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Literature summary for 3.4.22.15 extracted from

  • Mihelic, M.; Dobersek, A.; Guncar, G.; Turk, D.
    Inhibitory fragment from the p41 form of invariant chain can regulate activity of cysteine cathepsins in antigen presentation (2008), J. Biol. Chem., 283, 14453-14460.
    View publication on PubMed
Search for more literature for 3.4.22.15

Cloned(Commentary)

Cloned (Comment) Organism
amplification of cDNA by PCR, PCR-products cloned into Pichia pastoris expression vector pPIC9K with His-tag, transformation of Pichia pastoris strain GS115, 4 days of expression Homo sapiens
amplification of cDNA by PCR, PCR-products cloned into Pichia pastoris expression vector pPIC9K with His-tag, transformation of Pichia pastoris strain GS115, 4 days of expression Mus musculus

Crystallization (Commentary)

Crystallization (Comment) Organism
modelling 3D-structure of cathepsin L (PDB entry 1ICF), analysing residues binding the inhibitor p41-fragment, comparing binding sites of different Cathepsins Homo sapiens
modelling 3D-structure of cathepsin L (PDB entry 1ICF), analysing residues binding the inhibitor p41-fragment, comparing binding sites of different Cathepsins Mus musculus
molecular modeling of complex with fragment p41 of major histocompatibility complex class II-associated invariant chain Mus musculus
molecular modeling of complex with fragment p41 of major histocompatibility complex class II-associated invariant chain Homo sapiens

Protein Variants

Protein Variants Comment Organism
G139R 2fold decrease in binding affinity to the inhibitory fragment p41 of major histocompatibility complex class II-associated invariant chain Homo sapiens
G139R KI-value increased compared to wild-type Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
fragment p41 of major histocompatibility complex class II-associated invariant chain inhibitory to human cathepsin V, cathepsin L, cathepsin K, cathepsin F with Ki values in the low nanomolar range. Ki values are sufficiently low to ensure complex formation at physiological concentrations. Regulation of the proteolytic activity of most of the cysteine cathepsins by the p41 fragment is an important and widespread control mechanism of antigen presentation Homo sapiens
fragment p41 of major histocompatibility complex class II-associated invariant chain inhibitory to human cathepsin V, cathepsin L, cathepsin K, cathepsin F with Ki values in the low nanomolar range. Ki values are sufficiently low to ensure complex formation at physiological concentrations. Regulation of the proteolytic activity of most of the cysteine cathepsins by the p41 fragment is an important and widespread control mechanism of antigen presentation Mus musculus
p41-fragment-human 64 residues present in the p41 form of the human major histocompatibility complex II (MHCII)-associated invariant chain Homo sapiens
p41-fragment-human 64 residues present in the p41 form of the human major histocompatibility complex II (MHCII)-associated invariant chain Mus musculus
p41-fragment-mouse 64 residues present in the p41 form of the murine major histocompatibility complex II (MHCII)-associated invariant chain Mus musculus

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Homo sapiens P07711
-
-
Mus musculus
-
-
-
Mus musculus P06797
-
-

Purification (Commentary)

Purification (Comment) Organism
Ni-Sepharose 6 Fast Flow column, eluted with binding buffer containing 500 mM imidazole, activation of immature cathepsin L by dialysis, Sephadex-75 HR column, dialysis, blocked with 10-fold molar excess of methyl-methanethiosulfonate Homo sapiens
Ni-Sepharose 6 Fast Flow column, eluted with binding buffer containing 500 mM imidazole, activation of immature cathepsin L by dialysis, Sephadex-75 HR column, dialysis, blocked with 10-fold molar excess of methyl-methanethiosulfonate Mus musculus

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
benzyloxycarbonyl-Phe-Arg-4-methylcoumarin-7-amide + H2O
-
 Homo sapiens benzyloxycarbonyl-Phe-Arg + 7-amino-4-methylcoumarin
-
 ?
benzyloxycarbonyl-Phe-Arg-4-methylcoumarin-7-amide + H2O
-
 Mus musculus benzyloxycarbonyl-Phe-Arg + 7-amino-4-methylcoumarin
-
 ?
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
-
 Mus musculus benzyloxycarbonyl-Phe-Arg + 7-amino-4-methylcoumarin
-
 ?
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
-
 Homo sapiens benzyloxycarbonyl-Phe-Arg + 7-amino-4-methylcoumarin
-
 ?

Synonyms

Synonyms Comment Organism
cathepsin L
-
 Homo sapiens
cathepsin L
-
 Mus musculus

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00000000149
-
 p41-fragment-human substrate: benzyloxycarbonyl-Phe-Arg-4-methylcoumarin-7-amide, production rate of 7-amino-4-methylcoumarin measured, excitation and emission wavelengths of 370 and 460 nm, pseudo first order reaction conditions (inhibitor concentration at least 10-fold higher than enzyme concentration) Mus musculus
0.00000000552
-
 p41-fragment-human wild-type, substrate: benzyloxycarbonyl-Phe-Arg-4-methylcoumarin-7-amide, production rate of 7-amino-4-methylcoumarin measured, excitation and emission wavelengths of 370 and 460 nm, pseudo first order reaction conditions (inhibitor concentration at least 10-fold higher than enzyme concentration) Homo sapiens
0.0000000072
-
 fragment p41 of major histocompatibility complex class II-associated invariant chain pH 6.0, 25°C Mus musculus
0.00000000722
-
 p41-fragment-mouse substrate: benzyloxycarbonyl-Phe-Arg-4-methylcoumarin-7-amide, production rate of 7-amino-4-methylcoumarin measured, excitation and emission wavelengths of 370 and 460 nm, pseudo first order reaction conditions (inhibitor concentration at least 10-fold higher than enzyme concentration) Mus musculus
0.0000000101
-
 fragment p41 of major histocompatibility complex class II-associated invariant chain pH 6.0, 25°C Homo sapiens
0.0000000101
-
 p41-fragment-human G139R mutant, substrate: benzyloxycarbonyl-Phe-Arg-4-methylcoumarin-7-amide, production rate of 7-amino-4-methylcoumarin measured, excitation and emission wavelengths of 370 and 460 nm, pseudo first order reaction conditions (inhibitor concentration at least 10-fold higher than enzyme concentration) Homo sapiens