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  1. Book: Chemical proteomics

    Drewes, Gerard / Bantscheff, Marcus

    methods and protocols

    (Methods in molecular biology ; 803 ; Springer protocols)

    2012  

    Author's details ed. by Gerard Drewes and Marcus Bantscheff
    Series title Methods in molecular biology ; 803
    Springer protocols
    Collection
    Language English
    Size XI, 313 S. : Ill., graph. Darst.
    Publisher Humana Press
    Publishing place New York u.a.
    Publishing country United States
    Document type Book
    HBZ-ID HT016969993
    ISBN 978-1-61779-363-9 ; 9781617793646 ; 1-61779-363-9 ; 1617793647
    Database Catalogue ZB MED Medicine, Health

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    In stock of ZB MED Cologne/Königswinter

    Shelf markLoan statusLocation
    2011 A 5483 order for loan Magazin

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  2. Article ; Online: Chemical proteomics in drug discovery.

    Drewes, Gerard

    Methods in molecular biology (Clifton, N.J.)

    2012  Volume 803, Page(s) 15–21

    Abstract: Real-world drug discovery and development remains a notoriously unproductive and increasingly uneconomical process even in the Omics era. The dominating paradigm in the industry continues to be target-based drug design, with an increased perception of ... ...

    Abstract Real-world drug discovery and development remains a notoriously unproductive and increasingly uneconomical process even in the Omics era. The dominating paradigm in the industry continues to be target-based drug design, with an increased perception of the role of signaling pathways in homeostasis and in disease. Since proteins represent the major type of drug targets, proteomics-based approaches, which study proteins under relatively physiological conditions, have great potential if they can be reduced to practice such that they successfully complement the arsenal of drug discovery techniques. This chapter discusses examples of drug discovery processes where chemical proteomics-based assays using native endogenous proteins should have substantial impact.
    MeSH term(s) Drug Delivery Systems ; Drug Discovery/methods ; Proteomics/methods ; Reproducibility of Results ; Small Molecule Libraries/analysis ; Small Molecule Libraries/pharmacology
    Chemical Substances Small Molecule Libraries
    Language English
    Publishing date 2012
    Publishing country United States
    Document type Journal Article ; Review
    ISSN 1940-6029
    ISSN (online) 1940-6029
    DOI 10.1007/978-1-61779-364-6_2
    Database MEDical Literature Analysis and Retrieval System OnLINE

    Full text online

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  3. Article ; Online: Chemoproteomics and Chemical Probes for Target Discovery.

    Drewes, Gerard / Knapp, Stefan

    Trends in biotechnology

    2018  Volume 36, Issue 12, Page(s) 1275–1286

    Abstract: Chemical probes represent versatile tools to validate disease-modifying targets. However, evaluating the selectivity of chemical probes in complex cellular systems is a major challenge that needs to be addressed to better understand the mode of action of ...

    Abstract Chemical probes represent versatile tools to validate disease-modifying targets. However, evaluating the selectivity of chemical probes in complex cellular systems is a major challenge that needs to be addressed to better understand the mode of action of small molecules and the interpretation of their pharmacological effects. Chemoproteomics has emerged as a key technology to characterize the mode of action of pharmacological modulators such as chemical probes and drugs, and these studies have unraveled the cellular targets of many bioactive compounds. Here we review the role of chemical probes for the validation of new therapeutic targets and their characterization by proteome wide affinity- and activity-based chemical proteomics and recently developed label-free technologies.
    MeSH term(s) Drug Discovery/methods ; Pharmacology/methods ; Proteome/analysis ; Proteomics/methods
    Chemical Substances Proteome
    Language English
    Publishing date 2018-07-13
    Publishing country England
    Document type Journal Article ; Research Support, Non-U.S. Gov't ; Review
    ZDB-ID 47474-5
    ISSN 1879-3096 ; 0167-7799
    ISSN (online) 1879-3096
    ISSN 0167-7799
    DOI 10.1016/j.tibtech.2018.06.008
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 2750: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
    Jg. 1995 - 2021: Lesesall (2.OG)
    ab Jg. 2022: Lesesaal (EG)

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  4. Article: Chemoproteomics and Chemical Probes for Target Discovery

    Drewes, Gerard / Stefan Knapp

    Trends in biotechnology. 2018 Dec., v. 36, no. 12

    2018  

    Abstract: Chemical probes represent versatile tools to validate disease-modifying targets. However, evaluating the selectivity of chemical probes in complex cellular systems is a major challenge that needs to be addressed to better understand the mode of action of ...

