Details of the Target

General Information of Target

Target ID LDTP01775
Target Name Phenylalanine-4-hydroxylase (PAH)
Gene Name PAH
Gene ID 5053
Synonyms
Phenylalanine-4-hydroxylase; PAH; EC 1.14.16.1; Phe-4-monooxygenase
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MSTAVLENPGLGRKLSDFGQETSYIEDNCNQNGAISLIFSLKEEVGALAKVLRLFEENDV
NLTHIESRPSRLKKDEYEFFTHLDKRSLPALTNIIKILRHDIGATVHELSRDKKKDTVPW
FPRTIQELDRFANQILSYGAELDADHPGFKDPVYRARRKQFADIAYNYRHGQPIPRVEYM
EEEKKTWGTVFKTLKSLYKTHACYEYNHIFPLLEKYCGFHEDNIPQLEDVSQFLQTCTGF
RLRPVAGLLSSRDFLGGLAFRVFHCTQYIRHGSKPMYTPEPDICHELLGHVPLFSDRSFA
QFSQEIGLASLGAPDEYIEKLATIYWFTVEFGLCKQGDSIKAYGAGLLSSFGELQYCLSE
KPKLLPLELEKTAIQNYTVTEFQPLYYVAESFNDAKEKVRNFAATIPRPFSVRYDPYTQR
IEVLDNTQQLKILADSINSEIGILCSALQKIK
Target Type
Successful
Target Bioclass
Enzyme
Family
Biopterin-dependent aromatic amino acid hydroxylase family
Function Catalyzes the hydroxylation of L-phenylalanine to L-tyrosine.
TTD ID
T76213
Uniprot ID
P00439
DrugMap ID
TTGSVH2
Ensemble ID
ENST00000553106.6
HGNC ID
HGNC:8582
ChEMBL ID
CHEMBL3076

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 3 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
YN-1
 Probe Info  		100.00  LDD0444  [1]
IPM
 Probe Info  		C445(0.00); C265(0.00)  LDD0241  [2]
DBIA
 Probe Info  		C445(1.66)  LDD3424  [3]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 Hep 3B2.1-7 C445(2.19)  LDD2353  [3]
 LDCM0023  KB03 Hep 3B2.1-7 C445(3.37)  LDD2770  [3]
 LDCM0024  KB05 SK-HEP1 C445(1.66)  LDD3424  [3]

The Interaction Atlas With This Target

The Drug(s) Related To This Target

Approved
Click To Hide/Show 7 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Carbocisteine Small molecular drug DB04339
Droxidopa Small molecular drug DB06262
Norepinephrine Small molecular drug DB00368
Phenylalanine Small molecular drug DB00120
Sapropterin Small molecular drug DB00360
Sapropterin Hydrochloride Small molecular drug D0S2IQ
Pegvaliase . D0T8HZ
Phase 2
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Hepastem . D05XZQ
Phenylalanine Hydroxylase . D00IDR
Investigative
Click To Hide/Show 9 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Alpha-methylphenylalanine Small molecular drug D08URY
Bh4 Small molecular drug D0F9XO
Fenclonine Small molecular drug D0F2GG
Altu-236 . D07GET
Beta-2-thienyl-l-alanine . DB03673
Bmn-168 . D05TXS
D-norleucine . DB04419
L-erythro-78-dihydrobiopterin . DB04400
Quinonoid 78-tetrahydrobiopterin . DB02562

References

1 Ynamide Electrophile for the Profiling of Ligandable Carboxyl Residues in Live Cells and the Development of New Covalent Inhibitors. J Med Chem. 2022 Aug 11;65(15):10408-10418. doi: 10.1021/acs.jmedchem.2c00272. Epub 2022 Jul 26.
2 Oxidant-Induced Bioconjugation for Protein Labeling in Live Cells. ACS Chem Biol. 2023 Jan 20;18(1):112-122. doi: 10.1021/acschembio.2c00740. Epub 2022 Dec 21.
3 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