Target General Infomation
Target ID
T00140
Former ID
TTDS00112
Target Name
Arachidonate 5-lipoxygenase
Gene Name
ALOX5
Synonyms
5-LO; 5-LOX; 5-lipoxygenase; ALOX5
Target Type
Successful
Disease Atopic dermatitis [ICD9: 691.8, 692.9; ICD10: L00-L99]
Arthritis [ICD9: 710-719; ICD10: M00-M25]
Allergy [ICD9: 995.3; ICD10: T78.4]
Atherosclerosis [ICD9: 414.0, 440; ICD10: I70]
Asthma [ICD10: J45]
Chronic obstructive pulmonary disease [ICD9: 490-492, 494-496; ICD10: J40-J44, J47]
Dermatitis [ICD9: 692.9; ICD10: L20-L30]
Fungal infections [ICD9: 110-118; ICD10: B35-B49]
Inflammatory disease [ICD9: 140-229, 147, 173, 573.3, 710-719; ICD10: C11, C44, K75.9, M00-M25]
Inflammation [ICD10: E08-E13, E10.2, E11, E11.2, E13.2, I73.9, I80-I82, N00-N29, G89]
Lymphatic filariasis [ICD9: 125; ICD10: B74]
Osteoarthritis [ICD9: 715; ICD10: M15-M19, M47]
Pruritus [ICD9: 698; ICD10: L29]
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89]
Psoriasis [ICD9: 696; ICD10: L40]
Rheumatoid arthritis [ICD9: 710-719, 714; ICD10: M05-M06]
Respiratory disease [ICD10: J00-J99]
Rhinitis [ICD9: 472.0, 477; ICD10: J00, J30, J31.0]
Thrombosis [ICD9: 437.6, 453, 671.5, 671.9; ICD10: I80-I82]
Unspecified [ICD code not available]
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
T00140
UniProt ID
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) Diethylcarbamazine Drug Info Approved Lymphatic filariasis [536135], [551871]
Zileuton Drug Info Approved Asthma [536528], [540757]
Silymarin Drug Info Phase 4 Discovery agent [521938]
ABT-761 Drug Info Phase 3 Asthma [526129]
Flobufen Drug Info Phase 3 Rheumatoid arthritis [534411]
FPL-62064 Drug Info Phase 3 Inflammation [531310]
TENIDAP Drug Info Phase 3 Rheumatoid arthritis [529470], [539523]
Darbufelone Drug Info Phase 2/3 Asthma [532278]
CMI-392 Drug Info Phase 2 Psoriasis [526130]
E-6700 Drug Info Phase 2 Asthma [534187]
MK-866 Drug Info Phase 2 Unspecified [1560455]
PF-4191834 Drug Info Phase 2 Asthma [523080]
Rilopirox Drug Info Phase 2 Fungal infections [546060]
SK&F 86002 Drug Info Phase 2 Rheumatoid arthritis [534089], [541296]
TA-270 Drug Info Phase 2 Asthma [546872]
Tepoxalin Drug Info Phase 2 Asthma [534424]
Tipelukast Drug Info Phase 2 Asthma [525273]
UCB-35440 Drug Info Phase 2 Rhinitis [549930]
WY-50295-tromethamine Drug Info Phase 2 Asthma [525487]
BF-389 Drug Info Phase 1 Rheumatoid arthritis [526850]
SKF-105809 Drug Info Phase 1 Pain [529852]
Ibuproxam Drug Info Withdrawn from market Respiratory disease [533573]
Lonapalene Drug Info Discontinued in Phase 3 Psoriasis [545588]
CJ-13610 Drug Info Discontinued in Phase 2 Asthma [468230], [536223]
CV-6504 Drug Info Discontinued in Phase 2 Discovery agent [545370]
DuP-654 Drug Info Discontinued in Phase 2 Pruritus [545553]
E-3040 Drug Info Discontinued in Phase 2 Thrombosis [546036]
E-6080 Drug Info Discontinued in Phase 2 Asthma [545041]
ETH615 Drug Info Discontinued in Phase 2 Dermatitis [546166]
FPL-64170 Drug Info Discontinued in Phase 2 Psoriasis [545854]
Linetastine Drug Info Discontinued in Phase 2 Rhinitis [545155]
MK-591 Drug Info Discontinued in Phase 2 Asthma [544955]
MK-886 Drug Info Discontinued in Phase 2 Asthma [539722], [544532]
MLN-977 Drug Info Discontinued in Phase 2 Chronic obstructive pulmonary disease [546341]
R-68151 Drug Info Discontinued in Phase 2 Psoriasis [545537]
SC-45662 Drug Info Discontinued in Phase 2 Asthma [544863]
TEBUFELONE Drug Info Discontinued in Phase 2 Pain [545171]
AZD-4407 Drug Info Discontinued in Phase 1 Chronic obstructive pulmonary disease [546713]
CD-581 Drug Info Discontinued in Phase 1 Atopic dermatitis [546435]
Licofelone Drug Info Discontinued in Phase 1 Osteoarthritis [545621]
A-78773 Drug Info Terminated Asthma [545524]
A-79175 Drug Info Terminated Asthma [545797]
A-80263 Drug Info Terminated Inflammatory disease [545528]
AA-861 Drug Info Terminated Allergy [544544]
BI-L-357 Drug Info Terminated Asthma [545110]
BU-4601A Drug Info Terminated Asthma [545892]
BW A4C Drug Info Terminated Arthritis [544587]
BW B70C Drug Info Terminated Asthma [545111]
BW755C Drug Info Terminated Inflammatory disease [534109]
CGS 8515 Drug Info Terminated Discovery agent [545304]
CGS-26529 Drug Info Terminated Inflammatory disease [546004]
CI-986 Drug Info Terminated Rheumatoid arthritis [525669]
