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  1. Article ; Online: Targeting Mammalian Translational Inhibition with Tetracyclines.

    Boer, Robert E / Schneekloth, John S

    Cell chemical biology

    2018  Volume 25, Issue 12, Page(s) 1437–1438

    Abstract: In this issue of Cell Chemical Biology, Mortison et al. (2018) report an in-depth mechanistic study of targets of two different tetracyclines in mammalian cells. Unbiased chemoproteomics and RNA sequence mapping help identify specific ribosomal ... ...

    Abstract In this issue of Cell Chemical Biology, Mortison et al. (2018) report an in-depth mechanistic study of targets of two different tetracyclines in mammalian cells. Unbiased chemoproteomics and RNA sequence mapping help identify specific ribosomal substructures bound by tetracyclines, providing insight into the therapeutic potential for tetracyclines in many diseases.
    MeSH term(s) Animals ; Anti-Bacterial Agents ; Humans ; Ribosomes ; Tetracyclines
    Chemical Substances Anti-Bacterial Agents ; Tetracyclines
    Language English
    Publishing date 2018-12-21
    Publishing country United States
    Document type Journal Article ; Research Support, N.I.H., Extramural ; Research Support, N.I.H., Intramural ; Comment
    ISSN 2451-9448
    ISSN (online) 2451-9448
    DOI 10.1016/j.chembiol.2018.12.006
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article ; Online: Chemical Modulation of Pre-mRNA Splicing in Mammalian Systems.

    Boer, Robert E / Torrey, Zachary R / Schneekloth, John S

    ACS chemical biology

    2020  Volume 15, Issue 4, Page(s) 808–818

    Abstract: RNA splicing is a key component of gene expression and proteomic diversity in humans. The spliceosome assembles on and processes individual nascent pre-mRNA transcripts into distinct mature mRNAs that can code for different proteins. Splicing programs ... ...

    Abstract RNA splicing is a key component of gene expression and proteomic diversity in humans. The spliceosome assembles on and processes individual nascent pre-mRNA transcripts into distinct mature mRNAs that can code for different proteins. Splicing programs can be affected by somatic mutations and changes in response to exogenous stimuli. Importantly, alterations in splicing can be direct drivers of diseases including cancers. This Review describes recent advances and the potential for targeting and controlling pre-mRNA splicing in humans with small molecules, ranging from targeting spliceosomal proteins to direct targeting of individual RNA transcripts.
    MeSH term(s) G-Quadruplexes/drug effects ; Humans ; Protein Kinase Inhibitors/pharmacology ; RNA Precursors/drug effects ; RNA Precursors/metabolism ; RNA Splicing/drug effects ; Serine-Arginine Splicing Factors/metabolism ; Spliceosomes/drug effects
    Chemical Substances Protein Kinase Inhibitors ; RNA Precursors ; Serine-Arginine Splicing Factors (170974-22-8)
    Language English
    Publishing date 2020-04-07
    Publishing country United States
    Document type Journal Article ; Research Support, N.I.H., Intramural ; Review
    ISSN 1554-8937
    ISSN (online) 1554-8937
    DOI 10.1021/acschembio.0c00001
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  3. Article ; Online: The 5-lipoxygenase/cyclooxygenase-2 cross-over metabolite, hemiketal E

    Nakashima, Fumie / Giménez-Bastida, Juan A / Luis, Paula B / Presley, Sai H / Boer, Robert E / Chiusa, Manuel / Shibata, Takahiro / Sulikowski, Gary A / Pozzi, Ambra / Schneider, Claus

    The Journal of biological chemistry

    2023  Volume 299, Issue 4, Page(s) 103050

    Abstract: Consecutive oxygenation of arachidonic acid by 5-lipoxygenase and cyclooxygenase-2 yields the hemiketal eicosanoids, ... ...

