High-throughput interrogation of ligand binding mode using a fluorescence-based assay.
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.
University Chemical Laboratory, University of Cambridge, Lensfield Road, Cambridge CB2 1EW, UK.
Paweł
P
Śledź
Steffen
S
Lang
Christopher J
CJ
Stubbs
Chris
C
Abell
D001665:Binding Sites; D002151:Calorimetry; D005453:Fluorescence; D057166:High-Throughput Screening Assays; D008024:Ligands; D008958:Models, Molecular; D015394:Molecular Structure; D009154:Mutation; D011506:Proteins / Q000737:chemistry / Q000235:genetics; D013329:Structure-Activity Relationship; D013696:Temperature
D008024:Ligands; D011506:Proteins