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

Summary for 5LYX

• Entry DOI: 10.2210/pdb5lyx/pdb
• Descriptor: Methionine aminopeptidase 2, 5-[[(2~{R})-1-([1,2,4]triazolo[1,5-a]pyrimidin-7-yl)pyrrolidin-2-yl]methoxy]isoquinoline, MANGANESE (II) ION, ... (4 entities in total)
• Functional Keywords: hydrolase, peptidase, metal ion binding, proteolysis, hydrolase- hydrolase inhibitor complex
• Biological source: Homo sapiens (Human)
• Cellular location: Cytoplasm : P50579
• Total number of polymer chains: 1
• Total formula weight: 42926.47

Authors

Musil, D.,Heinrich, T.,Lehmann, M. (deposition date: 2016-09-29, release date: 2017-08-16)

• Primary citation: Heinrich, T.,Buchstaller, H.P.,Cezanne, B.,Rohdich, F.,Bomke, J.,Friese-Hamim, M.,Krier, M.,Knochel, T.,Musil, D.,Leuthner, B.,Zenke, F.; Novel reversible methionine aminopeptidase-2 (MetAP-2) inhibitors based on purine and related bicyclic templates.; Bioorg. Med. Chem. Lett., 27:551-556, 2017; PubMed: 27998678; DOI: 10.1016/j.bmcl.2016.12.019

Experimental method

X-RAY DIFFRACTION (1.9 Å)