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Literature summary extracted from

  • Kawatani, M.; Okumura, H.; Honda, K.; Kanoh, N.; Muroi, M.; Dohmae, N.; Takami, M.; Kitagawa, M.; Futamura, Y.; Imoto, M.; Osada, H.
    he identification of an osteoclastogenesis inhibitor through the inhibition of glyoxalase I (2008), Proc. Natl. Acad. Sci. USA, 105, 11691-11696.
    View publication on PubMedView publication on EuropePMC

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
4.4.1.5 complex with methyl-gerfelin, structural resolution at 1.7 A. The model contains one protein homodimer, two zinc ions, and two methyl-gerfelin molecules in an asymmetric unit. The two active sites of the homodimer are located at the dimer interface and are characterized by a zinc-ion-binding site, a glutathione-binding site, and a hydrophobic pocket. In the active site, the zinc ion is on octahedral coordination and is bound by Gln34, Glu100, His127, Glu173 and two hydroxyl groups of methyl-gerfelin directly Mus musculus

Inhibitors

EC Number Inhibitors Comment Organism Structure
4.4.1.5 gerfelin inhibitor of osteoclast differentiation, osteoclastogenesis, inhibition kinetics, competitive inhibition, pH 7.0, 30°C Mus musculus
4.4.1.5 methyl gerfelin inhibitor of osteoclast differentiation, osteoclastogenesis, inhibition kinetics from 0.5 to 2 microM, competitive inhibition, pH 7.0, 30°C Mus musculus
4.4.1.5 S-p-bromobenzylglutathione cyclopentyl diester GLO1 inhibitor, inhibiting osteoclastogenesis, inhibition kinetics from 0.03 to 3 microM, dose-dependently inhibited, strongest inhibition at 3 microM, pH 7.0, 30°C Mus musculus

Molecular Weight [Da]

EC Number Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
4.4.1.5 20810
-
 2 * 20810, calculated from sequence, MALDI-TOF mass spectrometry, SDS-PAGE Mus musculus
4.4.1.5 41620
-
 calculated from sequence, MALDI-TOF mass spectrometry Mus musculus

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
4.4.1.5 additional information Mus musculus GLO1 is required for osteoclastogenesis ?
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
4.4.1.5 Mus musculus Q9CPU0
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
4.4.1.5 osteoclast progenitor cell
-
 Mus musculus
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
4.4.1.5 methylglyoxal + glutathione the hemiacetal of methylglyoxal + glutathione is used as substrate, pH 7.0, 30°C Mus musculus S-((R)-lactoyl)glutathione the formation is measured by monitoring the increase of absorbance at 240 nm ?
4.4.1.5 additional information GLO1 is required for osteoclastogenesis Mus musculus ?
-
 ?

Subunits

EC Number Subunits Comment Organism
4.4.1.5 homodimer 2 * 20810, calculated from sequence, MALDI-TOF mass spectrometry, SDS-PAGE Mus musculus

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
4.4.1.5 0.00015
-
 gerfelin inhibitor of osteoclast differentiation, osteoclastogenesis, inhibition kinetics, competitive inhibition, pH 7.0, 30°C Mus musculus
4.4.1.5 0.00023
-
 methyl gerfelin inhibitor of osteoclast differentiation, osteoclastogenesis, inhibition kinetics from 0.5 to 2 microM, competitive inhibition, pH 7.0, 30°C Mus musculus