Literature summary for 3.4.11.18 extracted from

Alvarado, J.J.; Nemkal, A.; Sauder, J.M.; Russell, M.; Akiyoshi, D.E.; Shi, W.; Almo, S.C.; Weiss, L.M.
Structure of a microsporidian methionine aminopeptidase type 2 complexed with fumagillin and TNP-470 (2009), Mol. Biochem. Parasitol., 168, 158-167.

Search for more literature for 3.4.11.18

Cloned(Commentary)

Cloned (Comment)	Organism
expression of MetAP2 using the baculovirus transfection system	Encephalitozoon cuniculi

Crystallization (Commentary)

Crystallization (Comment)	Organism
purified recombinant MetAP2 with and without the bound inhibitors fumagillin and TNP-470, sitting drop vapor diffusion at 20°C, mixing of 2 mg/ml protein, in 10 mM HEPES, 150 mM NaCl, 10% glycerol, 5 mM DTT, pH 7.5, with 30% w/v PEG 4000, 0.2 M ammonium sulfate, for inhibitor bound enzyme crystals co-cyrstallization with 0.5 mM inhibitor in 27% PEG 4000, 0.2 M ammonium sulfate, ten days, X-ray diffraction structure determination and analysis at 2.18-2.89 A resolution, molecular replacement	Encephalitozoon cuniculi

Crystallization (Comment)

Organism

purified recombinant MetAP2 with and without the bound inhibitors fumagillin and TNP-470, sitting drop vapor diffusion at 20°C, mixing of 2 mg/ml protein, in 10 mM HEPES, 150 mM NaCl, 10% glycerol, 5 mM DTT, pH 7.5, with 30% w/v PEG 4000, 0.2 M ammonium sulfate, for inhibitor bound enzyme crystals co-cyrstallization with 0.5 mM inhibitor in 27% PEG 4000, 0.2 M ammonium sulfate, ten days, X-ray diffraction structure determination and analysis at 2.18-2.89 A resolution, molecular replacement

Encephalitozoon cuniculi

Protein Variants

Protein Variants	Comment	Organism
H382Y	the single site mutation in the S1 subsite of human MetAP2b results in inhibitor resistance	Homo sapiens
Y444C	the single site mutation in the S1 subsite of human MetAP2b results in inhibitor resistance	Homo sapiens

Inhibitors

Inhibitors	Comment	Organism
fumagillin	binding structure, overview	Encephalitozoon cuniculi
fumagillin	binding structure, overview. Fumagillin and its analogues show inhibitory activity in vitro and in animal models of microsporidiosis and human infections due to Enterocytozoon bieneusi	Enterocytozoon bieneusi
fumagillin	binding structure, specificity determinants lie in the S1 hydrophobic methionine binding subsite, overview	Homo sapiens
TNP-470	binding structure, overview	Encephalitozoon cuniculi
TNP-470	binding structure, overview	Enterocytozoon bieneusi
TNP-470	binding structure, specificity determinants lie in the S1 hydrophobic methionine binding subsite, overview	Homo sapiens

KM Value [mM]

KM Value [mM]	KM Value Maximum [mM]	Substrate	Comment	Organism	Structure
1.95	-	Met-Ala-Ser	pH 8.5, 37°C, recombinant MetAP2	Encephalitozoon cuniculi
2.08	-	Met-Ala-Ser	pH 8.5, 37°C	Homo sapiens

Metals/Ions

Metals/Ions	Comment	Organism
Co2+	activates	Homo sapiens
Co2+	activates	Encephalitozoon cuniculi
Fe2+	activates slightly	Encephalitozoon cuniculi
Mn2+	activates	Encephalitozoon cuniculi

Organism

Organism	UniProt	Comment	Textmining
Encephalitozoon cuniculi	-	-	-
Enterocytozoon bieneusi	B7XJ30	-	-
Enterocytozoon bieneusi H348	B7XJ30	-	-
Homo sapiens	-	-	-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg]	Specific Activity Maximum [µmol/min/mg]	Comment	Organism
2.9	-	in presence of Fe2+, purified recombinant MetAP2	Encephalitozoon cuniculi
7.9	-	in presence of Mn2+, purified recombinant MetAP2	Encephalitozoon cuniculi
8.3	-	-	Homo sapiens
11.7	-	in presence of Co2+, purified recombinant MetAP2	Encephalitozoon cuniculi

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.
Met-Ala-Ser + H2O	-	Homo sapiens	Met + Ala-Ser	-	?
Met-Ala-Ser + H2O	-	Encephalitozoon cuniculi	Met + Ala-Ser	-	?
additional information	active site structure and substrate binding, overview	Encephalitozoon cuniculi	?	-	?
additional information	active site structure and substrate binding, overview	Enterocytozoon bieneusi	?	-	?
additional information	active site strutcure and substrate binding, overview	Homo sapiens	?	-	?
additional information	active site structure and substrate binding, overview	Enterocytozoon bieneusi H348	?	-	?

Subunits

Subunits	Comment	Organism
More	EbMetAP2 structure analysis by homology modelling using the structure of EcMetAP2 from Enterocytozoon cuniculi	Enterocytozoon bieneusi
More	sequence comparisons, e.g. with the human enzyme structure, PDB ID 1YW9, overview	Encephalitozoon cuniculi
More	sequence comparisons, overview	Homo sapiens

Synonyms

Synonyms	Comment	Organism
MetAP2	-	Homo sapiens
MetAP2	-	Encephalitozoon cuniculi
MetAP2	-	Enterocytozoon bieneusi
methionine aminopeptidase type 2	-	Homo sapiens
methionine aminopeptidase type 2	-	Encephalitozoon cuniculi
methionine aminopeptidase type 2	-	Enterocytozoon bieneusi
More	EcMetAP2 as a member of the MetAP2c family	Encephalitozoon cuniculi

Temperature Optimum [°C]

Temperature Optimum [°C]	Temperature Optimum Maximum [°C]	Comment	Organism
37	-	assay at	Homo sapiens
37	-	assay at	Encephalitozoon cuniculi

pH Optimum

pH Optimum Minimum	pH Optimum Maximum	Comment	Organism
7.5	-	-	Homo sapiens
8.5	-	-	Encephalitozoon cuniculi

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
10.6	-	pH 8.5, 37°C, recombinant MetAP2	Encephalitozoon cuniculi	TNP-470
11.1	-	pH 8.5, 37°C, recombinant MetAP2	Encephalitozoon cuniculi	fumagillin