Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTT3IXG)

DTT Name Kynurenine oxoglutarate transaminase II (AADAT)
Synonyms
Kynurenineoxoglutarate transaminase II; Kynurenineoxoglutarate transaminase 2; Kynurenineoxoglutarate aminotransferase II; Kynurenine/alphaaminoadipate aminotransferase, mitochondrial; Kynurenine aminotransferase II; KAT/AadAT; Alphaaminoadipate aminotransferase; AadAT; 2aminoadipate transaminase; 2aminoadipate aminotransferase
Gene Name AADAT
DTT Type
Preclinical target
 [1]
BioChemical Class
Transaminase
UniProt ID
AADAT_HUMAN
TTD ID
T82668
3D Structure
Download
2D Sequence (FASTA)
Download
3D Structure (PDB)
Download
EC Number
EC 2.6.1.39
Sequence
MNYARFITAASAARNPSPIRTMTDILSRGPKSMISLAGGLPNPNMFPFKTAVITVENGKT
IQFGEEMMKRALQYSPSAGIPELLSWLKQLQIKLHNPPTIHYPPSQGQMDLCVTSGSQQG
LCKVFEMIINPGDNVLLDEPAYSGTLQSLHPLGCNIINVASDESGIVPDSLRDILSRWKP
EDAKNPQKNTPKFLYTVPNGNNPTGNSLTSERKKEIYELARKYDFLIIEDDPYYFLQFNK
FRVPTFLSMDVDGRVIRADSFSKIISSGLRIGFLTGPKPLIERVILHIQVSTLHPSTFNQ
LMISQLLHEWGEEGFMAHVDRVIDFYSNQKDAILAAADKWLTGLAEWHVPAAGMFLWIKV
KGINDVKELIEEKAVKMGVLMLPGNAFYVDSSAPSPYLRASFSSASPEQMDVAFQVLAQL
IKESL
Function
Transaminase with broad substrate specificity. Has transaminase activity towards aminoadipate, kynurenine, methionine and glutamate. Shows activity also towards tryptophan, aspartate and hydroxykynurenine. Accepts a variety of oxo-acids as amino- group acceptors, with a preference for 2-oxoglutarate, 2- oxocaproic acid, phenylpyruvate and alpha-oxo-gamma-methiol butyric acid. Can also use glyoxylate as amino-group acceptor (in vitro).
KEGG Pathway
Lysine degradation (hsa00310 )
Tryptophan metabolism (hsa00380 )
Metabolic pathways (hsa01100 )
2-Oxocarboxylic acid metabolism (hsa01210 )
Reactome Pathway
Tryptophan catabolism (R-HSA-71240 )
Lysine catabolism (R-HSA-71064 )
BioCyc Pathway
MetaCyc:HS03239-MON

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DTT
7 Patented Agent(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
US10065972, Example 281 DMBWJK4 N. A. N. A. Patented [2]
US10065972, Example 396 DMT8WVZ N. A. N. A. Patented [2]
US10065972, Example 560 DM9QCTJ N. A. N. A. Patented [2]
US8933095, 1 DMG3T7E N. A. N. A. Patented [3]
US8933095, 14 DMZUNJ4 N. A. N. A. Patented [4]
US8933095, 16 DMRN5F4 N. A. N. A. Patented [3]
US8933095, 18 DMOZ4FS N. A. N. A. Patented [4]
------------------------------------------------------------------------------------
⏷ Show the Full List of 7 Patented Agent(s)
3 Preclinical Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
(S)-4-(Ethylsulfonyl)benzoylalanine DMEJYV4 Cognitive impairment 6D71 Preclinical [5]
BFF-122 DM6BGJ9 Cognitive impairment 6D71 Preclinical [6]
PF-04859989 DM3U2S5 Cognitive impairment 6D71 Preclinical [7]
------------------------------------------------------------------------------------

References

1 Improvement of kynurenine aminotransferase-II inhibitors guided by mimicking sulfate esters. PLoS One. 2018 Apr 24;13(4):e0196404.
2 Bicyclic or tricyclic heterocyclic compound. US10065972.
3 KAT II inhibitors. US8933095.
4 KAT II inhibitors. US8598200.
5 Specific inhibition of kynurenate synthesis enhances extracellular dopamine levels in the rodent striatum. Neuroscience. 2009 Mar 3;159(1):196-203.
6 Tryptophan metabolism as a common therapeutic target in cancer, neurodegeneration and beyond. Nat Rev Drug Discov. 2019 May;18(5):379-401.
7 Investigating KYNA production and kynurenergic manipulation on acute mouse brain slice preparations. Brain Res Bull. 2019 Mar;146:185-191.