CMI-206 Drug Info Terminated Inflammatory disease [551572]
Epocarbazolin-A Drug Info Terminated Asthma [534037]
ER-34122 Drug Info Terminated Inflammatory disease [526240], [534759]
KC-11404 Drug Info Terminated Asthma [533776]
KC-11425 Drug Info Terminated Asthma [545947]
LY-221068 Drug Info Terminated Arthritis [545172]
NAFAZATROM Drug Info Terminated Discovery agent [544529]
PD-146176 Drug Info Terminated Atherosclerosis [546784]
R zileuton Drug Info Terminated Asthma [548595]
R-85355 Drug Info Terminated Discovery agent [545061]
REV-5901 Drug Info Terminated Discovery agent [544591]
RWJ-63556 Drug Info Terminated Arthritis [534446]
Sch-40120 Drug Info Terminated Pruritus [545555]
SKF-104351 Drug Info Terminated Rheumatoid arthritis [544770]
WY-28342 Drug Info Terminated Rheumatoid arthritis [545972]
ZD-7717 Drug Info Terminated Asthma [546302]
ZM-230487 Drug Info Terminated Asthma [545870]
Inhibitor 1,2-Dihydro-indazol-3-one Drug Info [529474]
1,2-Dihydroxy-10H-anthracen-9-one Drug Info [534507]
1,3,8-Trihydroxy-6-methyl-10H-anthracen-9-one Drug Info [534507]
1,5-Dihydroxy-10H-anthracen-9-one Drug Info [534507]
1,8,9-Trimethoxy-9,10-dihydro-anthracene Drug Info [534507]
1,8-Dichloro-10H-anthracen-9-one Drug Info [534507]
1,8-Dihydroxy-2-propionyl-10H-anthracen-9-one Drug Info [534507]
1-Benzyl-1,2-dihydro-indazol-3-one Drug Info [529474]
1-furan-2-yl-3-pyridin-2-yl-propenone (FPP-3) Drug Info [536971]
1-Hydroxy-10H-anthracen-9-one Drug Info [534507]
1-Hydroxy-8-methoxy-10H-anthracen-9-one Drug Info [534507]
1-Methyl-1,2-dihydro-indazol-3-one Drug Info [529474]
10-Acetyl-1,8-dihydroxy-10H-anthracen-9-one Drug Info [534507]
10-Benzoyl-1,8-dihydroxy-10H-anthracen-9-one Drug Info [534507]
15-hydroxyeicosatetraenoic acid Drug Info [535027], [538140]
2'-Nitro-biphenyl-4-carboxylic acid hydroxyamide Drug Info [532087]
2-(1H-Indol-3-ylmethyl)-1,2-dihydro-indazol-3-one Drug Info [529474]
2-(3-Phenyl-propyl)-1,2-dihydro-indazol-3-one Drug Info [529474]
2-(4-Butoxy-phenoxy)-N-hydroxy-acetamide Drug Info [532087]
2-(4-Butoxy-phenoxy)-N-hydroxy-N-methyl-acetamide Drug Info [532087]
2-(4-Butoxy-phenoxy)-N-hydroxy-propionamide Drug Info [532087]
2-(4-Butoxy-phenyl)-N-hydroxy-N-methyl-acetamide Drug Info [532087]
2-(4-hydroxylphenyl)-3-(3,5-dihydroxylphenyl) propenoic acid (NNU-hdpa) Drug Info [537200]
2-(4-Methoxy-phenyl)-5-phenyl-thiazol-4-ol Drug Info [531065]
2-(4-Phenyl-butyl)-1,2-dihydro-indazol-3-one Drug Info [529474]
2-Benzyl-1,2-dihydro-indazol-3-one Drug Info [529474]
2-Biphenyl-4-yl-N-hydroxy-N-methyl-acetamide Drug Info [532087]
2-Furan-2-ylmethyl-1,2-dihydro-indazol-3-one Drug Info [529474]
2-Methyl-1,2-dihydro-indazol-3-one Drug Info [529474]
2-Naphthalen-1-ylmethyl-1,2-dihydro-indazol-3-one Drug Info [529474]
2-Naphthalen-2-ylmethyl-1,2-dihydro-indazol-3-one Drug Info [529474]
2-Phenethyl-1,2-dihydro-indazol-3-one Drug Info [529474]
2-Phenyl-1,2-dihydro-indazol-3-one Drug Info [529474]
2-Pyridin-2-ylmethyl-1,2-dihydro-indazol-3-one Drug Info [529474]
2-Pyridin-3-ylmethyl-1,2-dihydro-indazol-3-one Drug Info [529474]
2-Pyridin-4-ylmethyl-1,2-dihydro-indazol-3-one Drug Info [529474]
2-Thiazol-5-ylmethyl-1,2-dihydro-indazol-3-one Drug Info [529474]
2-Thiophen-2-ylmethyl-1,2-dihydro-indazol-3-one Drug Info [529474]
3,4-Dihydroxy-10H-anthracen-9-one Drug Info [534507]
3-(4-Butoxy-phenyl)-N-hydroxy-N-methyl-acrylamide Drug Info [532087]
3-Benzoyl-N-hydroxy-benzamide Drug Info [532087]
3-Biphenyl-3-yl-N-hydroxy-N-methyl-acrylamide Drug Info [532087]
3-Biphenyl-4-yl-N-hydroxy-N-methyl-acrylamide Drug Info [532087]
4,5-Dihydroxy-10H-anthracen-9-one Drug Info [534507]
4,5-Dimethoxy-10H-anthracen-9-one Drug Info [534507]
4-(1H-indol-3-yl)-1-morpholinobutan-1-one Drug Info [528710]
4-Bromo-N-hydroxy-benzamide Drug Info [532087]
4-Butoxy-N-hydroxy-N-methyl-benzamide Drug Info [532087]
4-Hydroxy-5-methoxy-10H-anthracen-9-one Drug Info [534507]
4-Pentadeca-1,3,6-trienylsulfanyl-butyric acid Drug Info [532133]
5-Chloro-N-(4-ethylphenyl)benzo[d]oxazol-2-amine Drug Info [531178]
5-Chloro-N-phenylbenzo[d]oxazol-2-amine Drug Info [531178]
5-Hydroxyeicosatetraenoic acid Drug Info [535027], [538140]
5-Methoxy-N-phenylbenzo[d]oxazol-2-amine Drug Info [531178]
5-Methyl-2-p-tolyl-thiazol-4-ol Drug Info [531065]
5-Methyl-N-phenylbenzo[d]oxazol-2-amine Drug Info [531178]
