Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTWQM3J)

• DTT Name: Kynureninase (KYNU)
• Synonyms: L-kynurenine hydrolase; KYNU
• Gene Name: KYNU
• DTT Type: Preclinical target; [1]
• BioChemical Class: Carbon-carbon bonds hydrolase
• UniProt ID: KYNU_HUMAN
• TTD ID: T99912
• EC Number: EC 3.7.1.3
• Sequence:
  MEPSSLELPADTVQRIAAELKCHPTDERVALHLDEEDKLRHFRECFYIPKIQDLPPVDLS
  LVNKDENAIYFLGNSLGLQPKMVKTYLEEELDKWAKIAAYGHEVGKRPWITGDESIVGLM
  KDIVGANEKEIALMNALTVNLHLLMLSFFKPTPKRYKILLEAKAFPSDHYAIESQLQLHG
  LNIEESMRMIKPREGEETLRIEDILEVIEKEGDSIAVILFSGVHFYTGQHFNIPAITKAG
  QAKGCYVGFDLAHAVGNVELYLHDWGVDFACWCSYKYLNAGAGGIAGAFIHEKHAHTIKP
  ALVGWFGHELSTRFKMDNKLQLIPGVCGFRISNPPILLVCSLHASLEIFKQATMKALRKK
  SVLLTGYLEYLIKHNYGKDKAATKKPVVNIITPSHVEERGCQLTITFSVPNKDVFQELEK
  RGVVCDKRNPNGIRVAPVPLYNSFHDVYKFTNLLTSILDSAETKN
• Function: Catalyzes the cleavage of L-kynurenine (L-Kyn) and L-3- hydroxykynurenine (L-3OHKyn) into anthranilic acid (AA) and 3- hydroxyanthranilic acid (3-OHAA), respectively. Has a preference for the L-3-hydroxy form. Also has cysteine-conjugate-beta-lyase activity.
• KEGG Pathway:
  Tryptophan metabolism (hsa00380)
  Metabolic pathways (hsa01100)
• Reactome Pathway: Tryptophan catabolism (R-HSA-71240)
• BioCyc Pathway: MetaCyc:HS03952-MON

Molecular Interaction Atlas (MIA) of This DTT

2 Preclinical Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
2-Amino-4-[3-hydroxyphenyl]-4-hydroxybutanoic acid	DM1R3VC	Breast cancer	2C60-2C65	Preclinical	[2]
S-(2-Aminophenyl)-L-cysteine S,S-dioxide	DM9Y05C	Bacterial infection	1A00-1C4Z	Preclinical	[3]

4 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
3,6,9,12,15-Pentaoxaheptadecane	DMY8IOP	Discovery agent	N.A.	Investigative	[4]
3-hydroxydesaminokynurenine	DM5T6AM	Discovery agent	N.A.	Investigative	[1]
3-Hydroxyhippuric acid	DM2LBFW	Discovery agent	N.A.	Investigative	[4]
3-methoxydesaminokynurenine	DMHVIK3	Discovery agent	N.A.	Investigative	[1]

References

• [1] Comparative inhibition by substrate analogues 3-methoxy- and 3-hydroxydesaminokynurenine and an improved 3 step purification of recombinant human kynureninase. BMC Biochem. 2003 Sep 24;4:13.
• [2] 2-Amino-4-[3'-hydroxyphenyl]-4-hydroxybutanoic acid; a potent inhibitor of rat and recombinant human kynureninase. Bioorg Med Chem Lett. 2002 Feb 11;12(3):361-3.
• [3] Structure, mechanism, and substrate specificity of kynureninase. Biochim Biophys Acta. 2011 Nov;1814(11):1481-8.
• [4] The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.