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Literature summary for 3.5.3.1 extracted from

  • Golebiowski, A.; Paul Beckett, R.; Van Zandt, M.; Ji, M.K.; Whitehouse, D.; Ryder, T.R.; Jagdmann, E.; Andreoli, M.; Mazur, A.; Padmanilayam, M.; Cousido-Siah, A.; Mitschler, A.; Ruiz, F.X.; Podjarny, A.; Schroeter, H.
    2-Substituted-2-amino-6-boronohexanoic acids as arginase inhibitors (2013), Bioorg. Med. Chem. Lett., 23, 2027-2030.
    View publication on PubMed

Crystallization (Commentary)

Crystallization (Comment) Organism
in complex with inhibitors, vapor diffusion method, using 100 mM malonic acid, imidazol, boric system pH 5, and 25% or 30% (w/v) polyethylene glycol 1500 for aginase I or II, respectively Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
2-(aminomethyl)-6-borononorleucine
-
Homo sapiens
2-amino-6-borono-2-(difluoromethyl)-hexanoic acid
-
Homo sapiens
2-amino-6-borono-2-butylhexanoic acid
-
Homo sapiens
2-amino-6-borono-2-methyl-hexanoic acid
-
Homo sapiens
2-amino-6-boronohexanoic acid
-
Homo sapiens
2-[(benzylamino)methyl]-6-borononorleucine
-
Homo sapiens
6-borono-2-(2-hydroxyethyl)norleucine
-
Homo sapiens
6-borono-2-(3-methoxypropyl)norleucine
-
Homo sapiens
6-borono-2-(hydroxymethyl)norleucine
-
Homo sapiens
6-borono-2-ethylnorleucine
-
Homo sapiens
6-borono-2-methylnorleucine
-
Homo sapiens
6-borono-2-propan-2-ylnorleucine
-
Homo sapiens
6-borono-2-[2-(4-hydroxypiperidin-1-yl)ethyl]norleucine
-
Homo sapiens
6-borono-2-[2-(diethylamino)ethyl]norleucine
-
Homo sapiens
6-borono-2-[2-(morpholin-4-yl)ethyl]norleucine
-
Homo sapiens
6-borono-2-[2-(pyrrolidin-1-yl)ethyl]norleucine
-
Homo sapiens
alpha-(4-boronobutyl)histidine
-
Homo sapiens
alpha-(4-boronobutyl)phenylalanine
-
Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
mitochondrion
-
Homo sapiens 5739
-

Metals/Ions

Metals/Ions Comment Organism Structure
Mn2+ contains Mn2+ Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
L-arginine + H2O Homo sapiens
-
L-ornithine + urea
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens P78540
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
L-arginine + H2O
-
Homo sapiens L-ornithine + urea
-
?

Synonyms

Synonyms Comment Organism
Arg II
-
Homo sapiens
arginase II
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00032
-
arginase I, at pH 7.4 and 37°C Homo sapiens 6-borono-2-[2-(pyrrolidin-1-yl)ethyl]norleucine
0.00037
-
arginase I, at pH 7.4 and 37°C Homo sapiens 6-borono-2-[2-(4-hydroxypiperidin-1-yl)ethyl]norleucine
0.00052
-
arginase I, at pH 7.4 and 37°C Homo sapiens 6-borono-2-[2-(diethylamino)ethyl]norleucine
0.00062
-
arginase II, at pH 7.4 and 37°C Homo sapiens 6-borono-2-[2-(pyrrolidin-1-yl)ethyl]norleucine
0.000934
-
arginase II, at pH 7.4 and 37°C Homo sapiens 6-borono-2-[2-(diethylamino)ethyl]norleucine
0.00098
-
arginase II, at pH 7.4 and 37°C Homo sapiens 6-borono-2-[2-(4-hydroxypiperidin-1-yl)ethyl]norleucine
0.00135
-
arginase II, at pH 7.4 and 37°C Homo sapiens 2-(aminomethyl)-6-borononorleucine
0.00145
-
arginase I, at pH 7.4 and 37°C Homo sapiens 2-amino-6-boronohexanoic acid
0.00192
-
arginase II, at pH 7.4 and 37°C Homo sapiens 2-amino-6-boronohexanoic acid
0.00207
-
arginase I, at pH 7.4 and 37°C Homo sapiens 2-(aminomethyl)-6-borononorleucine
0.00225
-
arginase I, at pH 7.4 and 37°C Homo sapiens 6-borono-2-(hydroxymethyl)norleucine
0.00228
-
arginase I, at pH 7.4 and 37°C Homo sapiens alpha-(4-boronobutyl)histidine
0.00326
-
arginase I, at pH 7.4 and 37°C Homo sapiens 2-[(benzylamino)methyl]-6-borononorleucine
0.0034
-
arginase I, at pH 7.4 and 37°C Homo sapiens 6-borono-2-methylnorleucine
0.00372
-
arginase II, at pH 7.4 and 37°C Homo sapiens alpha-(4-boronobutyl)histidine
0.00402
-
arginase II, at pH 7.4 and 37°C Homo sapiens 6-borono-2-[2-(morpholin-4-yl)ethyl]norleucine
0.0041
-
arginase I, at pH 7.4 and 37°C Homo sapiens 6-borono-2-ethylnorleucine
0.00428
-
arginase II, at pH 7.4 and 37°C Homo sapiens 6-borono-2-(hydroxymethyl)norleucine
0.0045
-
arginase II, at pH 7.4 and 37°C Homo sapiens 2-amino-6-borono-2-butylhexanoic acid
0.0046
-
arginase II, at pH 7.4 and 37°C Homo sapiens 6-borono-2-ethylnorleucine
0.00512
-
arginase I, at pH 7.4 and 37°C Homo sapiens 6-borono-2-(3-methoxypropyl)norleucine
0.00538
-
arginase I, at pH 7.4 and 37°C Homo sapiens 6-borono-2-[2-(morpholin-4-yl)ethyl]norleucine
0.0057
-
arginase II, at pH 7.4 and 37°C Homo sapiens 6-borono-2-methylnorleucine
0.00598
-
arginase II, at pH 7.4 and 37°C Homo sapiens 2-[(benzylamino)methyl]-6-borononorleucine
0.00644
-
arginase II, at pH 7.4 and 37°C Homo sapiens 6-borono-2-(3-methoxypropyl)norleucine
0.0105
-
arginase I, at pH 7.4 and 37°C Homo sapiens alpha-(4-boronobutyl)phenylalanine
0.01124
-
arginase I, at pH 7.4 and 37°C Homo sapiens 6-borono-2-propan-2-ylnorleucine
0.0155
-
arginase II, at pH 7.4 and 37°C Homo sapiens 6-borono-2-propan-2-ylnorleucine
0.017
-
arginase II, at pH 7.4 and 37°C Homo sapiens alpha-(4-boronobutyl)phenylalanine
0.019
-
arginase I, at pH 7.4 and 37°C Homo sapiens 6-borono-2-(2-hydroxyethyl)norleucine
0.057
-
arginase II, at pH 7.4 and 37°C Homo sapiens 6-borono-2-(2-hydroxyethyl)norleucine