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NMR‐Guided Fragment‐Based Approach for the Design of tRNA Lys3 Ligands
Author(s) -
Chung Florence,
Tisné Carine,
Lecourt Thomas,
Dardel Frédéric,
Micouin Laurent
Publication year - 2007
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.200605201
Subject(s) - chemistry , dissociation constant , ligand (biochemistry) , dissociation (chemistry) , fragment (logic) , stereochemistry , transfer rna , crystallography , organic chemistry , mathematics , biochemistry , rna , receptor , algorithm , gene
Two in one : Two ligands for tRNA Lys3 that were identified from a compound library by flow‐injection NMR spectroscopic screening and found to have millimolar dissociation constants (on the left in the picture) inspired the fragment‐based synthesis of a new family of ligands with the general structural features of both initial compounds. Ligand 1 of this family is a selective D‐stem binder of tRNA Lys3 with a micromolar K d value.