Details of the Target

General Information of Target

Target ID LDTP03285
Target Name Thromboxane-A synthase (TBXAS1)
Gene Name TBXAS1
Gene ID 6916
Synonyms
CYP5; CYP5A1; TXAS; Thromboxane-A synthase; TXA synthase; TXS; EC 5.3.99.5; Cytochrome P450 5A1; Hydroperoxy icosatetraenoate dehydratase; EC 4.2.1.152
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MEALGFLKLEVNGPMVTVALSVALLALLKWYSTSAFSRLEKLGLRHPKPSPFIGNLTFFR
QGFWESQMELRKLYGPLCGYYLGRRMFIVISEPDMIKQVLVENFSNFTNRMASGLEFKSV
ADSVLFLRDKRWEEVRGALMSAFSPEKLNEMVPLISQACDLLLAHLKRYAESGDAFDIQR
CYCNYTTDVVASVAFGTPVDSWQAPEDPFVKHCKRFFEFCIPRPILVLLLSFPSIMVPLA
RILPNKNRDELNGFFNKLIRNVIALRDQQAAEERRRDFLQMVLDARHSASPMGVQDFDIV
RDVFSSTGCKPNPSRQHQPSPMARPLTVDEIVGQAFIFLIAGYEIITNTLSFATYLLATN
PDCQEKLLREVDVFKEKHMAPEFCSLEEGLPYLDMVIAETLRMYPPAFRFTREAAQDCEV
LGQRIPAGAVLEMAVGALHHDPEHWPSPETFNPERFTAEARQQHRPFTYLPFGAGPRSCL
GVRLGLLEVKLTLLHVLHKFRFQACPETQVPLQLESKSALGPKNGVYIKIVSR
Target Type
Clinical trial
Target Bioclass
Enzyme
Family
Cytochrome P450 family
Subcellular location
Endoplasmic reticulum membrane
Function
Catalyzes the conversion of prostaglandin H2 (PGH2) to thromboxane A2 (TXA2), a potent inducer of blood vessel constriction and platelet aggregation . Cleaves also PGH2 to 12-hydroxy-heptadecatrienoicacid (12-HHT) and malondialdehyde, which is known to act as a mediator of DNA damage. 12-HHT and malondialdehyde are formed stoichiometrically in the same amounts as TXA2. Additionally, displays dehydratase activity, toward (15S)-hydroperoxy-(5Z,8Z,11Z,13E)-eicosatetraenoate (15(S)-HPETE) producing 15-KETE and 15-HETE.
TTD ID
T78356
Uniprot ID
P24557
DrugMap ID
TTKNWZ4
Ensemble ID
ENST00000336425.10
HGNC ID
HGNC:11609
ChEMBL ID
CHEMBL1835

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
HCT116 SNV: p.F410I .
HCT15 SNV: p.R276I .
HT SNV: p.L230S .
HUH28 SNV: p.P51S .
NCIH358 SNV: p.P406L .

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  		C355(1.36)  LDD3314  [1]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 A101D C355(1.94); C464(1.37); C430(1.86)  LDD2250  [1]
 LDCM0023  KB03 A101D C355(2.69); C464(1.58); C430(2.19)  LDD2667  [1]
 LDCM0024  KB05 IGR37 C355(1.36)  LDD3314  [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