These authors contributed equally to this work.
High-Throughput Interrogation of Ligand Binding Mode Using a Fluorescence-Based Assay†
Article first published online: 22 JUN 2012
Copyright © 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim
Angewandte Chemie International Edition
Volume 51, Issue 31, pages 7680–7683, July 27, 2012
How to Cite
Śledź, P., Lang, S., Stubbs, C. J. and Abell, C. (2012), High-Throughput Interrogation of Ligand Binding Mode Using a Fluorescence-Based Assay . Angew. Chem. Int. Ed., 51: 7680–7683. doi: 10.1002/anie.201202660
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.
- Issue published online: 25 JUL 2012
- Article first published online: 22 JUN 2012
- Manuscript Received: 5 APR 2012
- Funded Access
- Wellcome Trust
- Gates Cambridge Trust
- St. Edmund’s College
- German Academic Exchange Service—DAAD
- Cancer Research UK
- binding mode;
- drug discovery;
- ligand design;
- protein structures;
- structure–activity relationships
Probing the pocket: A high-throughput fluorescence-based thermal shift (FTS) assay utilized different forms of a protein (in gray) to establish the binding mode of a ligand (see picture). The assay serves in the rapid evaluation of structure–activity binding-mode relationships for a series of ligands of Plk1, an important target of anticancer therapy.