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Human methionine aminopeptidase type 2 (hMetAP-2) was identified as the molecular target of anti-angiogenic agents such as fumagillin and its analogues. We describe here the crystal structure of hMetAP-2 in complex with l-methionine and d-methionine at 1.9 and 2.0A resolution, respectively. The comparison of the structure of the two complexes establishes the basis of enantiomer discrimination and provides some considerations for the design of selective MetAP-2 inhibitors.

Citation

M Cristina Nonato, Joanne Widom, Jon Clardy. Human methionine aminopeptidase type 2 in complex with L- and D-methionine. Bioorganic & medicinal chemistry letters. 2006 May 15;16(10):2580-3

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PMID: 16540317

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