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TitleNovel reversible methionine aminopeptidase-2 (MetAP-2) inhibitors based on purine and related bicyclic templates.
Journal, issue, pagesBioorg. Med. Chem. Lett., Vol. 27, Page 551-556, Year 2017
Publish dateSep 28, 2016 (structure data deposition date)
AuthorsHeinrich, T. / Buchstaller, H.P. / Cezanne, B. / Rohdich, F. / Bomke, J. / Friese-Hamim, M. / Krier, M. / Knochel, T. / Musil, D. / Leuthner, B. / Zenke, F.
External linksBioorg. Med. Chem. Lett. / PubMed:27998678
MethodsX-ray diffraction
Resolution1.69 - 1.9 Å
Structure data

PDB-5lyw:
CRYSTAL STRUCTURE OF HUMAN METHIONINE AMINOPEPTIDASE-2 IN COMPLEX; WITH AN INHIBITOR 6-((R)-2-o-Tolyloxymethyl-pyrrolidin-1-yl)-9H-purine
Method: X-RAY DIFFRACTION / Resolution: 1.69 Å

PDB-5lyx:
CRYSTAL STRUCTURE OF HUMAN METHIONINE AMINOPEPTIDASE-2 IN COMPLEX; WITH AN INHIBITOR 5-((R)-1-[1,2,4]Triazolo[1,5-a]pyrimidin-7-yl-pyrrolidin-2-ylmethoxy)-isoquinoline
Method: X-RAY DIFFRACTION / Resolution: 1.9 Å

Chemicals

ChemComp-7BH:
6-[(2~{R})-2-[(2-methylphenoxy)methyl]pyrrolidin-1-yl]-7~{H}-purine

ChemComp-MN:
Unknown entry

ChemComp-HOH:
WATER

ChemComp-7BF:
5-[[(2~{R})-1-([1,2,4]triazolo[1,5-a]pyrimidin-7-yl)pyrrolidin-2-yl]methoxy]isoquinoline

Source
  • homo sapiens (human)
KeywordsHYDROLASE / PEPTIDASE / METAL ION BINDING / PROTEOLYSIS / HYDROLASE- HYDROLASE INHIBITOR COMPLEX

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