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Literature summary for 3.4.11.18 extracted from

  • Arico-Muendel, C.C.; Benjamin, D.R.; Caiazzo, T.M.; Centrella, P.A.; Contonio, B.D.; Cook, C.M.; Doyle, E.G.; Hannig, G.; Labenski, M.T.; Searle, L.L.; Lind, K.; Morgan, B.A.; Olson, G.; Paradise, C.L.; Self, C.; Skinner, S.R.; Sluboski, B.; Svendsen, J.L.; Thompson, C.D.; Westlin, W.; White, K.F.
    Carbamate analogues of fumagillin as potent, targeted inhibitors of methionine aminopeptidase-2 (2009), J. Med. Chem., 52, 8047-8056.
    View publication on PubMed
Search for more literature for 3.4.11.18

Inhibitors

Inhibitors Comment Organism Structure
(2E,4E,6E,8E)-10-((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)-10-oxodeca-2,4,6,8-tetraenoic acid
-
 Homo sapiens
(3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-ol
-
 Homo sapiens
(3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl (2R)-3-methyl-1-(2-(1-methylpyrrolidin-2-yl)ethylamino)-1-oxobutan-2-ylcarbamate
-
 Homo sapiens
(3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl (R)-1-amino-3-methyl-1-oxobutan-2-yl carbamate i.e. PPI-2458, advanced into phase I clinical studies in non-Hodgkin's lymphoma and solid cancers, overview Homo sapiens
(3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl (R)-1-amino-3-methyl-1-oxobutan-2-ylcarbamate
-
 Homo sapiens
(3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl (R)-1-hydroxy-3-methylbutan-2-ylcarbamate
-
 Homo sapiens
(3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl (R)-3-methyl-1-(morpholinoamino)-1-oxobutan-2-ylcarbamate
-
 Homo sapiens
(3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl (R)-3-methyl-1-oxo-1-(2-(pyrrolidin-1-yl)ethylamino)butan-2-ylcarbamate
-
 Homo sapiens
(3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl 1-amino-2-methyl-1-oxopropan-2-ylcarbamate
-
 Homo sapiens
(3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl 1-carbamoylcyclopentylcarbamate
-
 Homo sapiens
(3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl 2-(1-methylpyrrolidin-2-yl)ethylcarbamate
-
 Homo sapiens
(3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl 2-(pyrrolidin-1-yl)ethylcarbamate
-
 Homo sapiens
(3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl isopropylcarbamate
-
 Homo sapiens
(3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl morpholinocarbamate
-
 Homo sapiens
(3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl tert-butylcarbamate
-
 Homo sapiens
(3R,5S,6R)-5-methoxy-4-[(3R)-2-methyl-3-(3-methylbut-2-en-1-yl)oxiran-2-yl]-1-oxaspiro[2.5]oct-6-yl (chloroacetyl)carbamate
-
 Homo sapiens
(R)-methyl 2-(((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)carbonylamino)-2-phenylacetate
-
 Homo sapiens
(R)-methyl 2-(((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)carbonylamino)-3-methylbutanoate
-
 Homo sapiens
(R)-methyl 2-(((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)carbonylamino)-4-methylpentanoate
-
 Homo sapiens
(S)-methyl 2-(((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)-carbonylamino)-3-methylbutanoate
-
 Homo sapiens
1-(((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)carbonyl)-piperidine-4-carboxylic acid
-
 Homo sapiens
2-(2-(((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)-carbonylamino)ethyl)-1,1-dimethylpyrrolidinium iodide
-
 Homo sapiens
3-(((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)carbonylamino)-N,N,N-trimethylpropan-1-aminium iodide
-
 Homo sapiens
3-((R)-2-(((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)-carbonylamino)-3-methylbutanamido)benzoic acid
-
 Homo sapiens
4-((((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)carbonylamino)methyl)benzoic acid
-
 Homo sapiens
fumagillin
-
 Homo sapiens
fumagillol i.e. (3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-ol Homo sapiens
additional information inhibitor synthesis, pharmacokinetics, and molecular modelling Homo sapiens
ovalicin
-
 Homo sapiens
TNP-470 AGM-1470 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
umbilical vein endothelial cell
-
 Homo sapiens
-

Synonyms

Synonyms Comment Organism
MetAP-2
-
 Homo sapiens
MetAP2
-
 Homo sapiens
methionine aminopeptidase-2
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000000018
-
 in HUVEC Homo sapiens (S)-methyl 2-(((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)-carbonylamino)-3-methylbutanoate
0.000000036
-
 in HUVEC Homo sapiens (R)-methyl 2-(((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)carbonylamino)-2-phenylacetate
0.000000038
-
 in HUVEC Homo sapiens (R)-methyl 2-(((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)carbonylamino)-4-methylpentanoate
0.00000004
-
 in HUVEC Homo sapiens (R)-methyl 2-(((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)carbonylamino)-3-methylbutanoate
0.00000006
-
 in HUVEC Homo sapiens (3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl isopropylcarbamate
0.000000095
-
 in HUVEC Homo sapiens (3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl (R)-1-amino-3-methyl-1-oxobutan-2-ylcarbamate
0.0000001
-
 in HUVEC Homo sapiens (3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl 2-(pyrrolidin-1-yl)ethylcarbamate
0.0000002
-
 above, in HUVEC Homo sapiens (3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl 2-(1-methylpyrrolidin-2-yl)ethylcarbamate
0.00000025
-
 in HUVEC Homo sapiens (3R,5S,6R)-5-methoxy-4-[(3R)-2-methyl-3-(3-methylbut-2-en-1-yl)oxiran-2-yl]-1-oxaspiro[2.5]oct-6-yl (chloroacetyl)carbamate
0.0000006
-
 above, in HUVEC Homo sapiens (3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl (2R)-3-methyl-1-(2-(1-methylpyrrolidin-2-yl)ethylamino)-1-oxobutan-2-ylcarbamate
0.0000006
-
 in HUVEC Homo sapiens (3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl (R)-3-methyl-1-oxo-1-(2-(pyrrolidin-1-yl)ethylamino)butan-2-ylcarbamate
0.0000007
-
 in HUVEC Homo sapiens (3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl 1-carbamoylcyclopentylcarbamate
0.0000007
-
 in HUVEC Homo sapiens (3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl morpholinocarbamate
0.0000007
-
 in HUVEC Homo sapiens 4-((((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)carbonylamino)methyl)benzoic acid
0.0000011
-
 in HUVEC Homo sapiens (3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl tert-butylcarbamate
0.0000013
-
 in HUVEC Homo sapiens 1-(((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)carbonyl)-piperidine-4-carboxylic acid
0.0000017
-
 in HUVEC Homo sapiens (3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl 1-amino-2-methyl-1-oxopropan-2-ylcarbamate
0.0000017
-
 in HUVEC Homo sapiens (3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl (R)-3-methyl-1-(morpholinoamino)-1-oxobutan-2-ylcarbamate
0.000015
-
 in HUVEC Homo sapiens 3-((R)-2-(((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)-carbonylamino)-3-methylbutanamido)benzoic acid
0.0001
-
 in HUVEC Homo sapiens 3-(((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)carbonylamino)-N,N,N-trimethylpropan-1-aminium iodide
0.0001
-
 in HUVEC Homo sapiens 2-(2-(((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)-carbonylamino)ethyl)-1,1-dimethylpyrrolidinium iodide