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Literature summary for 2.3.1.250 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
Search for more literature for 2.3.1.250

Application

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

Inhibitors

Inhibitors Comment Organism Structure
2-(4-(2-methylpyridin-4-yl)phenyl)-N-(4-(pyridin-3-yl)phenyl)acetamide i.e. C59 Homo sapiens
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

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

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
(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

Organism UniProt Comment Textmining
Homo sapiens Q9H237
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-

Purification (Commentary)

Purification (Comment) Organism
-
 Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
(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
-
 ?
(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
-
 ?
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
-
 ?
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
-
 ?
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
-
 ?
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
-
 ?
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

Synonyms Comment Organism
porcupine
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
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

General Information Comment Organism
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