Target Information
Target General Infomation | |||||
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Target ID |
T93566
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Former ID |
TTDR01369
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Target Name |
mRNA of human 5-lipoxygenase
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Gene Name |
ALOX5
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Synonyms |
5LO (mRNA); 5lipoxygenase (mRNA); ALOX5 (mRNA); Arachidonate 5lipoxygenase (mRNA); ALOX5
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Target Type |
Discontinued
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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.
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BioChemical Class |
Oxidoreductases acting on single donors
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Target Validation |
T93566
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UniProt ID | |||||
EC Number |
EC 1.13.11.34
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Sequence |
MPSYTVTVATGSQWFAGTDDYIYLSLVGSAGCSEKHLLDKPFYNDFERGAVDSYDVTVDE
ELGEIQLVRIEKRKYWLNDDWYLKYITLKTPHGDYIEFPCYRWITGDVEVVLRDGRAKLA RDDQIHILKQHRRKELETRQKQYRWMEWNPGFPLSIDAKCHKDLPRDIQFDSEKGVDFVL NYSKAMENLFINRFMHMFQSSWNDFADFEKIFVKISNTISERVMNHWQEDLMFGYQFLNG CNPVLIRRCTELPEKLPVTTEMVECSLERQLSLEQEVQQGNIFIVDFELLDGIDANKTDP CTLQFLAAPICLLYKNLANKIVPIAIQLNQIPGDENPIFLPSDAKYDWLLAKIWVRSSDF HVHQTITHLLRTHLVSEVFGIAMYRQLPAVHPIFKLLVAHVRFTIAINTKAREQLICECG LFDKANATGGGGHVQMVQRAMKDLTYASLCFPEAIKARGMESKEDIPYYFYRDDGLLVWE AIRTFTAEVVDIYYEGDQVVEEDPELQDFVNDVYVYGMRGRKSSGFPKSVKSREQLSEYL TVVIFTASAQHAAVNFGQYDWCSWIPNAPPTMRAPPPTAKGVVTIEQIVDTLPDRGRSCW HLGAVWALSQFQENELFLGMYPEEHFIEKPVKEAMARFRKNLEAIVSVIAERNKKKQLPY YYLSPDRIPNSVAI |
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Drugs and Mode of Action | |||||
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 545000 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001835) | ||||
Ref 526182 | J 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 527411 | Bioorg Med Chem Lett. 2005 Feb 15;15(4):1083-5.5-Lipoxygenase inhibition by N-hydroxycarbamates in dual-function compounds. | ||||
Ref 527799 | J Med Chem. 2005 Oct 20;48(21):6523-43.Designed multiple ligands. An emerging drug discovery paradigm. | ||||
Ref 528021 | Bioorg Med Chem Lett. 2006 May 1;16(9):2528-31. Epub 2006 Feb 7.Substituted coumarins as potent 5-lipoxygenase inhibitors. | ||||
Ref 528750 | J 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 528805 | J 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 529646 | J 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 530176 | Bioorg 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 530186 | J 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 530239 | Nat Chem Biol. 2009 Aug;5(8):585-92. Epub 2009 Jun 28.Bioactivity-guided mapping and navigation of chemical space. | ||||
Ref 530468 | J Nat Prod. 2009 Oct;72(10):1857-63.Using enzyme assays to evaluate the structure and bioactivity of sponge-derived meroterpenes. | ||||
Ref 530899 | Bioorg Med Chem. 2010 Jun 1;18(11):3910-24. Epub 2010 Apr 18.Synthesis and biological activity of N-aroyl-tetrahydro-gamma-carbolines. | ||||
Ref 534031 | J 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 534335 | J Med Chem. 1997 Feb 28;40(5):819-24.Nonsteroidal anti-inflammatory drugs as scaffolds for the design of 5-lipoxygenase inhibitors. | ||||
Ref 534459 | J 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 534697 | J 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. |
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