General Information of Target

Target ID LDTP06590
Target Name Prostacyclin synthase (PTGIS)
Gene Name PTGIS
Gene ID 5740
Synonyms
CYP8; CYP8A1; Prostacyclin synthase; EC 5.3.99.4; Hydroperoxy icosatetraenoate dehydratase; EC 4.2.1.152; Prostaglandin I2 synthase
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MAWAALLGLLAALLLLLLLSRRRTRRPGEPPLDLGSIPWLGYALDFGKDAASFLTRMKEK
HGDIFTILVGGRYVTVLLDPHSYDAVVWEPRTRLDFHAYAIFLMERIFDVQLPHYSPSDE
KARMKLTLLHRELQALTEAMYTNLHAVLLGDATEAGSGWHEMGLLDFSYSFLLRAGYLTL
YGIEALPRTHESQAQDRVHSADVFHTFRQLDRLLPKLARGSLSVGDKDHMCSVKSRLWKL
LSPARLARRAHRSKWLESYLLHLEEMGVSEEMQARALVLQLWATQGNMGPAAFWLLLFLL
KNPEALAAVRGELESILWQAEQPVSQTTTLPQKVLDSTPVLDSVLSESLRLTAAPFITRE
VVVDLAMPMADGREFNLRRGDRLLLFPFLSPQRDPEIYTDPEVFKYNRFLNPDGSEKKDF
YKDGKRLKNYNMPWGAGHNHCLGRSYAVNSIKQFVFLVLVHLDLELINADVEIPEFDLSR
YGFGLMQPEHDVPVRYRIRP
Target Type
Literature-reported
Target Bioclass
Enzyme
Family
Cytochrome P450 family
Subcellular location
Endoplasmic reticulum membrane
Function
Catalyzes the biosynthesis and metabolism of eicosanoids. Catalyzes the isomerization of prostaglandin H2 to prostacyclin (= prostaglandin I2), a potent mediator of vasodilation and inhibitor of platelet aggregation. Additionally, displays dehydratase activity, toward hydroperoxyeicosatetraenoates (HPETEs), especially toward (15S)-hydroperoxy-(5Z,8Z,11Z,13E)-eicosatetraenoate (15(S)-HPETE).
TTD ID
T83979
Uniprot ID
Q16647
DrugMap ID
TTLXKZR
Ensemble ID
ENST00000244043.5
HGNC ID
HGNC:9603
ChEMBL ID
CHEMBL4428

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info 
C441(2.10)  LDD3331  [1]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 GB-2 C231(1.30); C441(1.55)  LDD2335  [1]
 LDCM0023  KB03 G-415 C441(1.39)  LDD2749  [1]
 LDCM0024  KB05 MKN-1 C441(2.10)  LDD3331  [1]

References

1 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840