    Abstract Consecutive oxygenation of arachidonic acid by 5-lipoxygenase and cyclooxygenase-2 yields the hemiketal eicosanoids, HKE
    MeSH term(s) Mice ; Humans ; Animals ; Cyclooxygenase 2/metabolism ; Arachidonic Acid ; Vascular Endothelial Growth Factor Receptor-2/metabolism ; Arachidonate 5-Lipoxygenase ; Vascular Endothelial Growth Factor A/metabolism ; Neovascularization, Physiologic ; Human Umbilical Vein Endothelial Cells/metabolism ; Angiogenesis Inhibitors/pharmacology ; Cell Movement ; Cell Proliferation
    Chemical Substances Cyclooxygenase 2 (EC 1.14.99.1) ; Arachidonic Acid (27YG812J1I) ; Vascular Endothelial Growth Factor Receptor-2 (EC 2.7.10.1) ; Arachidonate 5-Lipoxygenase (EC 1.13.11.34) ; Vascular Endothelial Growth Factor A ; Angiogenesis Inhibitors
    Language English
    Publishing date 2023-02-21
    Publishing country United States
    Document type Journal Article ; Research Support, N.I.H., Extramural
    ZDB-ID 2997-x
    ISSN 1083-351X ; 0021-9258
    ISSN (online) 1083-351X
    ISSN 0021-9258
    DOI 10.1016/j.jbc.2023.103050
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Uc I Zs.108: Show issues Location:
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    bis Jg. 2021: Bestellungen von Artikeln über das Online-Bestellformular
    ab Jg. 2022: Lesesaal (EG)

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  4. Article: Total Synthesis and Biological Activity of the Arachidonic Acid Metabolite Hemiketal E2

    Boer, Robert E / Giménez-Bastida, Juan Antonio / Boutaud, Olivier / Jana, Somnath / Schneider, Claus / Sulikowski, Gary A

    Organic letters. 2018 June 19, v. 20, no. 13

    2018  

    Abstract: The total synthesis of hemiketal E2 (HKE2) has been accomplished using a gold(I)-mediated cycloisomerization followed by oxidation of the enol ether product to introduce a unique keto-hemiketal, the core structure of HKE2. Synthetic hemiketal E2 ... ...

    Abstract The total synthesis of hemiketal E2 (HKE2) has been accomplished using a gold(I)-mediated cycloisomerization followed by oxidation of the enol ether product to introduce a unique keto-hemiketal, the core structure of HKE2. Synthetic hemiketal E2 reproduced biosynthetically derived HKE2 in the inhibition of human platelet aggregation.
    Keywords arachidonic acid ; bioactive properties ; chemical structure ; enol ethers ; gold ; metabolites ; oxidation ; platelet aggregation
    Language English
    Dates of publication 2018-0619
    Size p. 4020-4022.
    Publishing place American Chemical Society
    Document type Article
    ISSN 1523-7052
    DOI 10.1021/acs.orglett.8b01578
    Database NAL-Catalogue (AGRICOLA)

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  5. Article ; Online: Discovery of Inhibitors of MicroRNA-21 Processing Using Small Molecule Microarrays.

    Connelly, Colleen M / Boer, Robert E / Moon, Michelle H / Gareiss, Peter / Schneekloth, John S

    ACS chemical biology

    2016  Volume 12, Issue 2, Page(s) 435–443

    Abstract: The identification of small molecules that bind to and perturb the function of microRNAs is an attractive approach for the treatment for microRNA-associated pathologies. However, there are only a few small molecules known to interact directly with ... ...

    Abstract The identification of small molecules that bind to and perturb the function of microRNAs is an attractive approach for the treatment for microRNA-associated pathologies. However, there are only a few small molecules known to interact directly with microRNAs. Here, we report the use of a small molecule microarray (SMM) screening approach to identify low molecular weight compounds that directly bind to a pre-miR-21 hairpin. Compounds identified using this approach exhibit good affinity for the RNA (ranging from 0.8-2.0 μM) and are not composed of a polycationic scaffold. Several of the highest affinity compounds inhibit Dicer-mediated processing, while in-line probing experiments indicate that the compounds bind to the apical loop of the hairpin, proximal to the Dicer site. This work provides evidence that small molecules can be developed to bind directly to and inhibit miR-21.
    MeSH term(s) Humans ; MicroRNAs/antagonists & inhibitors ; Small Molecule Libraries ; Structure-Activity Relationship
    Chemical Substances MIRN21 microRNA, human ; MicroRNAs ; Small Molecule Libraries
    Language English
    Publishing date 2016-12-23
    Publishing country United States
    Document type Journal Article ; Validation Study
    ISSN 1554-8937
    ISSN (online) 1554-8937
    DOI 10.1021/acschembio.6b00945
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  6. Article ; Online: Total Synthesis and Biological Activity of the Arachidonic Acid Metabolite Hemiketal E