7-tert-butyl-2, 3-dihydro-3, 3-dimethyl substituted dihydrofuran 30 (DHDMBF30) Drug Info [536698]
A-78773 Drug Info [534630]
A-79175 Drug Info [537871], [538075]
A-80263 Drug Info [550844]
AA-861 Drug Info [536343], [536532], [536917], [537748]
ABT-761 Drug Info [530760], [534862], [535369]
ACACETIN Drug Info [525606]
Acanthus ilicifolius Linn Drug Info [536815]
Acetic acid 2-phenyl-5-propyl-thiazol-4-yl ester Drug Info [531065]
Acetic acid 5-butyl-2-phenyl-thiazol-4-yl ester Drug Info [531065]
Anthracene-2-carboxylic acid hydroxyamide Drug Info [532087]
ANTHRONE Drug Info [534507]
AZD-4407 Drug Info [532630]
BAICALEIN Drug Info [529474]
BI-L-357 Drug Info [534012]
Biphenyl-3-carboxylic acid hydroxyamide Drug Info [532087]
Biphenyl-4-carboxylic acid hydroxyamide Drug Info [532087]
BU-4601A Drug Info [534063]
BUDDLEDIN A Drug Info [525606]
BW A360C Drug Info [536518]
BW A4C Drug Info [536189], [536518], [537431]
BW B218C Drug Info [536518]
BW B70C Drug Info [536518]
BW755C Drug Info [536815]
Caffeic acid Drug Info [535256], [536714], [536829]
CD-581 Drug Info [551871]
CGS 8515 Drug Info [537697]
CGS-26529 Drug Info [534079]
Chebulagic acid Drug Info [537395]
CJ-13610 Drug Info [536223]
CV-6504 Drug Info [535071], [537655]
CYLINDOL A Drug Info [551361]
Diethylcarbamazine Drug Info [534910]
DuP-654 Drug Info [534020]
E-3040 Drug Info [526097]
E-6080 Drug Info [526797]
Epocarbazolin-A Drug Info [534037]
ETH615 Drug Info [535027]
FPL-64170 Drug Info [534226]
Fuscoside Drug Info [535802]
Heme Drug Info [551374]
Hexanoic acid 2,5-diphenyl-thiazol-4-yl ester Drug Info [531065]
Hyperforin Drug Info [535615]
Ibuproxam Drug Info [533474]
ICI 207968 Drug Info [536189]
JUGLONE Drug Info [534507]
L-652,343 Drug Info [537735]
Licofelone Drug Info [535517], [536541], [536548], [536629]
Linetastine Drug Info [535027], [538079]
Lonapalene Drug Info [535027], [537662]
LY-221068 Drug Info [529094]
MK-591 Drug Info [537895], [538006]
MLN-977 Drug Info [544446]
N-(2-Ethylphenyl)-5-methylbenzo[d]oxazol-2-amine Drug Info [531178]
N-(3-Bromophenyl)-5-methoxybenzo[d]oxazol-2-amine Drug Info [531178]
N-(4-Ethylphenyl)-5-methylbenzo[d]oxazol-2-amine Drug Info [531178]
N-(4-Ethylphenyl)benzo[d]oxazol-2-amine Drug Info [531178]
N-Hydroxy-2-methyl-3-naphthalen-2-yl-acrylamide Drug Info [532087]
N-Hydroxy-2-naphthalen-2-yl-acetamide Drug Info [532087]
N-Hydroxy-3-naphthalen-2-yl-acrylamide Drug Info [532087]
N-Hydroxy-3-naphthalen-2-yl-N-p-tolyl-acrylamide Drug Info [532087]
N-Hydroxy-3-naphthalen-2-yl-N-phenyl-acrylamide Drug Info [532087]
N-Hydroxy-3-naphthalen-2-yl-propionamide Drug Info [532087]
N-Hydroxy-3-phenyl-acrylamide Drug Info [532087]
N-hydroxy-4-(naphthalen-1-yl)benzamide Drug Info [532087]
N-Hydroxy-4-iodo-benzamide Drug Info [532087]
N-Hydroxy-4-isobutyl-benzamide Drug Info [532087]
N-Hydroxy-4-naphthalen-2-yl-benzamide Drug Info [532087]
N-Hydroxy-N-methyl-2,3,3-triphenyl-acrylamide Drug Info [532087]
N-Hydroxy-N-methyl-2-naphthalen-2-yl-propionamide Drug Info [532087]
N-Hydroxy-N-methyl-3-naphthalen-1-yl-acrylamide Drug Info [532087]
N-Hydroxy-N-methyl-3-naphthalen-2-yl-acrylamide Drug Info [533474]
N-Hydroxy-N-methyl-3-naphthalen-2-yl-propionamide Drug Info [532087]
N-Hydroxy-N-methyl-3-phenanthren-2-yl-acrylamide Drug Info [532087]
N-Hydroxy-N-methyl-3-phenanthren-3-yl-acrylamide Drug Info [532087]
N-Hydroxy-N-methyl-3-phenanthren-9-yl-acrylamide Drug Info [532087]
N-Hydroxy-N-methyl-benzamide Drug Info [532087]
N-hydroxy-N-[1-(4-isobutylphenyl)ethyl]urea Drug Info [534335]
N-Phenylbenzo[d]oxazol-2-amine Drug Info [531178]
NAFAZATROM Drug Info [532133]
Naphthalene-2-carboxylic acid hydroxyamide Drug Info [532087]
NAPHTHAZALIN Drug Info [534507]
PF-4191834 Drug Info [530836]
Phenanthrene-2-carboxylic acid hydroxyamide Drug Info [532087]
Phenanthrene-3-carboxylic acid hydroxyamide Drug Info [532087]
PHENIDONE Drug Info [551361]
PYROGALLOL Drug Info [534507]
R zileuton Drug Info [526854]
R-68151 Drug Info [535027], [538009]
R-85355 Drug Info [538009]
REV-5901 Drug Info [529474]
Rilopirox Drug Info [529413]
SC-45662 Drug Info [528836]
Silymarin Drug Info [534984]
SK&F 107649 Drug Info [537907]
SK&F 86002 Drug Info [537659]
SKF-105809 Drug Info [529852]
TA-270 Drug Info [526720]
TEBUFELONE Drug Info [534599]
Tepoxalin Drug Info [537990]
