Target Information
| Target General Information | Top | |||||
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| Target ID |
T93566
(Former ID: TTDR01369)
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| Target Name |
LOX-5 messenger RNA (ALOX5 mRNA)
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| Synonyms |
LOG5 (mRNA); 5-lipoxygenase (mRNA); 5-LO (mRNA)
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| Gene Name |
ALOX5
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| Target Type |
Discontinued target
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[1] | ||||
| Disease | [+] 3 Target-related Diseases | + | ||||
| 1 | Asthma [ICD-11: CA23] | |||||
| 2 | Pain [ICD-11: MG30-MG3Z] | |||||
| 3 | Rheumatoid arthritis [ICD-11: FA20] | |||||
| Function |
Catalyzes the first step in leukotriene biosynthesis, and thereby plays a role in inflammatory processes.
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| BioChemical Class |
mRNA target
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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 Click to Show/Hide
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| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Discontinued Drug(s) | [+] 3 Discontinued Drugs | + | ||||
| 1 | TEBUFELONE | Drug Info | Discontinued in Phase 2 | Pain | [2] | |
| 2 | ZD-2138 | Drug Info | Discontinued in Phase 2 | Asthma | [3] | |
| 3 | BW A4C | Drug Info | Terminated | Arthritis | [4] | |
| Mode of Action | [+] 1 Modes of Action | + | ||||
| Inhibitor | [+] 45 Inhibitor drugs | + | ||||
| 1 | TEBUFELONE | Drug Info | [5] | |||
| 2 | ZD-2138 | Drug Info | [6] | |||
| 3 | BW A4C | Drug Info | [7] | |||
| 4 | (+)-3,3'-bisdemethyltanegool | Drug Info | [8] | |||
| 5 | (-)-3,3'-bisdemethylpinoresinol | Drug Info | [8] | |||
| 6 | (-)-pinoresinol | Drug Info | [8] | |||
| 7 | (N-(3-phenoxycinnamyl)-acetohydroxamic acid | Drug Info | [9] | |||
| 8 | 1-(4-methoxyphenyl)-3-(1,3,4-thiadiazol-2-yl)urea | Drug Info | [10] | |||
| 9 | 1-(4-methoxyphenyl)-3-(4-methylthiazol-2-yl)urea | Drug Info | [10] | |||
| 10 | 1-(4-methoxyphenyl)-3-(5-methylthiazol-2-yl)urea | Drug Info | [10] | |||
| 11 | 2,4'-Diacetoxy-5,3'-di-(2-propenyl)-biphenyl | Drug Info | [11] | |||
| 12 | 2,4'-Dimethoxy-5,3'-di-(2-propenyl)-biphenyl | Drug Info | [11] | |||
| 13 | 2,4,5-Triarylimidazole analogue | Drug Info | [12] | |||
| 14 | 2-(4-methoxyphenyl)-N-(thiazol-2-yl)acetamide | Drug Info | [10] | |||
| 15 | 2-(benzyloxy)naphthalene | Drug Info | [13] | |||
| 16 | 2-phenyl-N-(1,3,4-thiadiazol-2-yl)acetamide | Drug Info | [10] | |||
| 17 | 2-phenyl-N-(thiazol-2-yl)acetamide | Drug Info | [10] | |||
| 18 | 3,4,5-trimethoxy-N-(thiazol-2-yl)benzamide | Drug Info | [10] | |||
| 19 | 3-methoxy-N-(1,3,4-thiadiazol-2-yl)benzamide | Drug Info | [10] | |||
| 20 | 3-methoxy-N-(4-methylthiazol-2-yl)benzamide | Drug Info | [10] | |||
| 21 | 4'-Methoxy-5,3'-dipropyl-biphenyl-2ol | Drug Info | [11] | |||
| 22 | 4-(dimethylamino)-N-(thiazol-2-yl)benzamide | Drug Info | [10] | |||
| 23 | 4-methoxy-N-(thiazol-2-yl)benzamide | Drug Info | [10] | |||
| 24 | 5,3'-Dipropyl-biphenyl-2,4'-diol | Drug Info | [11] | |||
| 25 | HONOKIOL | Drug Info | [11] | |||
| 26 | ISAINDIGOTONE | Drug Info | [14] | |||
| 27 | Isojaspic acid | Drug Info | [16] | |||
| 28 | JASPAQUINOL | Drug Info | [16] | |||
| 29 | KAEMPFEROL | Drug Info | [8] | |||
| 30 | L-689065 | Drug Info | [17] | |||
| 31 | L-702-539 | Drug Info | [18] | |||
| 32 | L-746530 | Drug Info | [19] | |||
| 33 | Methyl 2-(Benzylamino)-1H-indole-3-carboxylate | Drug Info | [9] | |||
| 34 | Methyl 2-(Diallylamino)-1H-indole-3-carboxylate | Drug Info | [9] | |||
| 35 | METHYLHONOKIOL | Drug Info | [11] | |||
| 36 | N-(1,3,4-thiadiazol-2-yl)benzamide | Drug Info | [10] | |||
| 37 | N-(4-methylthiazol-2-yl)-2-phenylacetamide | Drug Info | [10] | |||
| 38 | N-(4-methylthiazol-2-yl)benzamide | Drug Info | [10] | |||
| 39 | N-(5-methylthiazol-2-yl)-2-phenylacetamide | Drug Info | [10] | |||
| 40 | N-(5-methylthiazol-2-yl)benzamide | Drug Info | [10] | |||
| 41 | N-(thiazol-2-yl)benzamide | Drug Info | [10] | |||
| 42 | N-hydroxy-N-[1-(4-isobutylphenyl)ethyl]urea | Drug Info | [20] | |||
| 43 | PD-169316 | Drug Info | [12] | |||
| 44 | PUUPEHEDIONE | Drug Info | [16] | |||
| 45 | PUUPEHENONE | Drug Info | [16] | |||
| Cell-based Target Expression Variations | Top | |||||
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| Cell-based Target Expression Variations | ||||||
