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Literature summary extracted from

  • Lee, C.J.; Rana, M.S.; Bae, C.; Li, Y.; Banerjee, A.
    In vitro reconstitution of Wnt acylation reveals structural determinants of substrate recognition by the acyltransferase human porcupine (2019), J. Biol. Chem., 294, 231-245 .
    View publication on PubMedView publication on EuropePMC

Application

EC Number Application Comment Organism
2.3.1.250 drug development PORCN is a prominent target for developing inhibitors for various cancers Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.3.1.250 2-(4-(2-methylpyridin-4-yl)phenyl)-N-(4-(pyridin-3-yl)phenyl)acetamide i.e. C59 Homo sapiens
2.3.1.250 2-[5-methyl-6-(2-methylpyridin-4-yl)pyridin-3-yl]-N-(5-pyrazin-2-ylpyridin-2-yl)acetamide i.e. LGK-974 Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
2.3.1.250 endoplasmic reticulum endoplasmic reticulum-resident integral membrane enzyme Homo sapiens 5783
-

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.3.1.250 (9Z)-hexadec-9-enoyl-CoA + [Wnt]-L-serine Homo sapiens the enzyme catalyzes posttranslational modification of Wnts with palmitoleic acid. PORCN is necessary and sufficient for Wnt acylation. PORCN intimately recognizes the local structure of Wnt around the site of acylation CoA + [Wnt]-O-(9Z)-hexadec-9-enoyl-L-serine
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.3.1.250 Homo sapiens Q9H237
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.3.1.250
-
 Homo sapiens

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.3.1.250 (9Z)-hexadec-9-enoyl-CoA + [Wnt]-L-serine the enzyme catalyzes posttranslational modification of Wnts with palmitoleic acid. PORCN is necessary and sufficient for Wnt acylation. PORCN intimately recognizes the local structure of Wnt around the site of acylation Homo sapiens CoA + [Wnt]-O-(9Z)-hexadec-9-enoyl-L-serine
-
 ?
2.3.1.250 (9Z)-hexadec-9-enoyl-CoA + [Wnt]-L-serine there is an increase in the catalytic activity from hexanoyl-CoA to decanoyl-CoA, after which there is an abrupt drop for dodecanoyl-CoA. Upon further increase in fatty acyl chain length, the activity stays at approximately the same level until the unsaturated palmitoleoyl-CoA, which is the best substrate Homo sapiens CoA + [Wnt]-O-(9Z)-hexadec-9-enoyl-L-serine
-
 ?
2.3.1.250 decanoyl-CoA + [Wnt]-L-serine about 30% of the activity as compared to (9Z)-hexadec-9-enoyl-CoA. There is an increase in the catalytic activity from hexanoyl-CoA to decanoyl-CoA, after which there is an abrupt drop for dodecanoyl-CoA. Upon further increase in fatty acyl chain length, the activity stays at approximately the same level until the unsaturated palmitoleoyl-CoA, which is the best substrate Homo sapiens CoA + [Wnt]-O-decanoyl-L-serine
-
 ?
2.3.1.250 dodecanoyl-CoA + [Wnt]-L-serine about 15% of the activity as compared to (9Z)-hexadec-9-enoyl-CoA. There is an increase in the catalytic activity from hexanoyl-CoA to decanoyl-CoA, after which there is an abrupt drop for dodecanoyl-CoA. Upon further increase in fatty acyl chain length, the activity stays at approximately the same level until the unsaturated palmitoleoyl-CoA, which is the best substrate Homo sapiens CoA + [Wnt]-O-dodecanoyl-L-serine
-
 ?
2.3.1.250 hexanoyl-CoA + [Wnt]-L-serine about 20% of the activity as compared to (9Z)-hexadec-9-enoyl-CoA. There is an increase in the catalytic activity from hexanoyl-CoA to decanoyl-CoA, after which there is an abrupt drop for dodecanoyl-CoA. Upon further increase in fatty acyl chain length, the activity stays at approximately the same level until the unsaturated palmitoleoyl-CoA, which is the best substrate Homo sapiens CoA + [Wnt]-O-hexanoyl-L-serine
-
 ?
2.3.1.250 octanoyl-CoA + [Wnt]-L-serine about 25% of the activity as compared to (9Z)-hexadec-9-enoyl-CoA. There is an increase in the catalytic activity from hexanoyl-CoA to decanoyl-CoA, after which there is an abrupt drop for dodecanoyl-CoA. Upon further increase in fatty acyl chain length, the activity stays at approximately the same level until the unsaturated palmitoleoyl-CoA, which is the best substrate Homo sapiens CoA + [Wnt]-O-octanoyl-L-serine
-
 ?
2.3.1.250 tetradecanoyl-CoA + [Wnt]-L-serine about 10% of the activity as compared to (9Z)-hexadec-9-enoyl-CoA. There is an increase in the catalytic activity from hexanoyl-CoA to decanoyl-CoA, after which there is an abrupt drop for dodecanoyl-CoA. Upon further increase in fatty acyl chain length, the activity stays at approximately the same level until the unsaturated palmitoleoyl-CoA, which is the best substrate Homo sapiens CoA + [Wnt]-O-tetradecanoyl-L-serine
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.3.1.250 porcupine
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.3.1.250 0.00067
-
 pH 7.3, 25°C Homo sapiens 2-(4-(2-methylpyridin-4-yl)phenyl)-N-(4-(pyridin-3-yl)phenyl)acetamide

General Information

EC Number General Information Comment Organism
2.3.1.250 metabolism the enzyme catalyzes posttranslational modification of Wnts with palmitoleic acid. This unique form of lipidation with palmitoleic acid is a vital step in the biogenesis and secretion of Wnt Homo sapiens