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  1. Article ; Online: The Rise of Molecular Glues.

    Schreiber, Stuart L

    Cell

    2021  Volume 184, Issue 1, Page(s) 3–9

    Abstract: 2021 marks the 30th anniversary of the revelation that cyclosporin A and FK506 act in a way previously not seen-as "molecular glues" that induce neo-protein-protein associations. As a torrent of new molecular-glue probes and medicines are fueling ... ...

    Abstract 2021 marks the 30th anniversary of the revelation that cyclosporin A and FK506 act in a way previously not seen-as "molecular glues" that induce neo-protein-protein associations. As a torrent of new molecular-glue probes and medicines are fueling interest in this field, I explore the arc of this story.
    MeSH term(s) Biological Products/chemistry ; Biological Products/pharmacology ; Cyclosporine/pharmacology ; Immunosuppressive Agents/pharmacology ; Tacrolimus/chemistry ; Tacrolimus/pharmacology
    Chemical Substances Biological Products ; Immunosuppressive Agents ; Cyclosporine (83HN0GTJ6D) ; Tacrolimus (WM0HAQ4WNM)
    Language English
    Publishing date 2021-01-08
    Publishing country United States
    Document type Journal Article
    ZDB-ID 187009-9
    ISSN 1097-4172 ; 0092-8674
    ISSN (online) 1097-4172
    ISSN 0092-8674
    DOI 10.1016/j.cell.2020.12.020
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    In stock of ZB MED Cologne/Königswinter

    Zs.A 1167: Show issues Location:
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    Jg. 1995 - 2021: Lesesall (1.OG)
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    Zs.MG 58: Show issues

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  2. Article ; Online: 1980s Camelot.

    Schreiber, Stuart L

    The Journal of antibiotics

    2019  Volume 72, Issue 6, Page(s) 323

    MeSH term(s) Chemistry, Organic/history ; History, 20th Century ; Massachusetts ; Mentoring/history ; Research/history
    Language English
    Publishing date 2019-05-27
    Publishing country Japan
    Document type Biography ; Editorial ; Historical Article
    ZDB-ID 390800-8
    ISSN 1881-1469 ; 0021-8820 ; 0368-3532
    ISSN (online) 1881-1469
    ISSN 0021-8820 ; 0368-3532
    DOI 10.1038/s41429-019-0174-z
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    Zs.A 207: Show issues Location:
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  3. Article ; Online: Proposed Resolution of a Mechanistic Puzzle of Long Duration: Self-Condensation of Cyclopentanone to Form an 11-Carbon Dienoic Acid.

    Peszko, Matthew T / Schreiber, Stuart L / Myers, Andrew G

    The Journal of organic chemistry

    2023  Volume 88, Issue 11, Page(s) 7557–7559

    Abstract: The mechanism proposed for the transformation of cyclopentanone to the dienoic ... ...

    Abstract The mechanism proposed for the transformation of cyclopentanone to the dienoic acid
    Language English
    Publishing date 2023-05-02
    Publishing country United States
    Document type Journal Article
    ZDB-ID 123490-0
    ISSN 1520-6904 ; 0022-3263
    ISSN (online) 1520-6904
    ISSN 0022-3263
    DOI 10.1021/acs.joc.3c00492
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    Zs.A 4473: Show issues Location:
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  4. Article: A Chemical Biology View of Bioactive Small Molecules and a Binder-Based Approach to Connect Biology to Precision Medicines.

    Schreiber, Stuart L

    Israel journal of chemistry

    2018  Volume 59, Issue 1-2, Page(s) 52–59

    Language English
    Publishing date 2018-10-30
    Publishing country Germany
    Document type Journal Article
    ZDB-ID 219351-6
    ISSN 1869-5868 ; 0021-2148
    ISSN (online) 1869-5868
    ISSN 0021-2148
    DOI 10.1002/ijch.201800113
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  5. Article ; Online: Unifying principles of bifunctional, proximity-inducing small molecules.

    Gerry, Christopher J / Schreiber, Stuart L

    Nature chemical biology

    2020  Volume 16, Issue 4, Page(s) 369–378

    Abstract: Nature uses a variety of tools to mediate the flow of information in cells, many of which control distances between key biomacromolecules. Researchers have thus generated compounds whose activities stem from interactions with two (or more) proteins ... ...

