Crystallization (Comment) | Organism |
---|---|
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 | Comment | Organism | Structure |
---|---|---|---|
gerfelin | inhibitor of osteoclast differentiation, osteoclastogenesis, inhibition kinetics, competitive inhibition, pH 7.0, 30°C | Mus musculus | |
methyl gerfelin | inhibitor of osteoclast differentiation, osteoclastogenesis, inhibition kinetics from 0.5 to 2 microM, competitive inhibition, pH 7.0, 30°C | Mus musculus | |
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] | Molecular Weight Maximum [Da] | Comment | Organism |
---|---|---|---|
20810 | - |
2 * 20810, calculated from sequence, MALDI-TOF mass spectrometry, SDS-PAGE | Mus musculus |
41620 | - |
calculated from sequence, MALDI-TOF mass spectrometry | Mus musculus |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
additional information | Mus musculus | GLO1 is required for osteoclastogenesis | ? | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Mus musculus | Q9CPU0 | - |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
osteoclast progenitor cell | - |
Mus musculus | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
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 | ? | |
additional information | GLO1 is required for osteoclastogenesis | Mus musculus | ? | - |
? |
Subunits | Comment | Organism |
---|---|---|
homodimer | 2 * 20810, calculated from sequence, MALDI-TOF mass spectrometry, SDS-PAGE | Mus musculus |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.00015 | - |
gerfelin | inhibitor of osteoclast differentiation, osteoclastogenesis, inhibition kinetics, competitive inhibition, pH 7.0, 30°C | Mus musculus | |
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 |