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Selective Identification of Cooperatively Binding Fragments in a High‐Throughput Ligation Assay Enables Development of a Picomolar Caspase‐3 Inhibitor
Author(s) -
Schmidt Marco F.,
ElDahshan Adeeb,
Keller Sandro,
Rademann Jörg
Publication year - 2009
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.200901647
Subject(s) - ligation , chemistry , proximity ligation assay , fluorescence anisotropy , fluorescence , derivative (finance) , combinatorial chemistry , biophysics , biochemistry , microbiology and biotechnology , biology , receptor , physics , quantum mechanics , membrane , financial economics , economics
Putting the pieces together : A chemically reactive fluorescence polarization (FP) probe can be use to detect positively cooperative fragments through the overadditive binding of their ligation products. For confirmation, an stable derivative of the ligation product was prepared and found to be significantly more active than all previously reported caspase‐3 inhibitors.