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Literature summary for 3.4.21.77 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
Search for more literature for 3.4.21.77

Inhibitors

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

KM Value [mM]

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

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Sus scrofa
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
4-morpholinecarbonyl-SKLQ-7-amido-4-methylcoumarin + H2O hydrolysis rate is 29.6 pmol/min per 100 pmol of PSA Homo sapiens ?
-
 ?
4-morpholinecarbonyl-SRKSQQY-7-amido-4-methylcoumarin + H2O
-
 Homo sapiens ?
-
 ?
GSAKLQ + H2O 207.2% relative hydrolysis rate Homo sapiens ?
-
 ?
GSSALQ + H2O 43.2% relative hydrolysis rate Homo sapiens ?
-
 ?
GSSKLA + H2O 31.5% relative hydrolysis rate Homo sapiens ?
-
 ?
GSSKLH + H2O 170.6% relative hydrolysis rate Homo sapiens ?
-
 ?
GSSKLQ + H2O 100% relative hydrolysis rate Homo sapiens ?
-
 ?
GSSKPQ + H2O 7.2% relative hydrolysis rate Homo sapiens ?
-
 ?
GSSKYQ + H2O 256.9% relative hydrolysis rate Homo sapiens ?
-
 ?
GSSSLQ + H2O 52.6% relative hydrolysis rate Homo sapiens ?
-
 ?
HSSKLQ-7-amido-4-methylcoumarin + H2O hydrolysis rate is 62.7 pmol/min per 100 pmol of PSA Homo sapiens ?
-
 ?
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 ?
-
 ?
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

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

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00651
-
 Cbz-SSKLL-CHO in 50 mM Tris buffer, 100 mM NaCl, pH 7.8, 10% DMSO Homo sapiens
0.01309
-
 Cbz-SSKYL-CHO in 50 mM Tris buffer, 100 mM NaCl, pH 7.8, 10% DMSO Homo sapiens
0.1553
-
 Cbz-SSKWL-CHO in 50 mM Tris buffer, 100 mM NaCl, pH 7.8, 10% DMSO Homo sapiens
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
0.5
-
 Cbz-SSKPL-CHO in 50 mM Tris buffer, 100 mM NaCl, pH 7.8, 10% DMSO Homo sapiens
1
-
 Cbz-SSKDL-CHO in 50 mM Tris buffer, 100 mM NaCl, pH 7.8, 10% DMSO Homo sapiens