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Literature summary extracted from

  • Xue, Y.; Ha, Y.
    The catalytic mechanism of rhomboid protease GlpG probed by 3,4-dichloroisocoumarin and diisopropyl fluorophosphonate (2012), J. Biol. Chem., 287, 3099-3107.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

EC Number Cloned (Comment) Organism
3.4.21.105
-
Escherichia coli

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
3.4.21.105 in complex with inhibitors 3,4-dichloroisocoumarin and diisopropyl fluorophosphonate, to 2.3 A resolution. Enzyme forms a covalent adduct with diisopropyl fluorophosphonate, which mimics the oxyanion-containing tetrahedral intermediate of the hydrolytic reaction. The oxyanion is stabilized by the main chain amide of residue Ser201 and by the side chains of His150 and Asn154. The phosphorylation of the catalytic Ser201 weakens its interaction with His254, causing the catalytic histidine to rotate away from the serine and accompanied by further rearrangement of the side chains of Tyr205 and Trp236 within the substrate-binding groove and by opening of the L5 cap and movement of transmembrane helix S5 toward S6 in a direction different from that predicted by the lateral gating model Escherichia coli
3.4.21.105 rhomboid protease GlpG in complex with 3,4-dichloroisocoumarin and diisopropyl fluorophosphonate, sitting drop vapor diffusion method, using 100 mM Bis-Tris propane (pH 7.0), and 3 M NaCl Escherichia coli

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.21.105 3,4-dichloroisocoumarin mechanism-based inhibitor Escherichia coli
3.4.21.105 diisopropyl fluorophosphonate irreversible inhibition; mechansim-based inhibitor Escherichia coli

Organism

EC Number Organism UniProt Comment Textmining
3.4.21.105 Escherichia coli
-
-
-
3.4.21.105 Escherichia coli P09391
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
3.4.21.105
-
Escherichia coli

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.21.105 3,4-dichloroisocoumarin + H2O a significant portion of the inhibitor 3,4-dichloroisocoumarin bound to GlpG is enzymatically turned over Escherichia coli ?
-
?
3.4.21.105 BODIPY FL casein + H2O
-
Escherichia coli ?
-
?

Synonyms

EC Number Synonyms Comment Organism
3.4.21.105 GlpG
-
Escherichia coli
3.4.21.105 rhomboid protease
-
Escherichia coli