    Boer, Robert E / Giménez-Bastida, Juan Antonio / Boutaud, Olivier / Jana, Somnath / Schneider, Claus / Sulikowski, Gary A

    Organic letters

    2018  Volume 20, Issue 13, Page(s) 4020–4022

    Abstract: The total synthesis of hemiketal ... ...

    Abstract The total synthesis of hemiketal E
    MeSH term(s) Arachidonic Acid/chemistry ; Blood Platelets ; Humans ; Molecular Structure ; Oxidation-Reduction
    Chemical Substances Arachidonic Acid (27YG812J1I)
    Language English
    Publishing date 2018-06-19
    Publishing country United States
    Document type Journal Article ; Research Support, N.I.H., Extramural ; Research Support, Non-U.S. Gov't
    ISSN 1523-7052
    ISSN (online) 1523-7052
    DOI 10.1021/acs.orglett.8b01578
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  7. Article ; Online: Custom DNA Microarrays Reveal Diverse Binding Preferences of Proteins and Small Molecules to Thousands of G-Quadruplexes.

    Ray, Sreejana / Tillo, Desiree / Boer, Robert E / Assad, Nima / Barshai, Mira / Wu, Guanhui / Orenstein, Yaron / Yang, Danzhou / Schneekloth, John S / Vinson, Charles

    ACS chemical biology

    2020  Volume 15, Issue 4, Page(s) 925–935

    Abstract: Single-stranded DNA (ssDNA) containing four guanine repeats can form G-quadruplex (G4) structures. While cellular proteins and small molecules can bind G4s, it has been difficult to broadly assess their DNA-binding specificity. Here, we use custom DNA ... ...

    Abstract Single-stranded DNA (ssDNA) containing four guanine repeats can form G-quadruplex (G4) structures. While cellular proteins and small molecules can bind G4s, it has been difficult to broadly assess their DNA-binding specificity. Here, we use custom DNA microarrays to examine the binding specificities of proteins, small molecules, and antibodies across ∼15,000 potential G4 structures. Molecules used include fluorescently labeled pyridostatin (Cy5-PDS, a small molecule), BG4 (Cy5-BG4, a G4-specific antibody), and eight proteins (GST-tagged nucleolin, IGF2, CNBP, FANCJ, PIF1, BLM, DHX36, and WRN). Cy5-PDS and Cy5-BG4 selectively bind sequences known to form G4s, confirming their formation on the microarrays. Cy5-PDS binding decreased when G4 formation was inhibited using lithium or when ssDNA features on the microarray were made double-stranded. Similar conditions inhibited the binding of all other molecules except for CNBP and PIF1. We report that proteins have different G4-binding preferences suggesting unique cellular functions. Finally, competition experiments are used to assess the binding specificity of an unlabeled small molecule, revealing the structural features in the G4 required to achieve selectivity. These data demonstrate that the microarray platform can be used to assess the binding preferences of molecules to G4s on a broad scale, helping to understand the properties that govern molecular recognition.
    MeSH term(s) DNA, Single-Stranded/genetics ; DNA, Single-Stranded/metabolism ; DNA-Binding Proteins/metabolism ; G-Quadruplexes ; Humans ; Oligonucleotide Array Sequence Analysis ; Polymorphism, Single Nucleotide ; Protein Binding
    Chemical Substances DNA, Single-Stranded ; DNA-Binding Proteins
    Language English
    Publishing date 2020-04-07
    Publishing country United States
    Document type Journal Article ; Research Support, N.I.H., Intramural
    ISSN 1554-8937
    ISSN (online) 1554-8937
    DOI 10.1021/acschembio.9b00934
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  8. Article ; Online: Synthetic ligands for PreQ