    Abstract Chemical probes represent versatile tools to validate disease-modifying targets. However, evaluating the selectivity of chemical probes in complex cellular systems is a major challenge that needs to be addressed to better understand the mode of action of small molecules and the interpretation of their pharmacological effects. Chemoproteomics has emerged as a key technology to characterize the mode of action of pharmacological modulators such as chemical probes and drugs, and these studies have unraveled the cellular targets of many bioactive compounds. Here we review the role of chemical probes for the validation of new therapeutic targets and their characterization by proteome wide affinity- and activity-based chemical proteomics and recently developed label-free technologies.
    Keywords bioactive compounds ; drugs ; mechanism of action ; proteome ; proteomics ; therapeutics
    Language English
    Dates of publication 2018-12
    Size p. 1275-1286.
    Publishing place Elsevier Ltd
    Document type Article
    ZDB-ID 47474-5
    ISSN 1879-3096 ; 0167-7799
    ISSN (online) 1879-3096
    ISSN 0167-7799
    DOI 10.1016/j.tibtech.2018.06.008
    Database NAL-Catalogue (AGRICOLA)

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 2750: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
    Jg. 1995 - 2021: Lesesall (2.OG)
    ab Jg. 2022: Lesesaal (EG)

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  5. Book: Chemical proteomics

    Bantscheff, Marcus / Drewes, Gerard

    methods and protocols

    (Methods in molecular biology ; 803 ; Springer protocols)

    2012  

    Author's details ed. by Gerard Drewes and Marcus Bantscheff
    Series title Methods in molecular biology ; 803
    Springer protocols
    MeSH term(s) Biochemistry/methods ; Chemistry Techniques, Analytical/methods ; Proteomics/methods
    Keywords Biochemistry ; Proteomics
    Language English
    Size XI, 313 S., Ill., graph. Darst
    Publisher Humana Pr
    Publishing place New York u.a.
    Document type Book
    Note Literaturangaben
    ISBN 1617793639 ; 9781617793639
    Database Leibniz Institute of Plant Biochemistry

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  6. Book: Chemical proteomics

    Drewes, Gerard / Bantscheff, Marcus

    methods and protocols

    (Methods in molecular biology, ; 803 ; Springer protocols)

    2012  

    Author's details edited by Gerard Drews and Marcus Bantscheff
    Series title Methods in molecular biology, ; 803
    Springer protocols
    MeSH term(s) Proteomics/methods ; Chemistry Techniques, Analytical ; Biochemical Phenomena
    Language English
    Size xi, 313 p. :, ill. ;, 27 cm.
    Publisher Humana Press
    Publishing place New York
    Document type Book
    ISBN 9781617793639 ; 1617793639 ; 9781617793646 ; 1617793647
    Database Catalogue of the US National Library of Medicine (NLM)

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  7. Article ; Online: Mapping the functional impact of non-coding regulatory elements in primary T cells through single-cell CRISPR screens.

    Alda-Catalinas, Celia / Ibarra-Soria, Ximena / Flouri, Christina / Gordillo, Jorge Esparza / Cousminer, Diana / Hutchinson, Anna / Sun, Bin / Pembroke, William / Ullrich, Sebastian / Krejci, Adam / Cortes, Adrian / Acevedo, Alison / Malla, Sunir / Fishwick, Carl / Drewes, Gerard / Rapiteanu, Radu

    Genome biology

    2024  Volume 25, Issue 1, Page(s) 42

    Abstract: Background: Drug targets with genetic evidence are expected to increase clinical success by at least twofold. Yet, translating disease-associated genetic variants into functional knowledge remains a fundamental challenge of drug discovery. A key issue ... ...

    Abstract Background: Drug targets with genetic evidence are expected to increase clinical success by at least twofold. Yet, translating disease-associated genetic variants into functional knowledge remains a fundamental challenge of drug discovery. A key issue is that the vast majority of complex disease associations cannot be cleanly mapped to a gene. Immune disease-associated variants are enriched within regulatory elements found in T-cell-specific open chromatin regions.
    Results: To identify genes and molecular programs modulated by these regulatory elements, we develop a CRISPRi-based single-cell functional screening approach in primary human T cells. Our pipeline enables the interrogation of transcriptomic changes induced by the perturbation of regulatory elements at scale. We first optimize an efficient CRISPRi protocol in primary CD4
    Conclusions: We describe "primary T cell crisprQTL" - a scalable, single-cell functional genomics approach for mapping regulatory elements to genes in primary human T cells. We show how this framework can facilitate the interrogation of immune disease GWAS hits and propose that the combination of experimental and QTL-based techniques is likely to address the variant-to-function problem.
    MeSH term(s) Humans ; Clustered Regularly Interspaced Short Palindromic Repeats ; T-Lymphocytes ; Regulatory Sequences, Nucleic Acid ; Chromatin/genetics ; Immune System Diseases/genetics ; Genome-Wide Association Study ; Polymorphism, Single Nucleotide
    Chemical Substances Chromatin
    Language English
    Publishing date 2024-02-02
    Publishing country England
    Document type Journal Article
    ZDB-ID 2040529-7
    ISSN 1474-760X ; 1474-760X
    ISSN (online) 1474-760X
    ISSN 1474-760X
    DOI 10.1186/s13059-024-03176-z
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  8. Article ; Online: Drug selectivity: Running in the family.