| Drug Property Profile of Target | Top | |
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| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Target Profiles in Patients | Top | |||||
|---|---|---|---|---|---|---|
| Target Expression Profile (TEP) | ||||||
| Target Affiliated Biological Pathways | Top | |||||
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| BioCyc | [+] 6 BioCyc Pathways | + | ||||
| 1 | Aspirin-triggered lipoxin biosynthesis | |||||
| 2 | Resolvin D biosynthesis | |||||
| 3 | Leukotriene biosynthesis | |||||
| 4 | Lipoxin biosynthesis | |||||
| 5 | Aspirin triggered resolvin D biosynthesis | |||||
| 6 | Aspirin triggered resolvin E biosynthesis | |||||
| KEGG Pathway | [+] 5 KEGG Pathways | + | ||||
| 1 | Arachidonic acid metabolism | |||||
| 2 | Metabolic pathways | |||||
| 3 | Serotonergic synapse | |||||
| 4 | Ovarian steroidogenesis | |||||
| 5 | Toxoplasmosis | |||||
| NetPath Pathway | [+] 1 NetPath Pathways | + | ||||
| 1 | IL4 Signaling Pathway | |||||
| Pathwhiz Pathway | [+] 1 Pathwhiz Pathways | + | ||||
| 1 | Arachidonic Acid Metabolism | |||||
| WikiPathways | [+] 3 WikiPathways | + | ||||
| 1 | Arachidonic acid metabolism | |||||
| 2 | Eicosanoid Synthesis | |||||
| 3 | Selenium Micronutrient Network | |||||
| Target-Related Models and Studies | Top | |||||
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| Target Validation | ||||||
| References | Top | |||||
|---|---|---|---|---|---|---|
| REF 1 | Designed multiple ligands. An emerging drug discovery paradigm. J Med Chem. 2005 Oct 20;48(21):6523-43. | |||||
| REF 2 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002346) | |||||
| REF 3 | 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 4 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000230) | |||||
| REF 5 | New cyclooxygenase-2/5-lipoxygenase inhibitors. 3. 7-tert-butyl-2, 3-dihydro-3,3-dimethylbenzofuran derivatives as gastrointestinal safe antiinflam... J Med Chem. 1998 Aug 27;41(18):3515-29. | |||||
| REF 6 | Synthesis and biological activity of N-aroyl-tetrahydro-gamma-carbolines. Bioorg Med Chem. 2010 Jun 1;18(11):3910-24. | |||||
| REF 7 | Novel and potent inhibitors of 5-lipoxygenase product synthesis based on the structure of pirinixic acid. J Med Chem. 2008 Sep 11;51(17):5449-53. | |||||
| REF 8 | Lipoxygenase inhibitory constituents of the fruits of noni (Morinda citrifolia) collected in Tahiti. J Nat Prod. 2007 May;70(5):859-62. | |||||
| REF 9 | Structural optimization and biological evaluation of 2-substituted 5-hydroxyindole-3-carboxylates as potent inhibitors of human 5-lipoxygenase. J Med Chem. 2009 Jun 11;52(11):3474-83. | |||||
| REF 10 | Identification of natural-product-derived inhibitors of 5-lipoxygenase activity by ligand-based virtual screening. J Med Chem. 2007 May 31;50(11):2640-6. | |||||
| REF 11 | Design and synthesis of ten biphenyl-neolignan derivatives and their in vitro inhibitory potency against cyclooxygenase-1/2 activity and 5-lipoxyge... Bioorg Med Chem. 2009 Jul 1;17(13):4459-65. | |||||
| REF 12 | 2,4,5- triarylimidazole inhibitors of IL-1 biosynthesis, Bioorg. Med. Chem. Lett. 5(11):1171-1176 (1995). | |||||
| REF 13 | Bioactivity-guided mapping and navigation of chemical space. Nat Chem Biol. 2009 Aug;5(8):585-92. | |||||
| REF 14 | Inhibition of leukocyte functions by the alkaloid isaindigotone from Isatis indigotica and some new synthetic derivatives. J Nat Prod. 2001 Oct;64(10):1297-300. | |||||
| REF 15 | US patent application no. 5,530,114, Oligonucleotide modulation of arachidonic acid metabolism. | |||||
| REF 16 | Using enzyme assays to evaluate the structure and bioactivity of sponge-derived meroterpenes. J Nat Prod. 2009 Oct;72(10):1857-63. | |||||
| REF 17 | Substituted thiopyrano[2,3,4-c,d]indoles as potent, selective, and orally active inhibitors of 5-lipoxygenase. Synthesis and biological evaluation ... J Med Chem. 1993 Sep 17;36(19):2771-87. | |||||
| REF 18 | Substituted (pyridylmethoxy)naphthalenes as potent and orally active 5-lipoxygenase inhibitors; synthesis, biological profile, and pharmacokinetics... J Med Chem. 1997 Aug 29;40(18):2866-75. | |||||
| REF 19 | Substituted coumarins as potent 5-lipoxygenase inhibitors. Bioorg Med Chem Lett. 2006 May 1;16(9):2528-31. | |||||
| REF 20 | Nonsteroidal anti-inflammatory drugs as scaffolds for the design of 5-lipoxygenase inhibitors. J Med Chem. 1997 Feb 28;40(5):819-24. | |||||
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