Target Information
Target General Infomation | |||||
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Target ID |
T03691
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Former ID |
TTDC00130
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Target Name |
Leukotriene A-4 hydrolase
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Gene Name |
LTA4H
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Synonyms |
LTA-4hydrolase; LTA-H; Leukotriene A(4) hydrolase; Leukotriene A(4)Leukotriene A-4 hydrolase hydrolase; Leukotriene A4 hydrolase; LTA4H
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Target Type |
Successful
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Disease | Acute myeloid leukemia [ICD9: 205; ICD10: C92.0] | ||||
Inflammatory disease [ICD9: 140-229, 147, 173, 573.3, 710-719; ICD10: C11, C44, K75.9, M00-M25] | |||||
Myocardial infarction [ICD9: 410; ICD10: I21, I22] | |||||
Function |
Epoxide hydrolase that catalyzes the final step in the biosynthesis of the proinflammatory mediator leukotriene B4. Has also aminopeptidase activity.
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BioChemical Class |
Etherhydrolase
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Target Validation |
T03691
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UniProt ID | |||||
EC Number |
EC 3.3.2.6
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Sequence |
MPEIVDTCSLASPASVCRTKHLHLRCSVDFTRRTLTGTAALTVQSQEDNLRSLVLDTKDL
TIEKVVINGQEVKYALGERQSYKGSPMEISLPIALSKNQEIVIEISFETSPKSSALQWLT PEQTSGKEHPYLFSQCQAIHCRAILPCQDTPSVKLTYTAEVSVPKELVALMSAIRDGETP DPEDPSRKIYKFIQKVPIPCYLIALVVGALESRQIGPRTLVWSEKEQVEKSAYEFSETES MLKIAEDLGGPYVWGQYDLLVLPPSFPYGGMENPCLTFVTPTLLAGDKSLSNVIAHEISH SWTGNLVTNKTWDHFWLNEGHTVYLERHICGRLFGEKFRHFNALGGWGELQNSVKTFGET HPFTKLVVDLTDIDPDVAYSSVPYEKGFALLFYLEQLLGGPEIFLGFLKAYVEKFSYKSI TTDDWKDFLYSYFKDKVDVLNQVDWNAWLYSPGLPPIKPNYDMTLTNACIALSQRWITAK EDDLNSFNATDLKDLSSHQLNEFLAQTLQRAPLPLGHIKRMQEVYNFNAINNSEIRFRWL RLCIQSKWEDAIPLALKMATEQGRMKFTRPLFKDLAAFDKSHDQAVRTYQEHKASMHPVT AMLVGKDLKVD |
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Drugs and Mode of Action | |||||
Inhibitor | (4-(thiophen-2-yl)phenyl)methanamine | Drug Info | [530549] | ||
(4-fluorophenyl)(pyridin-4-yl)methanone | Drug Info | [551374] | |||
(R)-2-((4-benzylphenoxy)methyl)piperidine | Drug Info | [530833] | |||
(R)-2-((4-phenoxyphenoxy)methyl)piperidine | Drug Info | [530833] | |||
(R)-2-(4-Benzylphenoxymethyl)pyrrolidine | Drug Info | [530549] | |||
(R)-N-benzyl-4-(pyrrolidin-2-ylmethoxy)aniline | Drug Info | [530267] | |||
(R/S)-2-((4-benzylphenoxy)methyl)piperazine | Drug Info | [530833] | |||
(R/S)-2-((4-benzylphenoxy)methyl)piperidine | Drug Info | [530833] | |||
(R/S)-2-((4-phenoxyphenoxy)methyl)piperidine | Drug Info | [530833] | |||
(S)-2-((4-phenoxyphenoxy)methyl)piperidine | Drug Info | [530833] | |||
1-(2,2'-bithiophen-5-yl)methanamine | Drug Info | [551374] | |||
1-(4-Phenoxyphenyl)piperazine | Drug Info | [530549] | |||
1-(4-thiophen-2-ylphenyl)methanamine | Drug Info | [551374] | |||
1-(pentyloxy)-4-phenoxybenzene | Drug Info | [529770] | |||
