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Literature summary extracted from

  • Singh, P.; LeBeau, A.M.; Lilja, H.; Denmeade, S.R.; Isaacs, J.T.
    Molecular insights into substrate specificity of prostate specific antigen through structural modeling (2009), Proteins, 77, 984-993.
    View publication on PubMedView publication on EuropePMC

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.21.77 CBZ-Ser-Ser-Lys-(4-bromo)Phe-Lys-aldehyde
-
 Homo sapiens
3.4.21.77 Cbz-SSKDL-CHO
-
 Homo sapiens
3.4.21.77 Cbz-SSKLL-CHO
-
 Homo sapiens
3.4.21.77 Cbz-SSKPL-CHO
-
 Homo sapiens
3.4.21.77 Cbz-SSKWL-CHO
-
 Homo sapiens
3.4.21.77 Cbz-SSKYL-CHO
-
 Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
3.4.21.77 0.14
-
 4-morpholinecarbonyl-SRKSQQY-7-amido-4-methylcoumarin in 50 mM Tris buffer, 0.1 M NaCl, pH 7.8 Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
3.4.21.77 Homo sapiens
-
-
-
3.4.21.77 Sus scrofa
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.21.77 4-morpholinecarbonyl-SKLQ-7-amido-4-methylcoumarin + H2O hydrolysis rate is 29.6 pmol/min per 100 pmol of PSA Homo sapiens ?
-
 ?
3.4.21.77 4-morpholinecarbonyl-SRKSQQY-7-amido-4-methylcoumarin + H2O
-
 Homo sapiens ?
-
 ?
3.4.21.77 GSAKLQ + H2O 207.2% relative hydrolysis rate Homo sapiens ?
-
 ?
3.4.21.77 GSSALQ + H2O 43.2% relative hydrolysis rate Homo sapiens ?
-
 ?
3.4.21.77 GSSKLA + H2O 31.5% relative hydrolysis rate Homo sapiens ?
-
 ?
3.4.21.77 GSSKLH + H2O 170.6% relative hydrolysis rate Homo sapiens ?
-
 ?
3.4.21.77 GSSKLQ + H2O 100% relative hydrolysis rate Homo sapiens ?
-
 ?
3.4.21.77 GSSKPQ + H2O 7.2% relative hydrolysis rate Homo sapiens ?
-
 ?
3.4.21.77 GSSKYQ + H2O 256.9% relative hydrolysis rate Homo sapiens ?
-
 ?
3.4.21.77 GSSSLQ + H2O 52.6% relative hydrolysis rate Homo sapiens ?
-
 ?
3.4.21.77 HSSKLQ-7-amido-4-methylcoumarin + H2O hydrolysis rate is 62.7 pmol/min per 100 pmol of PSA Homo sapiens ?
-
 ?
3.4.21.77 additional information no hydrolysis with NH2-Q-amido-4-methyl coumarin, 4-morpholinecarbonyl-LQ-7-amido-4-methylcoumarin and 4-morpholinecarbonyl-KLQ-7-amido-4-methylcoumarin as substrates Homo sapiens ?
-
 ?
3.4.21.77 additional information only P1-4 residues are major determinants of binding affinity and substrate specificity for PSA. The P1 residue binds at the specificity pocket lined by polar residues with the partial hydrophobic side-chains such as Ser217, Thr184, and Tyr219. The P2 residue side-chain is docked against the face of the imidazole ring of the catalytic His41 residue. The P3 residue acts as a lid to the specificity pocket and docks at a location just above the P1 binding site in the specificity pocket. Important role for Glu208 interactions in determining PSA specificity at the P3 residue. The P4 pocket is located in the lower groove area, and mainly formed by His164, Pro165, Gln166, and Trp205 residues Sus scrofa ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.4.21.77 prostate specific antigen
-
 Homo sapiens
3.4.21.77 prostate specific antigen
-
 Sus scrofa
3.4.21.77 PSA
-
 Homo sapiens
3.4.21.77 PSA
-
 Sus scrofa

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.4.21.77 0.00651
-
 Cbz-SSKLL-CHO in 50 mM Tris buffer, 100 mM NaCl, pH 7.8, 10% DMSO Homo sapiens
3.4.21.77 0.01309
-
 Cbz-SSKYL-CHO in 50 mM Tris buffer, 100 mM NaCl, pH 7.8, 10% DMSO Homo sapiens
3.4.21.77 0.1553
-
 Cbz-SSKWL-CHO in 50 mM Tris buffer, 100 mM NaCl, pH 7.8, 10% DMSO Homo sapiens
3.4.21.77 0.5
-
 CBZ-Ser-Ser-Lys-(4-bromo)Phe-Lys-aldehyde in 50 mM Tris buffer, 100 mM NaCl, pH 7.8, 10% DMSO Homo sapiens
3.4.21.77 0.5
-
 Cbz-SSKPL-CHO in 50 mM Tris buffer, 100 mM NaCl, pH 7.8, 10% DMSO Homo sapiens
3.4.21.77 1
-
 Cbz-SSKDL-CHO in 50 mM Tris buffer, 100 mM NaCl, pH 7.8, 10% DMSO Homo sapiens