    Muelbaier, Marcel / Drewes, Gerard

    Nature chemical biology

    2014  Volume 10, Issue 8, Page(s) 608–609

    MeSH term(s) Animals ; Dipeptidyl-Peptidase IV Inhibitors/pharmacology ; Enzyme Inhibitors/pharmacology ; Female ; High-Throughput Screening Assays/methods ; Humans ; Male
    Chemical Substances Dipeptidyl-Peptidase IV Inhibitors ; Enzyme Inhibitors
    Language English
    Publishing date 2014-07-06
    Publishing country United States
    Document type Journal Article ; Comment
    ZDB-ID 2202962-X
    ISSN 1552-4469 ; 1552-4450
    ISSN (online) 1552-4469
    ISSN 1552-4450
    DOI 10.1038/nchembio.1585
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 6251: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 2021: Bestellungen von Artikeln über das Online-Bestellformular
    ab Jg. 2022: Lesesaal (EG)
    Zs.MG 90: Show issues

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  9. Article ; Online: Correction: Inhibitors of Rho kinases (ROCK) induce multiple mitotic defects and synthetic lethality in BRCA2-deficient cells.

    Martino, Julieta / Siri, Sebastián Omar / Calzetta, Nicolás Luis / Paviolo, Natalia Soledad / Garro, Cintia / Pansa, Maria F / Carbajosa, Sofía / Brown, Aaron C / Bocco, José Luis / Gloger, Israel / Drewes, Gerard / Madauss, Kevin P / Soria, Gastón / Gottifredi, Vanesa

    eLife

    2023  Volume 12

    Language English
    Publishing date 2023-11-14
    Publishing country England
    Document type Published Erratum
    ZDB-ID 2687154-3
    ISSN 2050-084X ; 2050-084X
    ISSN (online) 2050-084X
    ISSN 2050-084X
    DOI 10.7554/eLife.94414
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  10. Article ; Online: Inhibitors of Rho kinases (ROCK) induce multiple mitotic defects and synthetic lethality in BRCA2-deficient cells.

    Martino, Julieta / Siri, Sebastián Omar / Calzetta, Nicolás Luis / Paviolo, Natalia Soledad / Garro, Cintia / Pansa, Maria F / Carbajosa, Sofía / Brown, Aaron C / Bocco, José Luis / Gloger, Israel / Drewes, Gerard / Madauss, Kevin P / Soria, Gastón / Gottifredi, Vanesa

    eLife

    2023  Volume 12

    Abstract: The trapping of Poly-ADP-ribose polymerase (PARP) on DNA caused by PARP inhibitors (PARPi) triggers acute DNA replication stress and synthetic lethality (SL) in BRCA2-deficient cells. Hence, DNA damage is accepted as a prerequisite for SL in BRCA2- ... ...

    Abstract The trapping of Poly-ADP-ribose polymerase (PARP) on DNA caused by PARP inhibitors (PARPi) triggers acute DNA replication stress and synthetic lethality (SL) in BRCA2-deficient cells. Hence, DNA damage is accepted as a prerequisite for SL in BRCA2-deficient cells. In contrast, here we show that inhibiting ROCK in BRCA2-deficient cells triggers SL independently from acute replication stress. Such SL is preceded by polyploidy and binucleation resulting from cytokinesis failure. Such initial mitosis abnormalities are followed by other M phase defects, including anaphase bridges and abnormal mitotic figures associated with multipolar spindles, supernumerary centrosomes and multinucleation. SL was also triggered by inhibiting Citron Rho-interacting kinase, another enzyme that, similarly to ROCK, regulates cytokinesis. Together, these observations demonstrate that cytokinesis failure triggers mitotic abnormalities and SL in BRCA2-deficient cells. Furthermore, the prevention of mitotic entry by depletion of Early mitotic inhibitor 1 (EMI1) augmented the survival of BRCA2-deficient cells treated with ROCK inhibitors, thus reinforcing the association between M phase and cell death in BRCA2-deficient cells. This novel SL differs from the one triggered by PARPi and uncovers mitosis as an Achilles heel of BRCA2-deficient cells.
    MeSH term(s) Anaphase ; DNA Damage ; Mitosis ; Poly(ADP-ribose) Polymerase Inhibitors/pharmacology ; Poly(ADP-ribose) Polymerases/metabolism ; Synthetic Lethal Mutations ; rho-Associated Kinases/antagonists & inhibitors ; BRCA2 Protein/genetics ; Humans
    Chemical Substances Poly(ADP-ribose) Polymerase Inhibitors ; Poly(ADP-ribose) Polymerases (EC 2.4.2.30) ; rho-Associated Kinases (EC 2.7.11.1) ; BRCA2 Protein
    Language English
    Publishing date 2023-04-19
    Publishing country England
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 2687154-3
    ISSN 2050-084X ; 2050-084X
    ISSN (online) 2050-084X
    ISSN 2050-084X
    DOI 10.7554/eLife.80254
    Database MEDical Literature Analysis and Retrieval System OnLINE

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