018-08-17 00:00:00

  • Fragment Assembly Approach Based on Graph/Network Theory with Quantum Chemistry Verifications for Assigning Multidimensional NMR Signals in Metabolite Mixtures.

    abstract::The abundant observation of chemical fragment information for molecular complexities is a major advantage of biological NMR analysis. Thus, the development of a novel technique for NMR signal assignment and metabolite identification may offer new possibilities for exploring molecular complexities. We propose a new sig...

    journal_title:ACS chemical biology

    pub_type: 杂志文章


    authors: Ito K,Tsutsumi Y,Date Y,Kikuchi J

    更新日期:2016-04-15 00:00:00

  • Development of a highly selective c-Src kinase inhibitor.

    abstract::Generating highly selective probes to interrogate protein kinase function in biological studies remains a challenge, and new strategies are required. Herein, we describe the development of the first highly selective and cell-permeable inhibitor of c-Src, a key signaling kinase in cancer. Our strategy involves extensio...

    journal_title:ACS chemical biology

    pub_type: 杂志文章


    authors: Brandvold KR,Steffey ME,Fox CC,Soellner MB

    更新日期:2012-08-17 00:00:00

  • An unbiased approach to identify endogenous substrates of "histone" deacetylase 8.

    abstract::Despite being extensively characterized structurally and biochemically, the functional role of histone deacetylase 8 (HDAC8) has remained largely obscure due in part to a lack of known cellular substrates. Herein, we describe an unbiased approach using chemical tools in conjunction with sophisticated proteomics method...

    journal_title:ACS chemical biology

    pub_type: 信件


    authors: Olson DE,Udeshi ND,Wolfson NA,Pitcairn CA,Sullivan ED,Jaffe JD,Svinkina T,Natoli T,Lu X,Paulk J,McCarren P,Wagner FF,Barker D,Howe E,Lazzaro F,Gale JP,Zhang YL,Subramanian A,Fierke CA,Carr SA,Holson EB

    更新日期:2014-10-17 00:00:00

  • Discovery of a nitric oxide responsive quorum sensing circuit in Vibrio harveyi.

    abstract::Bacteria use small molecules to assess the density and identity of nearby organisms and formulate a response. This process, called quorum sensing (QS), commonly regulates bioluminescence, biofilm formation, and virulence. Vibrio harveyi have three described QS circuits. Each involves the synthesis of a molecule that r...

    journal_title:ACS chemical biology

    pub_type: 杂志文章


    authors: Henares BM,Higgins KE,Boon EM

    更新日期:2012-08-17 00:00:00

  • Functional and Structural Insights into a Novel Promiscuous Ketoreductase of the Lugdunomycin Biosynthetic Pathway.

    abstract::Angucyclines are a structurally diverse class of actinobacterial natural products defined by their varied polycyclic ring systems, which display a wide range of biological activities. We recently discovered lugdunomycin (1), a highly rearranged polyketide antibiotic derived from the angucycline backbone that is synthe...

    journal_title:ACS chemical biology

    pub_type: 杂志文章


    authors: Xiao X,Elsayed SS,Wu C,van der Heul HU,Metsä-Ketelä M,Du C,Prota AE,Chen CC,Liu W,Guo RT,Abrahams JP,van Wezel GP

    更新日期:2020-09-18 00:00:00

  • Parsimonious discovery of synergistic drug combinations.

    abstract::Combination therapies that enhance efficacy or permit reduced dosages to be administered have seen great success in a variety of therapeutic applications. More fundamentally, the discovery of epistatic pathway interactions not only informs pharmacologic intervention but can be used to better understand the underlying ...

    journal_title:ACS chemical biology

    pub_type: 杂志文章


    authors: Severyn B,Liehr RA,Wolicki A,Nguyen KH,Hudak EM,Ferrer M,Caldwell JS,Hermes JD,Li J,Tudor M

    更新日期:2011-12-16 00:00:00

  • Seeing is believing.

    abstract::Modern visualization techniques are affording a peek into complex cellular processes. A recent paper describes an automated fluorescence microscopy method to map the subcellular localization of up to 100 different proteins in the same sample. ...

    journal_title:ACS chemical biology

    pub_type: 杂志文章


    authors: Jacquier V,Michnick SW

    更新日期:2006-12-15 00:00:00

  • Features of modularly assembled compounds that impart bioactivity against an RNA target.

    abstract::Transcriptomes provide a myriad of potential RNAs that could be the targets of therapeutics or chemical genetic probes of function. Cell-permeable small molecules, however, generally do not exploit these targets, owing to the difficulty in the design of high affinity, specific small molecules targeting RNA. As part of...

    journal_title:ACS chemical biology

    pub_type: 杂志文章


    authors: Rzuczek SG,Gao Y,Tang ZZ,Thornton CA,Kodadek T,Disney MD

    更新日期:2013-10-18 00:00:00

  • Targeting Regorafenib-Induced Toxicity through Inhibition of Gut Microbial β-Glucuronidases.

    abstract::Regorafenib (Stivarga) is an oral small molecule kinase inhibitor used to treat metastatic colorectal cancer, hepatocellular carcinomas, and gastrointestinal stromal tumors. Diarrhea is one of the most frequently observed adverse reactions associated with regorafenib. This toxicity may arise from the reactivation of t...

    journal_title:ACS chemical biology

    pub_type: 杂志文章


    authors: Ervin SM,Hanley RP,Lim L,Walton WG,Pearce KH,Bhatt AP,James LI,Redinbo MR

    更新日期:2019-12-20 00:00:00

  • ANS binding reveals common features of cytotoxic amyloid species.

    abstract::Oligomeric assemblies formed from a variety of disease-associated peptides and proteins have been strongly associated with toxicity in many neurodegenerative conditions, such as Alzheimer's disease. The precise nature of the toxic agents, however, remains still to be established. We show that prefibrillar aggregates o...

    journal_title:ACS chemical biology

    pub_type: 信件


    authors: Bolognesi B,Kumita JR,Barros TP,Esbjorner EK,Luheshi LM,Crowther DC,Wilson MR,Dobson CM,Favrin G,Yerbury JJ

    更新日期:2010-08-20 00:00:00

  • Surprising Non-Additivity of Methyl Groups in Drug-Kinase Interaction.

    abstract::Drug optimization is guided by biophysical methods with increasing popularity. In the context of lead structure modifications, the introduction of methyl groups is a simple but potentially powerful approach. Hence, it is crucial to systematically investigate the influence of ligand methylation on biophysical character...

    journal_title:ACS chemical biology

    pub_type: 杂志文章


    authors: Wienen-Schmidt B,Schmidt D,Gerber HD,Heine A,Gohlke H,Klebe G

    更新日期:2019-12-20 00:00:00