Crystal structure determination of microsomal prostaglandin E2 synthase 1 with the open active site.

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Human membrane protein MPGES1, which is a responsible protein for biosynthesis of prostaglandin E2 as a proinflammatory lipid mediator, was crystallized in a lipidic meso crystallization method. MPGES1 in the lipidic meso phase could be a structure more similar to a structure in cell membrane due to the similarity between the structures of the lipidic meso phase and cell membrane. The inhibitors for MPGES1 were found out from the candidates from the in silico screening targeted to the active site of leukotriene C4 synthase belonging in the same protein family with MPGES1. These results will contribute the elucidation of the structure basis of molecular functions of MPGES1.