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Literature summary for 3.1.8.1 extracted from

  • Ashani, Y.; Gupta, R.D.; Goldsmith, M.; Silman, I.; Sussman, J.L.; Tawfik, D.S.; Leader, H.
    Stereo-specific synthesis of analogs of nerve agents and their utilization for selection and characterization of paraoxonase (PON1) catalytic scavengers (2010), Chem. Biol. Interact., 187, 362-369.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.1.8.1

Application

Application Comment Organism
drug development PON1 variants with catalytic efficacy that will qualify them as potential drug candidate for prophylactic treatment of nerve agent intoxication synthetic construct

Cloned(Commentary)

Cloned (Comment) Organism
-
 synthetic construct

Protein Variants

Protein Variants Comment Organism
H115W as the wild-type, preference for the three RP isomers of the O-alkyl methylphosphonyl-3-cyano-7-hydroxy-4-methylcoumarin analogs, regardless of the size of the alkyl group synthetic construct
additional information variant 3B3 hydrolyzes almost exclusively the RP isomer whereas variant 3D8 is capable of hydrolyzing both RP and SP enantiomers. Variant 3B3 displays even greater stereo-specificity towards the RP enantiomers as the wild-type and mutant H115W synthetic construct

Organism

Organism UniProt Comment Textmining
synthetic construct
-
 variant G3C9 of the gene shuffling products of four mammalian PON1s
-

Purification (Commentary)

Purification (Comment) Organism
-
 synthetic construct

Storage Stability

Storage Stability Organism
4°C, 2 weeks synthetic construct

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
RP-O-ethyl methylphosphonyl-3-cyano-7-hydroxy-4-methylcoumarin + H2O
-
 synthetic construct ?
-
 ?
RP-O-n-propyl methylphosphonyl-3-cyano-7-hydroxy-4-methylcoumarin + H2O
-
 synthetic construct ?
-
 ?
SP-O-ethyl methylphosphonyl-3-cyano-7-hydroxy-4-methylcoumarin + H2O
-
 synthetic construct ?
-
 ?
SP-O-n-propyl methylphosphonyl-3-cyano-7-hydroxy-4-methylcoumarin + H2O
-
 synthetic construct ?
-
 ?

Synonyms

Synonyms Comment Organism
paraoxonase
-
 synthetic construct
PON1
-
 synthetic construct

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.15
-
 SP-O-ethyl methylphosphonyl-3-cyano-7-hydroxy-4-methylcoumarin wild-type, in 50 mM Tris buffer, 1 mM CaCl2, pH 8.0, 25°C synthetic construct
0.167
-
 RP-O-n-propyl methylphosphonyl-3-cyano-7-hydroxy-4-methylcoumarin mutant H115W, in 50 mM Tris buffer, 1 mM CaCl2, pH 8.0, 25°C synthetic construct
0.5
-
 SP-O-ethyl methylphosphonyl-3-cyano-7-hydroxy-4-methylcoumarin mutant H115W, in 50 mM Tris buffer, 1 mM CaCl2, pH 8.0, 25°C synthetic construct
0.55
-
 RP-O-ethyl methylphosphonyl-3-cyano-7-hydroxy-4-methylcoumarin mutant H115W, in 50 mM Tris buffer, 1 mM CaCl2, pH 8.0, 25°C synthetic construct
1.83
-
 SP-O-n-propyl methylphosphonyl-3-cyano-7-hydroxy-4-methylcoumarin wild-type, in 50 mM Tris buffer, 1 mM CaCl2, pH 8.0, 25°C synthetic construct
4.95
-
 RP-O-n-propyl methylphosphonyl-3-cyano-7-hydroxy-4-methylcoumarin wild-type, in 50 mM Tris buffer, 1 mM CaCl2, pH 8.0, 25°C synthetic construct
6.467
-
 SP-O-n-propyl methylphosphonyl-3-cyano-7-hydroxy-4-methylcoumarin mutant H115W, in 50 mM Tris buffer, 1 mM CaCl2, pH 8.0, 25°C synthetic construct
11.72
-
 RP-O-ethyl methylphosphonyl-3-cyano-7-hydroxy-4-methylcoumarin wild-type, in 50 mM Tris buffer, 1 mM CaCl2, pH 8.0, 25°C synthetic construct

kcat/KM [mM/s]

kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
1.05
-
 SP-O-ethyl methylphosphonyl-3-cyano-7-hydroxy-4-methylcoumarin wild-type, in 50 mM Tris buffer, 1 mM CaCl2, pH 8.0, 25°C synthetic construct
6.7
-
 SP-O-ethyl methylphosphonyl-3-cyano-7-hydroxy-4-methylcoumarin mutant H115W, in 50 mM Tris buffer, 1 mM CaCl2, pH 8.0, 25°C synthetic construct
13.6
-
 SP-O-n-propyl methylphosphonyl-3-cyano-7-hydroxy-4-methylcoumarin wild-type, in 50 mM Tris buffer, 1 mM CaCl2, pH 8.0, 25°C synthetic construct
25
-
 SP-O-n-propyl methylphosphonyl-3-cyano-7-hydroxy-4-methylcoumarin mutant H115W, in 50 mM Tris buffer, 1 mM CaCl2, pH 8.0, 25°C synthetic construct
617
-
 RP-O-ethyl methylphosphonyl-3-cyano-7-hydroxy-4-methylcoumarin wild-type, in 50 mM Tris buffer, 1 mM CaCl2, pH 8.0, 25°C synthetic construct
767
-
 RP-O-ethyl methylphosphonyl-3-cyano-7-hydroxy-4-methylcoumarin mutant H115W, in 50 mM Tris buffer, 1 mM CaCl2, pH 8.0, 25°C synthetic construct
883
-
 RP-O-n-propyl methylphosphonyl-3-cyano-7-hydroxy-4-methylcoumarin mutant H115W, in 50 mM Tris buffer, 1 mM CaCl2, pH 8.0, 25°C synthetic construct
933
-
 RP-O-n-propyl methylphosphonyl-3-cyano-7-hydroxy-4-methylcoumarin wild-type, in 50 mM Tris buffer, 1 mM CaCl2, pH 8.0, 25°C synthetic construct