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Kinetic Template‐Guided Tethering of Fragments
Author(s) -
oo Rebecca H.,
Armstrong Alan,
Mann David J.
Publication year - 2012
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201200404
Subject(s) - tethering , chemistry , conjugate , mass spectrometry , adduct , combinatorial chemistry , acrylamide , small molecule , biophysics , thiol , stereochemistry , biochemistry , chromatography , organic chemistry , biology , polymer , monomer , microbiology and biotechnology , mathematical analysis , mathematics
Birds of a tether: A tethering strategy for the site‐directed discovery of low‐molecular‐weight fragments that bind weakly to defined protein surfaces is described. A solvent‐exposed protein thiol captures acrylamide‐modified fragments in a conjugate addition reaction that requires a template to produce a measureable quantity of protein–fragment adduct, which can be rapidly identified by mass spectrometry.