1-butoxy-4-phenoxybenzene | Drug Info | [529770] | |||
1-[4-(4-Iodophenoxy)phenyl]piperazine | Drug Info | [530549] | |||
1-[4-(Benzothiazol-2-yloxy)benzyl]piperidin-4-ol | Drug Info | [529569] | |||
2-(4-benzylphenoxy)ethanamine | Drug Info | [529770] | |||
2-(4-phenoxyphenoxy)ethanamine | Drug Info | [529770] | |||
2-(4-Piperidin-1-ylmethylphenoxy)benzothiazole | Drug Info | [529569] | |||
2-(7-(benzyloxy)-1H-indol-3-yl)ethanamine | Drug Info | [529868] | |||
2-Amino-N-[4-(phenylmethoxy)phenyl]-acetamide | Drug Info | [529408] | |||
2-[4-(2-Azepan-1-ylethoxy)phenoxy]benzooxazole | Drug Info | [529569] | |||
2-[4-(2-Azepan-1-ylethoxy)phenoxy]benzothiazole | Drug Info | [529569] | |||
2-[4-(2-Morpholin-4-ylethoxy)phenoxy]benzooxazole | Drug Info | [529569] | |||
2-[4-(2-Piperidin-1-ylethyl)phenoxy]benzothiazole | Drug Info | [529569] | |||
3-(Benzyloxy)Pyridin-2-Amine | Drug Info | [551393] | |||
4-(2-amino-1,3-thiazol-4-yl)phenol | Drug Info | [551374] | |||
4-(4-(pentyloxy)phenoxy)phenol | Drug Info | [529770] | |||
4-(4-butoxyphenoxy)phenol | Drug Info | [529770] | |||
4-(4-propoxyphenoxy)phenol | Drug Info | [529770] | |||
4-amino-N-[4-(benzyloxy)phenyl]butanamide | Drug Info | [551374] | |||
4-Amino-N-[4-(phenylmethoxy)phenyl]butanamide | Drug Info | [529408] | |||
4-[2-(4-Benzylphenoxy)ethyl]pyridine | Drug Info | [530549] | |||
4S-4,5-Diamino-N-(4-phenoxyphenyl)pentanamide | Drug Info | [529408] | |||
5-[2-(1H-pyrrol-1-yl)ethoxy]-1H-indole | Drug Info | [551374] | |||
5-[2-(4-hydroxyphenyl)ethyl]benzene-1,3-diol | Drug Info | [551374] | |||
8(S)-amino-2(R)-methyl-7-oxononanoic acid | Drug Info | [534266] | |||
Acetate Ion | Drug Info | [551393] | |||
Bestatin | Drug Info | [551391] | |||
DG051 | Drug Info | [536080], [536517] | |||
JNJ-10392980 | Drug Info | [529569] | |||
N-(pyridin-3-ylmethyl)aniline | Drug Info | [551374] | |||
N-benzyl-4-[(2R)-pyrrolidin-2-ylmethoxy]aniline | Drug Info | [551374] | |||
N-methyl-1-(2-thiophen-2-ylphenyl)methanamine | Drug Info | [551374] | |||
N-[4-(benzyloxy)phenyl]glycinamide | Drug Info | [551374] | |||
N1-[4-(Phenylmethoxy)phenyl]-D-aspartamine | Drug Info | [529408] | |||
N1-[4-(Phenylmethoxy)phenyl]-D-glutamine | Drug Info | [529408] | |||
N1-[4-(Phenylmethoxy)phenyl]-L-aspartamine | Drug Info | [529408] | |||
N1-[4-(Phenylmethoxy)phenyl]-L-glutamine | Drug Info | [529408] | |||
N4-[4-(Phenylmethoxy)phenyl]-L-aspartamine | Drug Info | [529408] | |||
N5-(4-Phenoxyphenyl)-L-glutamine | Drug Info | [529408] | |||
N5-[(4-Phenoxy)-3-pyridyl]-L-glutamamide | Drug Info | [529408] | |||
N5-[4-(1H-pyrrol-1-yl)phenyl]-L-glutamamide | Drug Info | [529408] | |||
N5-[4-(2-methylphenoxy)phenyl]-L-glutamamide | Drug Info | [529408] | |||
N5-[4-(2-Oxo-3-phenylpropoxy)phenyl]-L-glutamine | Drug Info | [529408] | |||
N5-[4-(2-phenylethoxy)phenyl]-L-glutamine | Drug Info | [529408] | |||
N5-[4-(3-methylphenoxy)phenyl]-L-glutamamide | Drug Info | [529408] | |||
N5-[4-(3-Phenylpropoxy)phenyl]-L-glutamine | Drug Info | [529408] | |||
