| 摘要 |
<P>PROBLEM TO BE SOLVED: To solve important problems associated with trials to crystallize GPCR, namely their lack of stability in surfactants and the fact that they exist in multiple steric structures. <P>SOLUTION: A method for selecting a G-protein coupled receptor (GPCR) with increased stability is disclosed. The method comprises (a) a process of providing one or more mutants of a parent GPCR, (b) a process of selecting a ligand, which binds to the parent GPCR when it includes a particular steric structures, (c) a process of measuring whether or not either the GPCR mutants or each of them has increased stability with respect to binding the selected ligand compared to the stability of the parent GPCR with respect to binding that ligand, and (d) a process of selecting those mutants that have increased stability compared to the parent GPCR with respect to binding the selected ligand. Mutants of β-adrenergic receptor, adenosine receptor and neurotensin receptor are also disclosed. <P>COPYRIGHT: (C)2012,JPO&INPIT |
