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Literature summary for 3.4.24.79 extracted from

  • Mikkelsen, J.H.; Gyrup, C.; Kristensen, P.; Overgaard, M.T.; Poulsen, C.B.; Laursen, L.S.; Oxvig, C.
    Selective inhibition of the proteolytic activity of pregnancy-associated plasma protein-A by targeting substrate exosite binding (2008), J. Biol. Chem., 283, 16772-16780.
    View publication on PubMed
Search for more literature for 3.4.24.79

Cloned(Commentary)

Cloned (Comment) Organism
expression of His-tagged wild-type and mutant chimeric PAPP-A and PAPP-A2 in HEK-293T cells Homo sapiens

Protein Variants

Protein Variants Comment Organism
E483A a proteolytically inactive PAPP-A mutant Homo sapiens
additional information construction of chimeras between PAPP-A and PAPP-A2 of human and murine sequences, overview Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
additional information monoclonal phage-derived scFv antibodies selectively inhibit the cleavage of IGFBP-4 by PAPP-A, none of the antibodies inhibit the homologous proteinase PAPP-A2, which allowed mapping of antibody binding by means of chimeras between PAPP-A and PAPP-A2 to the C-terminal Lin12-Notch repeat module, separated from the proteolytic domain by almost 1000 amino acids, the LNR module requires bound calcium for antibody binding, selective inhibition of IGFBP-4 cleavage by interference with exosite binding, binding site mapping, overview Homo sapiens
PAC1 specific monoclonal antibody inhibiting PAPP-A activity against IGFBP-4, only slight inhibition of IGFBP-5 proteolysis Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Ca2+ the LNR module reversibly binds a calcium ion and that bound calcium is required for antibody binding Homo sapiens
Zn2+ zinc metalloproteinase Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
IGF-binding protein-4 + H2O Homo sapiens i.e. IGFBP-4 ?
-
 ?
IGF-binding protein-5 + H2O Homo sapiens i.e. IGFBP-5 ?
-
 ?
additional information Homo sapiens inhibition of IGF signaling is relevant in human disease, and several drugs in development target the IGF receptor, overview ?
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
 isozymes PAPP-A and PAPP-A2
-

Purification (Commentary)

Purification (Comment) Organism
recombinant His-tagged wild-type and mutant chimeric PAPP-A and PAPP-A2 from HEK-293T cells Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
IGF-binding protein-4 + H2O i.e. IGFBP-4 Homo sapiens ?
-
 ?
IGF-binding protein-4 + H2O i.e. IGFBP-4, PAPP-A cleaves IGFBP-4 at a single site in the central domain causing the release of bioactive IGF Homo sapiens ?
-
 ?
IGF-binding protein-5 + H2O i.e. IGFBP-5 Homo sapiens ?
-
 ?
IGF-binding protein-5 + H2O i.e. IGFBP-5, PAPP-A cleaves IGFBP-5 at a single site in the central domain causing the release of bioactive IGF Homo sapiens ?
-
 ?
additional information inhibition of IGF signaling is relevant in human disease, and several drugs in development target the IGF receptor, overview Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
PAPP-A
-
 Homo sapiens
PAPP-A2
-
 Homo sapiens
pregnancy-associated plasma protein-A
-
 Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
 assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5
-
 assay at Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0000012
-
 PAC1 antibody pH 7.5, 37°C, inhibition of PAPP-A Homo sapiens