TZI-41127 Drug Info [551270]
WY-50295-tromethamine Drug Info [525487]
Zileuton Drug Info [535027], [535474], [536892], [536901], [537073], [537169]
ZM-230487 Drug Info [536489]
Modulator BF-389 Drug Info [526850]
BW-858C Drug Info [534049]
BW-A137C Drug Info
CGS-23885 Drug Info
CI-986 Drug Info [525669]
CMI-206 Drug Info
CMI-392 Drug Info [526130]
Darbufelone Drug Info [532278]
E-6700 Drug Info [534187]
ER-34122 Drug Info [526240], [534759]
Flobufen Drug Info [534411]
FPL-62064 Drug Info [531310]
FR-122788 Drug Info
ICI-211965 Drug Info
KC-11404 Drug Info [533776]
MK-866 Drug Info
MK-886 Drug Info
PD-146176 Drug Info
RWJ-63556 Drug Info [534446]
SB-202235 Drug Info
SC-41661A Drug Info
Sch-40120 Drug Info [526810]
SKF-104351 Drug Info [550942]
TENIDAP Drug Info [529470]
Tipelukast Drug Info
UCB-35440 Drug Info [527359]
WY-28342 Drug Info [533715]
ZD-7717 Drug Info [550946]
Antagonist KC-11425 Drug Info [551926]
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 Vitamin D Receptor Pathway
Arachidonic acid metabolism
Eicosanoid Synthesis
Selenium Micronutrient Network
References
Ref 468230(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: 5169).
Ref 521938ClinicalTrials.gov (NCT00412763) Efficacy of Silymarin for Acute Hepatitis. U.S. National Institutes of Health.
Ref 523080ClinicalTrials.gov (NCT01147458) A Study Of The Safety And Efficacy Of PF-04191834 In Patients With Osteoarthritis Of The Knee. U.S. National Institutes of Health.
Ref 525273ClinicalTrials.gov (NCT02503657) Safety and Tolerability Study in Subjects With Idiopathic Pulmonary Fibrosis (IPF).
Ref 525487WY-50295 tromethamine: a 5-lipoxygenase inhibitor without activity in human whole blood. Prostaglandins Leukot Essent Fatty Acids. 1999 Jan;60(1):31-41.
Ref 525669Role of leukotrienes on coronary vasoconstriction in isolated hearts of arthritic rats: effect of in vivo treatment with CI-986, a dual inhibitor of cyclooxygenase and lipoxygenase. Pharmacology. 2000 Jan;60(1):41-6.
Ref 526129ABT-761 (Abbott). Curr Opin Investig Drugs. 2001 Jan;2(1):68-71.
Ref 526130Anti-inflammatory activities of LDP-392, a dual PAF receptor antagonist and 5-lipoxygenase inhibitor. Pharmacol Res. 2001 Sep;44(3):213-20.
Ref 526240Improvement of dissolution and oral absorption of ER-34122, a poorly water-soluble dual 5-lipoxygenase/cyclooxygenase inhibitor with anti-inflammatory activity by preparing solid dispersion. J Pharm Sci. 2002 Jan;91(1):258-66.
Ref 526850Antiarthritic profile of BF-389--a novel anti-inflammatory agent with low ulcerogenic liability. Agents Actions. 1992 Sep;37(1-2):90-8.
Ref 529470The in vitro free radical scavenging activity of tenidap, a new dual cyclo-oxygenase and 5-1ipoxygenase inhibitor. Mediators Inflamm. 1992;1(2):141-3.
Ref 529852Analgetic activity of SK&F 105809, a dual inhibitor of arachidonic acid metabolism. Agents Actions Suppl. 1991;32:113-7.
Ref 531310FPL 62064, a topically active 5-lipoxygenase/cyclooxygenase inhibitor. Agents Actions. 1990 Jun;30(3-4):432-42.
Ref 532278Novel dual cyclooxygenase and lipoxygenase inhibitors targeting hyaluronan-CD44v6 pathway and inducing cytotoxicity in colon cancer cells. Bioorg Med Chem. 2013 May 1;21(9):2551-9.
Ref 533573Anti-inflammatory agents: determination of ibuproxam and its metabolite humans. Correlation between bioavailability, tolerance and chemico-physical characteristics. Arzneimittelforschung. 1980;30(9):1607-9.
Ref 533776Synthesis, structure-activity relationships, and pharmacological evaluation of pyrrolo[3,2,1-ij]quinoline derivatives: potent histamine and platelet activating factor antagonism and 5-lipoxygenase inhibitory properties. Potential therapeutic application in asthma. J Med Chem. 1995 Feb 17;38(4):669-85.
Ref 534037Epocarbazolins A and B, novel 5-lipoxygenase inhibitors. Taxonomy, fermentation, isolation, structures and biological activities. J Antibiot (Tokyo). 1993 Jan;46(1):25-33.
Ref 534089The effects of antiinflammatory and antiallergic drugs on cytokine release after stimulation of human whole blood by lipopolysaccharide and zymosan A. Inflamm Res. 1995 Jul;44(7):269-74.
Ref 534109BW755C, a dual lipoxygenase/cyclooxygenase inhibitor, reduces mural platelet and neutrophil deposition and vasoconstriction after angioplasty injury in pigs. J Pharmacol Exp Ther. 1996 Apr;277(1):17-21.
