Target Information

Target General Infomation
Target ID
T93566
Former ID
TTDR01369
Target Name
mRNA of human 5-lipoxygenase
Gene Name
ALOX5
Synonyms
5LO (mRNA); 5lipoxygenase (mRNA); ALOX5 (mRNA); Arachidonate 5lipoxygenase (mRNA); ALOX5
Target Type
Discontinued
Disease Asthma [ICD10: J45]
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89]
Function
Catalyzes the first step in leukotriene biosynthesis, and thereby plays a role in inflammatory processes.
BioChemical Class
Oxidoreductases acting on single donors
Target Validation
T93566
UniProt ID
P09917
EC Number
EC 1.13.11.34
Sequence
MPSYTVTVATGSQWFAGTDDYIYLSLVGSAGCSEKHLLDKPFYNDFERGAVDSYDVTVDE
ELGEIQLVRIEKRKYWLNDDWYLKYITLKTPHGDYIEFPCYRWITGDVEVVLRDGRAKLA
RDDQIHILKQHRRKELETRQKQYRWMEWNPGFPLSIDAKCHKDLPRDIQFDSEKGVDFVL
NYSKAMENLFINRFMHMFQSSWNDFADFEKIFVKISNTISERVMNHWQEDLMFGYQFLNG
CNPVLIRRCTELPEKLPVTTEMVECSLERQLSLEQEVQQGNIFIVDFELLDGIDANKTDP
CTLQFLAAPICLLYKNLANKIVPIAIQLNQIPGDENPIFLPSDAKYDWLLAKIWVRSSDF
HVHQTITHLLRTHLVSEVFGIAMYRQLPAVHPIFKLLVAHVRFTIAINTKAREQLICECG
LFDKANATGGGGHVQMVQRAMKDLTYASLCFPEAIKARGMESKEDIPYYFYRDDGLLVWE
AIRTFTAEVVDIYYEGDQVVEEDPELQDFVNDVYVYGMRGRKSSGFPKSVKSREQLSEYL
TVVIFTASAQHAAVNFGQYDWCSWIPNAPPTMRAPPPTAKGVVTIEQIVDTLPDRGRSCW
HLGAVWALSQFQENELFLGMYPEEHFIEKPVKEAMARFRKNLEAIVSVIAERNKKKQLPY
YYLSPDRIPNSVAI
Drugs and Mode of Action
Drug(s) CMI-977 Drug Info Discontinued in Phase 2 Discovery agent [546341]
TEBUFELONE Drug Info Discontinued in Phase 2 Pain [545171]
ZD-2138 Drug Info Discontinued in Phase 2 Asthma [545000]
Inhibitor (+)-3,3'-bisdemethyltanegool Drug Info [528750]
(-)-3,3'-bisdemethylpinoresinol Drug Info [528750]
(-)-pinoresinol Drug Info [528750]
(N-(3-phenoxycinnamyl)-acetohydroxamic acid Drug Info [530186]
1-(4-methoxyphenyl)-3-(1,3,4-thiadiazol-2-yl)urea Drug Info [528805]
1-(4-methoxyphenyl)-3-(4-methylthiazol-2-yl)urea Drug Info [528805]
1-(4-methoxyphenyl)-3-(5-methylthiazol-2-yl)urea Drug Info [528805]
2,4'-Diacetoxy-5,3'-di-(2-propenyl)-biphenyl Drug Info [530176]
2,4'-Dimethoxy-5,3'-di-(2-propenyl)-biphenyl Drug Info [530176]
2,4,5-Triarylimidazole analogue Drug Info [551278]
2-(4-methoxyphenyl)-N-(thiazol-2-yl)acetamide Drug Info [528805]
2-(benzyloxy)naphthalene Drug Info [530239]
2-phenyl-N-(1,3,4-thiadiazol-2-yl)acetamide Drug Info [528805]
2-phenyl-N-(thiazol-2-yl)acetamide Drug Info [528805]
3,4,5-trimethoxy-N-(thiazol-2-yl)benzamide Drug Info [528805]
3-methoxy-N-(1,3,4-thiadiazol-2-yl)benzamide Drug Info [528805]
3-methoxy-N-(4-methylthiazol-2-yl)benzamide Drug Info [528805]
4'-Methoxy-5,3'-dipropyl-biphenyl-2ol Drug Info [530176]
4-(dimethylamino)-N-(thiazol-2-yl)benzamide Drug Info [528805]
4-methoxy-N-(thiazol-2-yl)benzamide Drug Info [528805]
5,3'-Dipropyl-biphenyl-2,4'-diol Drug Info [530176]
CMI-977 Drug Info [527799]
HONOKIOL Drug Info [530176]
ISAINDIGOTONE Drug Info [526182]
Isojaspic acid Drug Info [530468]
JASPAQUINOL Drug Info [530468]
KAEMPFEROL Drug Info [528750]
L-689065 Drug Info [534031]
L-702-539 Drug Info [534459]
L-746530 Drug Info [528021]
Methyl 2-(Benzylamino)-1H-indole-3-carboxylate Drug Info [530186]
Methyl 2-(Diallylamino)-1H-indole-3-carboxylate Drug Info [530186]
METHYLHONOKIOL Drug Info [530176]
N-(1,3,4-thiadiazol-2-yl)benzamide Drug Info [528805]
N-(3-phenoxycinnamyl)-N-hydroxyacetamide Drug Info [529646]
N-(4-methylthiazol-2-yl)-2-phenylacetamide Drug Info [528805]
N-(4-methylthiazol-2-yl)benzamide Drug Info [528805]
N-(5-methylthiazol-2-yl)-2-phenylacetamide Drug Info [528805]
N-(5-methylthiazol-2-yl)benzamide Drug Info [528805]
N-(thiazol-2-yl)benzamide Drug Info [528805]
N-hydroxy-N-[1-(4-isobutylphenyl)ethyl]urea Drug Info [534335]
N-hydroxycarbamate derivative Drug Info [527411]
PD-169316 Drug Info [551278]
PUUPEHEDIONE Drug Info [530468]
PUUPEHENONE Drug Info [530468]
TEBUFELONE Drug Info [534697]
