Literature summary for 3.4.23.B2 extracted from
Konvalinka, J.; Kraeusslich, H.
Simian immunodeficiency virus retropepsin (2004), Handbook of Proteolytic Enzymes (Barrett, J. ; Rawlings, N. D. ; Woessner, J. F. , eds. ), 1, 158-160.
No PubMed abstract available
Application
Application |
Comment |
Organism |
additional information |
SIV retropepsin can serve as an inhibitor-resistant retrovirus variant model of HIV-1 retropepsin |
Simian immunodeficiency virus |
Cloned(Commentary)
Cloned (Comment) |
Organism |
expression in Escherichia coli, expression as N-terminally capped, biotin-labeled precursor |
Simian immunodeficiency virus |
Crystallization (Commentary)
Crystallization (Comment) |
Organism |
crystal structure determination and analysis of free enzyme and enzyme-inhibitor complexes, e.g. with 1,2-epoxy-3-(4-nitrophenoxy)propane at 2.4 A resolution, or with SKF107457 at 2.5 A resolution |
Simian immunodeficiency virus |
Protein Variants
Protein Variants |
Comment |
Organism |
S4H |
site-directed mutagenesis, the mutation of the major autodegeneration site stabilizes the enzyme without significantly affecting the kinetic parameters |
Simian immunodeficiency virus |
Inhibitors
Inhibitors |
Comment |
Organism |
Structure |
1,2-epoxy-3-(4-nitrophenoxy)propane |
specific inhibition |
Simian immunodeficiency virus |
|
additional information |
several HIV-1 peptomimetic inhibitors also inhibit the SIV retropepsin, inhibitor binding structure |
Simian immunodeficiency virus |
|
pepstatin A |
specific inhibition |
Simian immunodeficiency virus |
|
SKF107457 |
a hydroxyethylene inhibitor |
Simian immunodeficiency virus |
|
Organism
Organism |
UniProt |
Comment |
Textmining |
Simian immunodeficiency virus |
- |
SIV, a lenti-retrovirus, derived from different monkey species, the virus is pathogenic not in all of the species, overview |
- |
Posttranslational Modification
Posttranslational Modification |
Comment |
Organism |
proteolytic modification |
the retropepsin is expressed as part of a larger polyprotein precursor, which it cleaves into functional proteins, the major autodegradation site of the enzyme is Phe3-Ser4 |
Simian immunodeficiency virus |
Purification (Commentary)
Purification (Comment) |
Organism |
recombinant enzyme from Escherichia coli by ammonium sulfate fractionation, and ion exchange or affinity chromatography on a pepstatin A resin, recombinant N-terminally capped, biotin-labeled precursor by streptavidin affinity chromatography, the tag is autocatalytically cleaved after refolding of the enzyme |
Simian immunodeficiency virus |
Reaction
Reaction |
Comment |
Organism |
Reaction ID |
The enzyme may have a wide substrate specificity. Good cleavage of the peptide bonds Met-Met and Tyr-Pro. Cleavage is also observed at Phe-Pro, Phe-Leu, Leu-Phe, Leu-Ala, Glu-Ala and Tyr-Ala |
aspartic acid protease, structure-function relation ship, the active site conformation changes from open to closed upon substrate binding, overview |
Simian immunodeficiency virus |
|
Renatured (Commentary)
Renatured (Comment) |
Organism |
refolding from recombinant cytoplasmic inclusion bodies, refolding of recombinant N-terminally capped, biotin-labeled precursor |
Simian immunodeficiency virus |
Substrates and Products (Substrate)
Substrates |
Comment Substrates |
Organism |
Products |
Comment (Products) |
Rev. |
Reac. |
SIV Gag precursor protein + H2O |
determination of cleavage sites and substrate specificity |
Simian immunodeficiency virus |
? |
- |
? |
|
Subunits
Subunits |
Comment |
Organism |
dimer |
the active enzyme is a homodimer, each subunit contains an Asn-Thr-Gly aspartic acid protease motif |
Simian immunodeficiency virus |
Synonyms
Synonyms |
Comment |
Organism |
More |
the enzyme belongs to the A2 peptidase family |
Simian immunodeficiency virus |
simian immunodeficiency virus retropepsin |
- |
Simian immunodeficiency virus |
SIV retropepsin |
- |
Simian immunodeficiency virus |
Ki Value [mM]
Ki Value [mM] |
Ki Value maximum [mM] |
Inhibitor |
Comment |
Organism |
Structure |
additional information |
- |
additional information |
- |
Simian immunodeficiency virus |
|