Ref 534187Structure-activity relationships of (E)-3-(1,4-benzoquinonyl)-2-[(3-pyridyl)-alkyl]-2-propenoic acid derivatives that inhibit both 5-lipoxygenase and thromboxane A2 synthetase. J Med Chem. 1996 Aug 2;39(16):3148-57.
Ref 534411Pharmacological profile of the novel potent antirheumatic 4-(2',4'-difluorobiphenyl-4-yl)-2-methyl-4-oxobutanoic acid. Arzneimittelforschung. 1997 May;47(5):648-52.
Ref 534424Effects of tepoxalin, a dual inhibitor of cyclooxygenase/5-lipoxygenase, on events associated with NSAID-induced gastrointestinal inflammation. Prostaglandins Leukot Essent Fatty Acids. 1997 Jun;56(6):417-23.
Ref 534446Evaluation of the antiinflammatory activity of a dual cyclooxygenase-2 selective/5-lipoxygenase inhibitor, RWJ 63556, in a canine model of inflammation. J Pharmacol Exp Ther. 1997 Aug;282(2):1094-101.
Ref 534759ER-34122, a novel dual 5-lipoxygenase/cyclooxygenase inhibitor with potent anti-inflammatory activity in an arachidonic acid-induced ear inflammation model. Inflamm Res. 1998 Oct;47(10):375-83.
Ref 536135Opportunities and challenges in antiparasitic drug discovery. Nat Rev Drug Discov. 2005 Sep;4(9):727-40.
Ref 536223Emerging drugs for the treatment of chronic obstructive pulmonary disease. Expert Opin Emerg Drugs. 2006 May;11(2):275-91.
Ref 536528Current and emerging drugs for idiopathic pulmonary fibrosis. Expert Opin Emerg Drugs. 2007 Nov;12(4):627-46.
Ref 539523(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: 2395).
Ref 539722(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: 2655).
Ref 540757(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: 5297).
Ref 541296(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: 6040).
Ref 544529Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000069)
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Ref 548595Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026867)
Ref 549930Clinical pipeline report, company report or official report of UCB.
Ref 551572Cmi206: A potent dual platelet activating factor antagonist and 5-lipoxygenase inhibitor. Bioorganic & Medicinal Chemistry Letters. 03/1995; 5(6):643-648.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 1560455Inhibition of leukotriene synthesis with MK-886 prevents a rise in blood pressure and reduces noradrenaline-evoked contraction in L-NAME-treated rats
Ref 525487WY-50295 tromethamine: a 5-lipoxygenase inhibitor without activity in human whole blood. Prostaglandins Leukot Essent Fatty Acids. 1999 Jan;60(1):31-41.
Ref 525606J Nat Prod. 1999 Sep;62(9):1241-5.Novel and known constituents from Buddleja species and their activity against leukocyte eicosanoid generation.
Ref 525669Role of leukotrienes on coronary vasoconstriction in isolated hearts of arthritic rats: effect of in vivo treatment with CI-986, a dual inhibitor of cyclooxygenase and lipoxygenase. Pharmacology. 2000 Jan;60(1):41-6.
Ref 526097In vitro effects of E3040, a dual inhibitor of 5-lipoxygenase and thromboxane A(2) synthetase, on eicosanoid production. Eur J Pharmacol. 2001 Jun 22;422(1-3):209-16.
Ref 526130Anti-inflammatory activities of LDP-392, a dual PAF receptor antagonist and 5-lipoxygenase inhibitor. Pharmacol Res. 2001 Sep;44(3):213-20.
Ref 526240Improvement of dissolution and oral absorption of ER-34122, a poorly water-soluble dual 5-lipoxygenase/cyclooxygenase inhibitor with anti-inflammatory activity by preparing solid dispersion. J Pharm Sci. 2002 Jan;91(1):258-66.
Ref 526720TA-270 [4-hydroxy-1-methyl-3-octyloxy-7-sinapinoylamino-2(1H)-quinolinone], an anti-asthmatic agent, inhibits leukotriene production induced by IgE receptor stimulation in RBL-2H3 cells. J Pharmacol Exp Ther. 2003 Nov;307(2):583-8. Epub 2003 Sep 11.
Ref 526797Effects of the new 5-lipoxygenase inhibitor E6080 on leukotriene release in vitro. Int Arch Allergy Immunol. 1992;97(4):267-73.
Ref 526810Actions of a 5-lipoxygenase inhibitor, Sch 40120, on acute inflammatory responses. J Pharmacol Exp Ther. 1992 Aug;262(2):721-8.
Ref 526850Antiarthritic profile of BF-389--a novel anti-inflammatory agent with low ulcerogenic liability. Agents Actions. 1992 Sep;37(1-2):90-8.
Ref 526854Mechanism-based inhibition of human liver microsomal cytochrome P450 1A2 by zileuton, a 5-lipoxygenase inhibitor. Drug Metab Dispos. 2003 Nov;31(11):1352-60.
Ref 527359The effect of a novel, dual function histamine H1 receptor antagonist/5-lipoxygenase enzyme inhibitor on in vivo dermal inflammation and extravasation. Eur J Pharmacol. 2005 Jan 4;506(3):265-71. Epub 2004 Dec 1.
Ref 528710Bioorg Med Chem Lett. 2007 May 1;17(9):2414-20. Epub 2007 Feb 17.Indole derivatives as potent inhibitors of 5-lipoxygenase: design, synthesis, biological evaluation, and molecular modeling.
Ref 528836The immunosuppressive properties of enisoprost and a 5-lipoxygenase inhibitor (SC-45662). Transplantation. 1991 Dec;52(6):1053-7.
Ref 529094Anti-inflammatory effects of LY221068 and LY269415. Agents Actions. 1991 Sep;34(1-2):100-2.
Ref 529413Therapy of seborrheic eczema with an antifungal agent with an antiphlogistic effect. Mycoses. 1991;34 Suppl 1:91-3.