ZD-2138 Drug Info [530899]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
BioCyc Pathway Aspirin-triggered lipoxin biosynthesis
Resolvin D biosynthesis
Leukotriene biosynthesis
Lipoxin biosynthesis
Aspirin triggered resolvin D biosynthesis
Aspirin triggered resolvin E biosynthesis
KEGG Pathway Arachidonic acid metabolism
Metabolic pathways
Serotonergic synapse
Ovarian steroidogenesis
Toxoplasmosis
NetPath Pathway IL4 Signaling Pathway
PathWhiz Pathway Arachidonic Acid Metabolism
WikiPathways Arachidonic acid metabolism
Eicosanoid Synthesis
Selenium Micronutrient Network
References
Ref 545000Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001835)
Ref 545171Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002346)
Ref 546341Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007577)
Ref 526182J Nat Prod. 2001 Oct;64(10):1297-300.Inhibition of leukocyte functions by the alkaloid isaindigotone from Isatis indigotica and some new synthetic derivatives.
Ref 527411Bioorg Med Chem Lett. 2005 Feb 15;15(4):1083-5.5-Lipoxygenase inhibition by N-hydroxycarbamates in dual-function compounds.
Ref 527799J Med Chem. 2005 Oct 20;48(21):6523-43.Designed multiple ligands. An emerging drug discovery paradigm.
Ref 528021Bioorg Med Chem Lett. 2006 May 1;16(9):2528-31. Epub 2006 Feb 7.Substituted coumarins as potent 5-lipoxygenase inhibitors.
Ref 528750J Nat Prod. 2007 May;70(5):859-62. Epub 2007 Mar 23.Lipoxygenase inhibitory constituents of the fruits of noni (Morinda citrifolia) collected in Tahiti.
Ref 528805J Med Chem. 2007 May 31;50(11):2640-6. Epub 2007 Apr 27.Identification of natural-product-derived inhibitors of 5-lipoxygenase activity by ligand-based virtual screening.
Ref 529646J Med Chem. 2008 Sep 11;51(17):5449-53. Epub 2008 Aug 19.Novel and potent inhibitors of 5-lipoxygenase product synthesis based on the structure of pirinixic acid.
Ref 530176Bioorg Med Chem. 2009 Jul 1;17(13):4459-65. Epub 2009 May 18.Design and synthesis of ten biphenyl-neolignan derivatives and their in vitro inhibitory potency against cyclooxygenase-1/2 activity and 5-lipoxygenase-mediated LTB4-formation.
Ref 530186J Med Chem. 2009 Jun 11;52(11):3474-83.Structural optimization and biological evaluation of 2-substituted 5-hydroxyindole-3-carboxylates as potent inhibitors of human 5-lipoxygenase.
Ref 530239Nat Chem Biol. 2009 Aug;5(8):585-92. Epub 2009 Jun 28.Bioactivity-guided mapping and navigation of chemical space.
Ref 530468J Nat Prod. 2009 Oct;72(10):1857-63.Using enzyme assays to evaluate the structure and bioactivity of sponge-derived meroterpenes.
Ref 530899Bioorg Med Chem. 2010 Jun 1;18(11):3910-24. Epub 2010 Apr 18.Synthesis and biological activity of N-aroyl-tetrahydro-gamma-carbolines.
Ref 534031J Med Chem. 1993 Sep 17;36(19):2771-87.Substituted thiopyrano[2,3,4-c,d]indoles as potent, selective, and orally active inhibitors of 5-lipoxygenase. Synthesis and biological evaluation of L-691,816.
Ref 534335J Med Chem. 1997 Feb 28;40(5):819-24.Nonsteroidal anti-inflammatory drugs as scaffolds for the design of 5-lipoxygenase inhibitors.
Ref 534459J Med Chem. 1997 Aug 29;40(18):2866-75.Substituted (pyridylmethoxy)naphthalenes as potent and orally active 5-lipoxygenase inhibitors; synthesis, biological profile, and pharmacokinetics of L-739,010.
Ref 534697J Med Chem. 1998 Aug 27;41(18):3515-29.New cyclooxygenase-2/5-lipoxygenase inhibitors. 3. 7-tert-butyl-2, 3-dihydro-3,3-dimethylbenzofuran derivatives as gastrointestinal safe antiinflammatory and analgesic agents: variations at the 5 position.
Ref 549595US patent application no. 5,530,114, Oligonucleotide modulation of arachidonic acid metabolism.
Ref 5512782,4,5- triarylimidazole inhibitors of IL-1 biosynthesis, Bioorg. Med. Chem. Lett. 5(11):1171-1176 (1995).

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