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High-Throughput Interrogation of Ligand Binding Mode Using a Fluorescence-Based Assay

Authors

  • Dr. Paweł Śledź,

    1. University Chemical Laboratory, University of Cambridge, Lensfield Road, Cambridge CB2 1EW (UK)
    2. Current address: Max Planck Institute of Biochemistry, Am Klopferspitz 18, 82152 Martinsried (Germany)
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    • These authors contributed equally to this work.

  • Dr. Steffen Lang,

    1. University Chemical Laboratory, University of Cambridge, Lensfield Road, Cambridge CB2 1EW (UK)
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    • These authors contributed equally to this work.

  • Christopher J. Stubbs,

    1. University Chemical Laboratory, University of Cambridge, Lensfield Road, Cambridge CB2 1EW (UK)
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  • Prof. Chris Abell

    Corresponding author
    1. University Chemical Laboratory, University of Cambridge, Lensfield Road, Cambridge CB2 1EW (UK)
    • University Chemical Laboratory, University of Cambridge, Lensfield Road, Cambridge CB2 1EW (UK)
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  • We thank Dr. Marko Hyvönen for helpful discussions and Dr. Dima Chirgadze for maintaining the Crystallographic X-ray Facility at the Department of Biochemistry, University of Cambridge. This work was supported by the Wellcome Trust. Furthermore, we acknowledge the funding from the Gates Cambridge Trust and St. Edmund’s College (P.Ś.), German Academic Exchange Service—DAAD (S.L.), and Cancer Research UK (C.J.S.). The use of beamtime at the European Synchrotron Radiation Facility is gratefully acknowledged.

Abstract

original image

Tascheninspektion: Ein fluoreszenzbasierter Hochdurchsatz-Assay (FTS-Assay), der auf der temperaturabhängigen Entfaltung von verschiedenen Formen eines Proteins (in Grau) beruht, wurde für die Bestimmung von Bindungsmodi eines Liganden entwickelt. Dieser Assay wurde durch die rasche Beurteilung von bindungsmodusabhängigen Struktur-Aktivitäts-Beziehungen der Polobox-Domäne von Plk1, einem wichtigen Ziel in der Krebstherapie, validiert.

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