Ref 529470The in vitro free radical scavenging activity of tenidap, a new dual cyclo-oxygenase and 5-1ipoxygenase inhibitor. Mediators Inflamm. 1992;1(2):141-3.
Ref 529474J Med Chem. 1991 Mar;34(3):1028-36.Indazolinones, a new series of redox-active 5-lipoxygenase inhibitors with built-in selectivity and oral activity.
Ref 529852Analgetic activity of SK&F 105809, a dual inhibitor of arachidonic acid metabolism. Agents Actions Suppl. 1991;32:113-7.
Ref 530760Treatment with 5-lipoxygenase inhibitor VIA-2291 (Atreleuton) in patients with recent acute coronary syndrome. Circ Cardiovasc Imaging. 2010 May;3(3):298-307.
Ref 530836Pharmacology of PF-4191834, a novel, selective non-redox 5-lipoxygenase inhibitor effective in inflammation and pain. J Pharmacol Exp Ther. 2010 Jul;334(1):294-301.
Ref 531065J Med Chem. 1991 Jul;34(7):2158-65.4-hydroxythiazole inhibitors of 5-lipoxygenase.
Ref 531178Bioorg Med Chem. 2010 Nov 1;18(21):7580-5. Epub 2010 Oct 1.Synthesis and evaluation of benzoxazole derivatives as 5-lipoxygenase inhibitors.
Ref 531310FPL 62064, a topically active 5-lipoxygenase/cyclooxygenase inhibitor. Agents Actions. 1990 Jun;30(3-4):432-42.
Ref 532087J Med Chem. 1990 Mar;33(3):992-8.Hydroxamic acid inhibitors of 5-lipoxygenase: quantitative structure-activity relationships.
Ref 532133J Med Chem. 1990 Apr;33(4):1163-70.Design, synthesis, and 5-lipoxygenase-inhibiting properties of 1-thio-substituted butadienes.
Ref 532278Novel dual cyclooxygenase and lipoxygenase inhibitors targeting hyaluronan-CD44v6 pathway and inducing cytotoxicity in colon cancer cells. Bioorg Med Chem. 2013 May 1;21(9):2551-9.
Ref 532630Palladium catalyzed aryl(alkyl)thiolation of unactivated arenes. Org Lett. 2014 Feb 7;16(3):848-51.
Ref 533474J Med Chem. 1987 Nov;30(11):2121-6.In vivo characterization of hydroxamic acid inhibitors of 5-lipoxygenase.
Ref 533715Synthesis and antiinflammatory activity of certain 5,6,7,8-tetrahydroquinolines and related compounds. J Med Chem. 1995 Apr 28;38(9):1473-81.
Ref 533776Synthesis, structure-activity relationships, and pharmacological evaluation of pyrrolo[3,2,1-ij]quinoline derivatives: potent histamine and platelet activating factor antagonism and 5-lipoxygenase inhibitory properties. Potential therapeutic application in asthma. J Med Chem. 1995 Feb 17;38(4):669-85.
Ref 534012A prodrug of a 2,6-disubstituted 4-(2-arylethenyl)phenol is a selective and orally active 5-lipoxygenase inhibitor. J Pharmacol Exp Ther. 1993 May;265(2):483-9.
Ref 534020The lipoxygenase inhibitor 2-phenylmethyl-1-naphthol (DuP 654) is a 12(S)-hydroxyeicosatetraenoic acid receptor antagonist in the human epidermal cell line SCL-II. Skin Pharmacol. 1993;6(2):148-51.
Ref 534037Epocarbazolins A and B, novel 5-lipoxygenase inhibitors. Taxonomy, fermentation, isolation, structures and biological activities. J Antibiot (Tokyo). 1993 Jan;46(1):25-33.
Ref 534049Effect of BW B70C, a novel inhibitor of arachidonic acid 5-lipoxygenase, on allergen-induced bronchoconstriction and late-phase lung eosinophil accumulation in sensitised guinea-pigs. Agents Actions.1993 Jan;38(1-2):8-18.
Ref 5340635-Hydroxyanthranilic acid derivatives as potent 5-lipoxygenase inhibitors. J Antibiot (Tokyo). 1993 May;46(5):705-11.
Ref 534079CGS 26529: the biological profile of a novel, orally active 5-lipoxygenase inhibitor with an extended duration of action. Inflamm Res. 1995 Aug;44 Suppl 2:S147-8.
Ref 534187Structure-activity relationships of (E)-3-(1,4-benzoquinonyl)-2-[(3-pyridyl)-alkyl]-2-propenoic acid derivatives that inhibit both 5-lipoxygenase and thromboxane A2 synthetase. J Med Chem. 1996 Aug 2;39(16):3148-57.
Ref 534226Selective blockade of leukotriene production by a single dose of the FPL 64170XX 0.5% enema in active ulcerative colitis. Pharmacol Toxicol. 1995 Dec;77(6):371-6.
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 534411Pharmacological profile of the novel potent antirheumatic 4-(2',4'-difluorobiphenyl-4-yl)-2-methyl-4-oxobutanoic acid. Arzneimittelforschung. 1997 May;47(5):648-52.
Ref 534446Evaluation of the antiinflammatory activity of a dual cyclooxygenase-2 selective/5-lipoxygenase inhibitor, RWJ 63556, in a canine model of inflammation. J Pharmacol Exp Ther. 1997 Aug;282(2):1094-101.
Ref 534507J Med Chem. 1997 Nov 7;40(23):3773-80.Simple analogues of anthralin: unusual specificity of structure and antiproliferative activity.
Ref 534599J Med Chem. 1998 Mar 26;41(7):1124-37.New cyclooxygenase-2/5-lipoxygenase inhibitors. 2. 7-tert-butyl-2,3-dihydro-3,3-dimethylbenzofuran derivatives as gastrointestinal safe antiinflammatory and analgesic agents: variations of the dihydrobenzofuran ring.