    Abstract Nature uses a variety of tools to mediate the flow of information in cells, many of which control distances between key biomacromolecules. Researchers have thus generated compounds whose activities stem from interactions with two (or more) proteins simultaneously. In this Perspective, we describe how these 'bifunctional' small molecules facilitate the study of an increasingly wide range of complex biological phenomena and enable the drugging of otherwise challenging therapeutic targets and processes. Despite their structural and functional differences, all bifunctional molecules employ Nature's strategy of altering interactomes and inducing proximity to modulate biology. They therefore exhibit a shared set of chemical and biophysical principles that have not yet been appreciated fully. By highlighting these commonalities-and their wide-ranging consequences-we hope to chip away at the artificial barriers that threaten to constrain this interdisciplinary field. Doing so promises to yield remarkable benefits for biological research and therapeutics discovery.
    MeSH term(s) Animals ; Humans ; Protein Binding/physiology ; Protein Interaction Domains and Motifs/physiology ; Proteins/chemistry ; Small Molecule Libraries ; Structure-Activity Relationship
    Chemical Substances Proteins ; Small Molecule Libraries
    Language English
    Publishing date 2020-03-20
    Publishing country United States
    Document type Journal Article ; Research Support, N.I.H., Extramural ; Review
    ZDB-ID 2202962-X
    ISSN 1552-4469 ; 1552-4450
    ISSN (online) 1552-4469
    ISSN 1552-4450
    DOI 10.1038/s41589-020-0469-1
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    Zs.A 6251: Show issues Location:
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  6. Article ; Online: Progress in Understanding Ferroptosis and Challenges in Its Targeting for Therapeutic Benefit.

    Zou, Yilong / Schreiber, Stuart L

    Cell chemical biology

    2020  Volume 27, Issue 4, Page(s) 463–471

    Abstract: Ferroptosis is an iron-dependent cell-death modality driven by oxidative phospholipid damage. In contrast to apoptosis, which enables organisms to eliminate targeted cells purposefully at specific times, ferroptosis appears to be a vulnerability of cells ...

    Abstract Ferroptosis is an iron-dependent cell-death modality driven by oxidative phospholipid damage. In contrast to apoptosis, which enables organisms to eliminate targeted cells purposefully at specific times, ferroptosis appears to be a vulnerability of cells that otherwise use high levels of polyunsaturated lipids to their advantage. Cells in this high polyunsaturated lipid state generally have safeguards that mitigate ferroptotic risk. Since its recognition, ferroptosis has been implicated in degenerative diseases in tissues including kidney and brain, and is a targetable vulnerability in multiple cancers-each likely characterized by the high polyunsaturated lipid state with insufficient or overwhelmed ferroptotic safeguards. In this Perspective, we present progress toward defining the essential roles and key mediators of lipid peroxidation and ferroptosis in disease contexts. Moreover, we discuss gaps in our understanding of ferroptosis and list key challenges that have thus far limited the full potential of targeting ferroptosis for improving human health.
    MeSH term(s) Animals ; Fatty Acids, Unsaturated/metabolism ; Ferroptosis/drug effects ; Humans ; Lipid Peroxidation/drug effects ; Molecular Probes/chemistry ; Molecular Probes/metabolism ; Molecular Probes/pharmacology ; Molecular Probes/therapeutic use ; Neoplasms/metabolism ; Neoplasms/pathology ; Neoplasms/therapy ; Phospholipid Hydroperoxide Glutathione Peroxidase/antagonists & inhibitors ; Phospholipid Hydroperoxide Glutathione Peroxidase/metabolism ; Reactive Oxygen Species/metabolism ; Reperfusion Injury/metabolism ; Reperfusion Injury/pathology ; Reperfusion Injury/therapy
    Chemical Substances Fatty Acids, Unsaturated ; Molecular Probes ; Reactive Oxygen Species ; Phospholipid Hydroperoxide Glutathione Peroxidase (EC 1.11.1.12)
    Language English
    Publishing date 2020-06-04
    Publishing country United States
    Document type Journal Article ; Research Support, N.I.H., Extramural ; Review
    ISSN 2451-9448
    ISSN (online) 2451-9448
    DOI 10.1016/j.chembiol.2020.03.015
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  7. Article: Bifunctional small molecules that induce nuclear localization and targeted transcriptional regulation.

    Gibson, William J / Sadagopan, Ananthan / Shoba, Veronika M / Choudhary, Amit / Meyerson, Matthew / Schreiber, Stuart L

    bioRxiv : the preprint server for biology

    2023  

    Abstract: The aberrant localization of proteins in cells is a key factor in the development of various diseases, including cancer and neurodegenerative disease. To better understand and potentially manipulate protein localization for therapeutic purposes, we ... ...

    Abstract The aberrant localization of proteins in cells is a key factor in the development of various diseases, including cancer and neurodegenerative disease. To better understand and potentially manipulate protein localization for therapeutic purposes, we engineered bifunctional compounds that bind to proteins in separate cellular compartments. We show these compounds induce nuclear import of cytosolic cargoes, using nuclear-localized BRD4 as a "carrier" for co-import and nuclear trapping of cytosolic proteins. We use this system to calculate kinetic constants for passive diffusion across the nuclear pore and demonstrate single-cell heterogeneity in response to these bifunctional molecules, with cells requiring high carrier to cargo expression for complete import. We also observe incorporation of cargoes into BRD4-containing condensates. Proteins shown to be substrates for nuclear transport include oncogenic mutant nucleophosmin (NPM1c) and mutant PI3K catalytic subunit alpha (PIK3CA
    Language English
    Publishing date 2023-07-07
    Publishing country United States
    Document type Preprint
    DOI 10.1101/2023.07.07.548101
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  8. Article: Bicyclic pyrrolidine inhibitors of

    Ence, Chloe C / Uddin, Taher / Borrel, Julien / Mittal, Payal / Xie, Han / Zoller, Jochen / Sharma, Amit / Comer, Eamon / Schreiber, Stuart L / Melillo, Bruno / Sibley, L David / Chatterjee, Arnab K

    bioRxiv : the preprint server for biology

    2024  

    Abstract: Previous studies have shown that bicyclic azetidines are potent and selective inhibitors of apicomplexan phenylalanine tRNA synthetase (PheRS), leading to parasite growth ... ...