    Connelly, Colleen M / Numata, Tomoyuki / Boer, Robert E / Moon, Michelle H / Sinniah, Ranu S / Barchi, Joseph J / Ferré-D'Amaré, Adrian R / Schneekloth, John S

    Nature communications

    2019  Volume 10, Issue 1, Page(s) 1501

    Abstract: Riboswitches are naturally occurring RNA aptamers that regulate gene expression by binding to specific small molecules. Riboswitches control the expression of essential bacterial genes and are important models for RNA-small molecule recognition. Here, we ...

    Abstract Riboswitches are naturally occurring RNA aptamers that regulate gene expression by binding to specific small molecules. Riboswitches control the expression of essential bacterial genes and are important models for RNA-small molecule recognition. Here, we report the discovery of a class of synthetic small molecules that bind to PreQ
    MeSH term(s) Aptamers, Nucleotide/chemistry ; Aptamers, Nucleotide/genetics ; Aptamers, Nucleotide/metabolism ; Crystallography, X-Ray ; Ligands ; Nucleic Acid Conformation ; Pyrimidinones/chemical synthesis ; Pyrimidinones/chemistry ; Pyrimidinones/metabolism ; Pyrroles/chemical synthesis ; Pyrroles/chemistry ; Pyrroles/metabolism ; RNA Folding ; Riboswitch
    Chemical Substances 7-(aminomethyl)-7-deazaguanine ; Aptamers, Nucleotide ; Ligands ; Pyrimidinones ; Pyrroles ; Riboswitch
    Language English
    Publishing date 2019-04-02
    Publishing country England
    Document type Journal Article ; Research Support, N.I.H., Extramural ; Research Support, N.I.H., Intramural ; Research Support, Non-U.S. Gov't
    ZDB-ID 2553671-0
    ISSN 2041-1723 ; 2041-1723
    ISSN (online) 2041-1723
    ISSN 2041-1723
    DOI 10.1038/s41467-019-09493-3
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  9. Article ; Online: HNRNPH1-dependent splicing of a fusion oncogene reveals a targetable RNA G-quadruplex interaction.

    Neckles, Carla / Boer, Robert E / Aboreden, Nicholas / Cross, Allison M / Walker, Robert L / Kim, Bong-Hyun / Kim, Suntae / Schneekloth, John S / Caplen, Natasha J

    RNA (New York, N.Y.)

    2019  Volume 25, Issue 12, Page(s) 1731–1750

    Abstract: The primary oncogenic event in ∼85% of Ewing sarcomas is a chromosomal translocation that generates a fusion oncogene encoding an aberrant transcription factor. The exact genomic breakpoints within the translocated genes, ...

    Abstract The primary oncogenic event in ∼85% of Ewing sarcomas is a chromosomal translocation that generates a fusion oncogene encoding an aberrant transcription factor. The exact genomic breakpoints within the translocated genes,
    MeSH term(s) G-Quadruplexes ; Heterogeneous-Nuclear Ribonucleoproteins/metabolism ; Oncogene Proteins, Fusion/genetics ; Oncogene Proteins, Fusion/metabolism ; Protein Binding ; RNA Splicing ; RNA, Messenger/chemistry ; RNA, Messenger/genetics ; RNA, Messenger/metabolism ; RNA-Binding Proteins
    Chemical Substances Heterogeneous-Nuclear Ribonucleoproteins ; Oncogene Proteins, Fusion ; RNA, Messenger ; RNA-Binding Proteins
    Language English
    Publishing date 2019-09-11
    Publishing country United States
    Document type Journal Article ; Research Support, N.I.H., Intramural
    ZDB-ID 1241540-6
    ISSN 1469-9001 ; 1355-8382
    ISSN (online) 1469-9001
    ISSN 1355-8382
    DOI 10.1261/rna.072454.119
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 4777: Show issues Location:
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    Jg. 1995 - 2021: Lesesall (2.OG)
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