Ref 534630J Med Chem. 1998 May 21;41(11):1970-9.(+/-)-trans-2-[3-methoxy-4-(4-chlorophenylthioethoxy)-5-(N-methyl-N- hydroxyureidyl)methylphenyl]-5-(3,4, 5-trimethoxyphenyl)tetrahydrofuran (CMI-392), a potent dual 5-lipoxygenase inhibitor and platelet-activating factor receptor antagonist.
Ref 534759ER-34122, a novel dual 5-lipoxygenase/cyclooxygenase inhibitor with potent anti-inflammatory activity in an arachidonic acid-induced ear inflammation model. Inflamm Res. 1998 Oct;47(10):375-83.
Ref 534862N-hydroxyurea and hydroxamic acid inhibitors of cyclooxygenase and 5-lipoxygenase. Bioorg Med Chem Lett. 1999 Apr 5;9(7):979-84.
Ref 534910Inhibition of leukotriene formation by diethylcarbamazine modifies the acid-base balance in the rabbits with blast injuries of the lungs. Vojnosanit Pregl. 1999 May-Jun;56(3):243-7.
Ref 534984Anti-inflammatory and anti-arthritic activities of silymarin acting through inhibition of 5-lipoxygenase. Phytomedicine. 2000 Mar;7(1):21-4.
Ref 535027Preview of potential therapeutic applications of leukotriene B4 inhibitors in dermatology. Skin Pharmacol Appl Skin Physiol. 2000 Sep-Oct;13(5):235-45.
Ref 535071A phase II study of the 5-lipoxygenase inhibitor, CV6504, in advanced pancreatic cancer: correlation of clinical data with pharmacokinetic and pharmacodynamic endpoints. Ann Oncol. 2000 Sep;11(9):1165-70.
Ref 535256Involvement of the 5-lipoxygenase pathway in the neurotoxicity of the prion peptide PrP106-126. J Neurosci Res. 2001 Sep 15;65(6):565-72.
Ref 535369The novel 5-lipoxygenase inhibitor ABT-761 attenuates cerebral vasospasm in a rabbit model of subarachnoid hemorrhage. Neurosurgery. 2001 Nov;49(5):1205-12; discussion 1212-3.
Ref 535474Leukotrienes in respiratory disease. Paediatr Respir Rev. 2001 Sep;2(3):238-44.
Ref 535517Licofelone (ML-3000), a dual inhibitor of 5-lipoxygenase and cyclooxygenase, reduces the level of cartilage chondrocyte death in vivo in experimental dog osteoarthritis: inhibition of pro-apoptotic factors. J Rheumatol. 2002 Jul;29(7):1446-53.
Ref 535615Hyperforin is a dual inhibitor of cyclooxygenase-1 and 5-lipoxygenase. Biochem Pharmacol. 2002 Dec 15;64(12):1767-75.
Ref 535802Fuscoside: an anti-inflammatory marine natural product which selectively inhibits 5-lipoxygenase. Part II: Biochemical studies in the human neutrophil. J Pharmacol Exp Ther. 1992 Aug;262(2):874-82.
Ref 536189Tumour necrosis factor production in a rat airpouch model of inflammation: role of eicosanoids. Agents Actions. 1991 Mar;32(3-4):289-94.
Ref 536223Emerging drugs for the treatment of chronic obstructive pulmonary disease. Expert Opin Emerg Drugs. 2006 May;11(2):275-91.
Ref 536343Characterization and modulation of antigen-induced effects in isolated rat heart. J Cardiovasc Pharmacol. 1991 Oct;18(4):556-65.
Ref 536489Pharmacological nature of nicotine-induced contraction in the rat basilar artery: involvement of arachidonic acid metabolites. Eur J Pharmacol. 2007 Dec 22;577(1-3):109-14. Epub 2007 Aug 14.
Ref 536518Hydroxamic acids and hydroxyureas as novel, selective 5-lipoxygenase inhibitors for possible use in asthma. Agents Actions Suppl. 1991;34:189-99.
Ref 536532Leukotriene B4/leukotriene B4 receptor pathway is involved in hepatic microcirculatory dysfunction elicited by endotoxin. Shock. 2008 Jul;30(1):87-91.
Ref 536541Licofelone, a dual COX/5-LOX inhibitor, induces apoptosis in HCA-7 colon cancer cells through the mitochondrial pathway independently from its ability to affect the arachidonic acid cascade. Carcinogenesis. 2008 Feb;29(2):371-80. Epub 2007 Nov 21.
Ref 536548Activity and potential role of licofelone in the management of osteoarthritis. Clin Interv Aging. 2007;2(1):73-9.
Ref 536629Cyclooxygenase (COX) and 5-lipoxygenase (5-LOX) selectivity of COX inhibitors. Prostaglandins Leukot Essent Fatty Acids. 2008 Feb;78(2):99-108. Epub 2008 Feb 15.
Ref 536698Effect of 5-LOX/COX-2 common inhibitor DHDMBF30 on pancreatic cancer cell Capan2. World J Gastroenterol. 2008 Apr 28;14(16):2494-500.
Ref 536714Protection of mouse brain from aluminum-induced damage by caffeic acid. CNS Neurosci Ther. 2008 Spring;14(1):10-6.
Ref 536815Anti-inflammatory activity of Acanthus ilicifolius. J Ethnopharmacol. 2008 Oct 30;120(1):7-12. Epub 2008 Jul 25.
Ref 536829Phenidone protects the nigral dopaminergic neurons from LPS-induced neurotoxicity. Neurosci Lett. 2008 Nov 7;445(1):1-6. Epub 2008 Aug 22.
Ref 536892Overexpression of 5-lipoxygenase in colon polyps and cancer and the effect of 5-LOX inhibitors in vitro and in a murine model. Clin Cancer Res. 2008 Oct 15;14(20):6525-30.
Ref 536901Oxygen-glucose deprivation activates 5-lipoxygenase mediated by oxidative stress through the p38 mitogen-activated protein kinase pathway in PC12 cells. J Neurosci Res. 2009 Mar;87(4):991-1001.
