| 摘要 |
<P>PROBLEM TO BE SOLVED: To provide a method for screening an inhibitor of a γ-glutamylcysteine synthetase (γGCS) specific to parasites, etc. <P>SOLUTION: The screening method contains a step to prepare a human-type γGCS having arginine as the 132nd amino acid residue of E.coli γGCS and a non-human-type γGCS having an amino acid residue other than arginine as the 132nd residue of the above γGCS, contact a prepared candidate drug compound with the human-type γGCS and the non-human-type γGCS, evaluate the bond strength and select the drug candidate compound exhibiting higher bond strength to the non-human-type γGCS than the human-type γGCS. Preferably, the design of the drug candidate compound to be used in the screening method is a cocrystal of the E.coli γGCS and a substrate transition state analog, and is based on the steric structure data of the γGCS obtained by the analysis of a crystal having P2<SB>1</SB>space group. <P>COPYRIGHT: (C)2006,JPO&NCIPI |