    Abstract Previous studies have shown that bicyclic azetidines are potent and selective inhibitors of apicomplexan phenylalanine tRNA synthetase (PheRS), leading to parasite growth inhibition
    Language English
    Publishing date 2024-02-28
    Publishing country United States
    Document type Preprint
    DOI 10.1101/2024.02.28.582607
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  9. Article ; Online: Modular Synthesis of Cyclopropane-Fused N-Heterocycles Enabled by Underexplored Diazo Reagents.

    Richter, Matthieu J R / Zécri, Frédéric J / Briner, Karin / Schreiber, Stuart L

    Angewandte Chemie (International ed. in English)

    2022  Volume 61, Issue 38, Page(s) e202203221

    Abstract: Cyclopropane-fused N-heterocycles are featured in various biologically active compounds and represent attractive scaffolds in medicinal chemistry. However, synthesis routes to access structurally and functionally diverse cyclopropane-fused N-heterocycles ...

    Abstract Cyclopropane-fused N-heterocycles are featured in various biologically active compounds and represent attractive scaffolds in medicinal chemistry. However, synthesis routes to access structurally and functionally diverse cyclopropane-fused N-heterocycles remain underexplored. Leveraging novel α-diazo acylating agents, we report a general approach for the direct and modular synthesis of cyclopropane-fused lactams from unsaturated amines. The operationally simple transformation, which proceeds through successive acylation, (3+2) cycloaddition and fragmentation, tolerates a broad range of functional groups and yields a wide spectrum of complex molecular scaffolds, including fused, bridged and spiro ring systems. We demonstrate the utility of this transformation in the concise syntheses of therapeutic agents milnaciprane and amitifadine.
    MeSH term(s) Amines/chemistry ; Cycloaddition Reaction ; Cyclopropanes/chemistry ; Indicators and Reagents ; Lactams
    Chemical Substances Amines ; Cyclopropanes ; Indicators and Reagents ; Lactams
    Language English
    Publishing date 2022-04-25
    Publishing country Germany
    Document type Journal Article ; Research Support, N.I.H., Extramural ; Research Support, Non-U.S. Gov't
    ZDB-ID 2011836-3
    ISSN 1521-3773 ; 1433-7851
    ISSN (online) 1521-3773
    ISSN 1433-7851
    DOI 10.1002/anie.202203221
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  10. Article ; Online: Bifunctional Small Molecules That Induce Nuclear Localization and Targeted Transcriptional Regulation.

    Gibson, William J / Sadagopan, Ananthan / Shoba, Veronika M / Choudhary, Amit / Meyerson, Matthew / Schreiber, Stuart L

    Journal of the American Chemical Society

    2023  Volume 145, Issue 48, Page(s) 26028–26037

    Abstract: The aberrant localization of proteins in cells is a key factor in the development of various diseases, including cancer and neurodegenerative disease. To better understand and potentially manipulate protein localization for therapeutic purposes, we ... ...

    Abstract The aberrant localization of proteins in cells is a key factor in the development of various diseases, including cancer and neurodegenerative disease. To better understand and potentially manipulate protein localization for therapeutic purposes, we engineered bifunctional compounds that bind to proteins in separate cellular compartments. We show these compounds induce nuclear import of cytosolic cargoes, using nuclear-localized BRD4 as a "carrier" for co-import and nuclear trapping of cytosolic proteins. We use this system to calculate kinetic constants for passive diffusion across the nuclear pore and demonstrate single-cell heterogeneity in response to these bifunctional molecules with cells requiring high carrier to cargo expression for complete import. We also observe incorporation of cargo into BRD4-containing condensates. Proteins shown to be substrates for nuclear transport include oncogenic mutant nucleophosmin (NPM1c) and mutant PI3K catalytic subunit alpha (PIK3CA
    MeSH term(s) Humans ; Nuclear Proteins/metabolism ; Cell Nucleus/metabolism ; Neurodegenerative Diseases/metabolism ; Transcription Factors/metabolism ; Active Transport, Cell Nucleus ; Cell Cycle Proteins/metabolism
    Chemical Substances Nuclear Proteins ; Transcription Factors ; BRD4 protein, human ; Cell Cycle Proteins
    Language English
    Publishing date 2023-11-22
    Publishing country United States
    Document type Journal Article ; Research Support, N.I.H., Extramural ; Research Support, Non-U.S. Gov't
    ZDB-ID 3155-0
    ISSN 1520-5126 ; 0002-7863
    ISSN (online) 1520-5126
    ISSN 0002-7863
    DOI 10.1021/jacs.3c06179
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