Ref 536917Platelets stimulate airway smooth muscle cell proliferation through mechanisms involving 5-lipoxygenase and reactive oxygen species. Platelets. 2008 Nov;19(7):528-36.
Ref 536971The anti-angiogenic effects of 1-furan-2-yl-3-pyridin-2-yl-propenone are mediated through the suppression of both VEGF production and VEGF-induced signaling. Vascul Pharmacol. 2009 Mar-Apr;50(3-4):123-31. Epub 2008 Nov 28.
Ref 5370735-lipoxygenase pharmacogenetics in asthma: overlap with Cys-leukotriene receptor antagonist loci. Pharmacogenet Genomics. 2009 Mar;19(3):244-7.
Ref 5371695-lipoxygenase inhibitor zileuton attenuates ischemic brain damage: involvement of matrix metalloproteinase 9. Neurol Res. 2009 Mar 23.
Ref 537200Anti-inflammatory effects and gastrointestinal safety of NNU-hdpa, a novel dual COX/5-LOX inhibitor. Eur J Pharmacol. 2009 Jun 2;611(1-3):100-6. Epub 2009 Apr 1.
Ref 537395Chebulagic acid, a COX-LOX dual inhibitor isolated from the fruits of Terminalia chebula Retz., induces apoptosis in COLO-205 cell line. J Ethnopharmacol. 2009 Jul 30;124(3):506-12. Epub 2009 May 28.
Ref 537431Reactive oxygen species and lipoxygenases regulate the oncogenicity of NPM-ALK-positive anaplastic large cell lymphomas. Oncogene. 2009 Jul 23;28(29):2690-6. Epub 2009 Jun 8.
Ref 537655Involvement of thromboxane A2, leukotrienes and free radicals in puromycin nephrosis in rats. Kidney Int. 1991 May;39(5):920-9.
Ref 537659Therapeutic intervention in a rat model of ARDS: I. Dual inhibition of arachidonic acid metabolism. Circ Shock. 1990 Nov;32(3):231-42.
Ref 537662Pharmacologic and clinical effects of lonapalene (RS 43179), a 5-lipoxygenase inhibitor, in psoriasis. J Invest Dermatol. 1990 Jul;95(1):50-4.
Ref 537697Characterization of CGS 8515 as a selective 5-lipoxygenase inhibitor using in vitro and in vivo models. Biochim Biophys Acta. 1988 Apr 15;959(3):332-42.
Ref 537735Pharmacology of the dual inhibitor of cyclooxygenase and 5-lipoxygenase 3-hydroxy-5-trifluoromethyl-N-(2-(2-thienyl)-2-phenyl-ethenyl)-benzo (b)thiophene-2-carboxamide. Arzneimittelforschung. 1988 Mar;38(3):372-8.
Ref 537748Effect of 5-lipoxygenase inhibitor on experimental delayed cerebral vasospasm. Stroke. 1987 Mar-Apr;18(2):512-8.
Ref 537871Stereoselective metabolism of the 5-lipoxygenase inhibitor A-78773. Ann N Y Acad Sci. 1994 Nov 15;744:262-73.
Ref 537895Inhibition of antigen-induced contraction of guinea-pig airways by a leukotriene synthesis inhibitor, BAY x1005. Eur J Pharmacol. 1994 Jun 2;258(1-2):95-102.
Ref 537907Selective inhibition of 5-lipoxygenase attenuates glomerulonephritis in the rat. Kidney Int. 1994 May;45(5):1301-10.
Ref 537990Preclinical toxicity evaluation of tepoxalin, a dual inhibitor of cyclooxygenase and 5-lipoxygenase, in Sprague-Dawley rats and beagle dogs. Fundam Appl Toxicol. 1996 Sep;33(1):38-48.
Ref 538006Antileukotriene therapy for asthma. Am J Health Syst Pharm. 1996 Dec 1;53(23):2821-30; quiz 2877-8.
Ref 538009Topical R-85355, a potent and selective 5-lipoxygenase inhibitor, fails to improve psoriasis. Skin Pharmacol. 1996;9(5):307-11.
Ref 538075The role of platelet-activating factor (PAF) and the efficacy of ABT-491, a highly potent and selective PAF antagonist, in experimental allergic rhinitis. J Pharmacol Exp Ther. 1998 Jan;284(1):83-8.
Ref 538079Effects of TMK688, a novel anti-allergic drug, on allergic nasal obstruction and exudative responses in sensitized guinea pigs. Naunyn Schmiedebergs Arch Pharmacol. 1997 Dec;356(6):815-9.
Ref 538140Cellular oxygenation of 12-hydroxyeicosatetraenoic acid and 15-hydroxyeicosatetraenoic acid by 5-lipoxygenase is stimulated by 5-lipoxygenase-activating protein. J Biol Chem. 1998 Dec 4;273(49):32842-7.
Ref 544446Inflammation, Cancer and Oxidative Lipoxygenase Activity are Intimately Linked. Cancers (Basel) 2014 September; 6(3): 1500-1521.
Ref 550844CA patent application no. 445634, Acne treatment comprising lipoxygenase inhibitors.
Ref 550942WO patent application no. 2006,1317,37, Method and composition for treating inflammatory disorders.
Ref 550946CA patent application no. 445634, Acne treatment comprising lipoxygenase inhibitors.
Ref 551270Design of pyrrolo-1,4-benzoxazine derivatives as inhibitors of 5-lipoxygenase and PAF antagonists with anthihistaminic properties, Bioorg. Med. Chem. Lett. 4(20):2383-2388 (1994).
Ref 551361Cylindol A, a novel biphenyl ether with 5-lipoxygenase inhibitory activity, and a related compound from Imperata Cylindrica. J Nat Prod. 1994 Sep;57(9):1290-3.
Ref 551374The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 551926WO patent application no. 2002,01223,5, 1,4-dihydropyridines as bradykinin antagonists.
Ref 1587926URL: https://www.ebi.ac.uk/chembl/ The ChEMBL database in 2017

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