N5-[4-(4-(3-Furyl)phenoxy)phenyl]-L-glutamamide | Drug Info | [529408] | |||
N5-[4-(4-methylphenoxy)phenyl]-L-glutamamide | Drug Info | [529408] | |||
N5-[4-(N-Phenylamino)phenyl]-L-glutamine | Drug Info | [529408] | |||
N5-[4-(Phenylmethoxy)phenyl]-D-glutamine | Drug Info | [529408] | |||
N5-[4-(Phenylmethoxy)phenyl]-L-glutamamide | Drug Info | [529408] | |||
N5-[4-(Phenylmethoxy)phenyl]-L-glutamine | Drug Info | [529408] | |||
N5-[4-Benzylphenyl]-L-glutamamide | Drug Info | [529408] | |||
N6-[4-(4-methylphenoxy)phenyl]-L-homoglutamine | Drug Info | [529408] | |||
SA-6541 | Drug Info | [529829] | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
BioCyc Pathway | Leukotriene biosynthesis | ||||
KEGG Pathway | Arachidonic acid metabolism | ||||
Metabolic pathways | |||||
PathWhiz Pathway | Arachidonic Acid Metabolism | ||||
WikiPathways | Arachidonic acid metabolism | ||||
Eicosanoid Synthesis | |||||
References | |||||
Ref 468215 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5151). | ||||
Ref 541672 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6548). | ||||
Ref 529408 | Bioorg Med Chem. 2008 May 1;16(9):4963-83. Epub 2008 Mar 20.Synthesis of glutamic acid analogs as potent inhibitors of leukotriene A4 hydrolase. | ||||
Ref 529569 | J Med Chem. 2008 Jul 24;51(14):4150-69. Epub 2008 Jun 28.Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity. | ||||
Ref 529770 | Bioorg Med Chem Lett. 2008 Dec 15;18(24):6549-52. Epub 2008 Oct 14.Activation and inhibition of leukotriene A4 hydrolase aminopeptidase activity by diphenyl ether and derivatives. | ||||
Ref 529829 | Bioorg Med Chem Lett. 2009 Jan 15;19(2):442-6. Epub 2008 Nov 18.Synthesis and biological evaluation of N-mercaptoacylcysteine derivatives as leukotriene A4 hydrolase inhibitors. | ||||
Ref 529868 | J Med Chem. 2008 Dec 25;51(24):7882-8.Discovery of multitarget inhibitors by combining molecular docking with common pharmacophore matching. | ||||
Ref 530267 | J Med Chem. 2009 Aug 13;52(15):4694-715.Discovery of leukotriene A4 hydrolase inhibitors using metabolomics biased fragment crystallography. | ||||
Ref 530549 | J Med Chem. 2010 Jan 28;53(2):573-85.Discovery of 4-[(2S)-2-{[4-(4-chlorophenoxy)phenoxy]methyl}-1-pyrrolidinyl]butanoic acid (DG-051) as a novel leukotriene A4 hydrolase inhibitor of leukotriene B4 biosynthesis. | ||||
Ref 530833 | Bioorg Med Chem Lett. 2010 May 1;20(9):2851-4. Epub 2010 Mar 12.Discovery of novel leukotriene A4 hydrolase inhibitors based on piperidine and piperazine scaffolds. | ||||
Ref 534266 | J Nat Prod. 1996 Oct;59(10):962-4.Isolation and structure of leukotriene-A4 hydrolase inhibitor: 8(S)-amino-2(R)-methyl-7-oxononanoic acid produced by Streptomyces diastaticus. | ||||
Ref 536080 | Effects of a 5-lipoxygenase-activating protein inhibitor on biomarkers associated with risk of myocardial infarction: a randomized trial. JAMA. 2005 May 11;293(18):2245-56. | ||||
Ref 536517 | BAY x 1005 attenuates atherosclerosis in apoE/LDLR - double knockout mice. J Physiol Pharmacol. 2007 Sep;58(3):583-8. |
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