USE OF TWO-DIMENSIONAL 15N/1H NMR CORRELATION SPECTROSCOPY IN A PROCESS FOR DESIGNING HIGH-AFFINITY LIGANDS TO TARGET MOLECULES

摘要

A process for designing a high affinity ligand to a given target molecule, comprising: (a) identifying at least two ligands to the target molecule which bind to distinct binding sites on the target molecule using two dimensional 15N/1H NMR correlation spectroscopy; (b) forming at least a ternary complex by exposing the at least two ligands to the target molecule; (c) determining the three dimensional structure of the complex and the spatial orientation of the at least two ligands on the target molecule; and (d) using the spatial orientation determined in step (c) to design the affinity ligand. 989 י" ב בסיון התשס" ד - June 1, 2004