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High‐Throughput Interrogation of Ligand Binding Mode Using a Fluorescence‐Based Assay
Author(s) -
Śledź Paweł,
Lang Steffen,
Stubbs Christopher J.,
Abell Chris
Publication year - 2012
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.201202660
Subject(s) - ligand binding assay , fluorescence , ligand (biochemistry) , high throughput screening , chemistry , interrogation , throughput , biophysics , combinatorial chemistry , computational biology , computer science , biochemistry , biology , receptor , physics , optics , telecommunications , archaeology , wireless , history
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.
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