Target Information

Target General Infomation
Target ID
T60529
Former ID
TTDS00040
Target Name
Prostaglandin G/H synthase 1
Gene Name
PTGS1
Synonyms
COX-1; Cyclooxygenase -1; Cyclooxygenase-1; PGH synthase 1; PGHS-1; PHS 1; Prostaglandin H2 synthase 1; Prostaglandin-endoperoxide synthase 1; PTGS1
Target Type
Successful
Disease Alzheimer disease [ICD9: 331; ICD10: G30]
Arthritis [ICD9: 710-719; ICD10: M00-M25]
Acne vulgaris; Dermatitis [ICD9:706.1, 692.9; ICD10: L70.0, L20-L30]
Cancer [ICD9: 140-229; ICD10: C00-C96]
Colorectal cancer [ICD9: 153, 154; ICD10: C18-C21]
Dietary shortage [ICD9: 260-269; ICD10: E40-E46]
Diabetic neuropathy [ICD9: 250, 250.6, 356.0, 356.8; ICD10: E11.40]
Dysmenorrhea [ICD9: 625.3; ICD10: N94.4-N94.6]
Gout [ICD9: 274.00274.1274.8274.9; ICD10: M10]
Inflammation [ICD10: E08-E13, E10.2, E11, E11.2, E13.2, I73.9, I80-I82, N00-N29, G89]
Inflammatory disease [ICD9: 140-229, 147, 173, 573.3, 710-719; ICD10: C11, C44, K75.9, M00-M25]
Inflammatory bowel disease [ICD9: 555, 556; ICD10: K50, K51]
Joint and muscular pain; Arthritis; Dysmenorrhea [ICD10: M00-M25, N94]
Miosis during ocular surgery; Dysmenorrhea [ICD9:379.42, 625.3; ICD10: H57.03, N94.4-N94.6]
Neuropathic pain [ICD9: 356.0, 356.8; ICD10: G64, G90.0]
Osteoarthritis; Rheumatoid arthritis [ICD9: 714, 715; ICD10: M05-M06, M15-M19, M47]
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89]
Postoperative inflammation [ICD9: 998; ICD10: T81]
Rheumatold arthritis; Osteoarthritis [ICD9: 714, 715; ICD10: M05-M06, M15-M19, M47]
Type 2 diabetes [ICD9: 250; ICD10: E11]
Ulcerative colitis [ICD9: 556; ICD10: K51]
Unspecified [ICD code not available]
Function
May play an important role in regulating or promoting cell proliferation in some normal and neoplastically transformed cells.
BioChemical Class
Oxidoreductases acting on paired donors
Target Validation
T60529
UniProt ID
P23219
EC Number
EC 1.14.99.1
Sequence
MSRSLLLWFLLFLLLLPPLPVLLADPGAPTPVNPCCYYPCQHQGICVRFGLDRYQCDCTR
TGYSGPNCTIPGLWTWLRNSLRPSPSFTHFLLTHGRWFWEFVNATFIREMLMRLVLTVRS
NLIPSPPTYNSAHDYISWESFSNVSYYTRILPSVPKDCPTPMGTKGKKQLPDAQLLARRF
LLRRKFIPDPQGTNLMFAFFAQHFTHQFFKTSGKMGPGFTKALGHGVDLGHIYGDNLERQ
YQLRLFKDGKLKYQVLDGEMYPPSVEEAPVLMHYPRGIPPQSQMAVGQEVFGLLPGLMLY
ATLWLREHNRVCDLLKAEHPTWGDEQLFQTTRLILIGETIKIVIEEYVQQLSGYFLQLKF
DPELLFGVQFQYRNRIAMEFNHLYHWHPLMPDSFKVGSQEYSYEQFLFNTSMLVDYGVEA
LVDAFSRQIAGRIGGGRNMDHHILHVAVDVIRESREMRLQPFNEYRKRFGMKPYTSFQEL
VGEKEMAAELEELYGDIDALEFYPGLLLEKCHPNSIFGESMIEIGAPFSLKGLLGNPICS
PEYWKPSTFGGEVGFNIVKTATLKKLVCLNTKTCPYVSFRVPDASQDDGPAVERPSTEL
Drugs and Mode of Action
Drug(s) Aminosalicylic Acid Drug Info Approved Inflammatory bowel disease [1]
Balsalazide Drug Info Approved Inflammatory bowel disease [2]
Bromfenac Drug Info Approved Postoperative inflammation [3], [4]
FENBUFEN Drug Info Approved Arthritis [1]
Flufenamic Acid Drug Info Approved Dysmenorrhea [5], [1]
Gamma-Homolinolenic acid Drug Info Approved Dietary shortage [6]
Meclofenamate Sodium Drug Info Approved Joint and muscular pain; Arthritis; Dysmenorrhea [1]
Mesalazine Drug Info Approved Ulcerative colitis [7], [8]
Naproxen Drug Info Approved Osteoarthritis; Rheumatoid arthritis [1]
Piroxicam Drug Info Approved Pain [9], [10]
Salicyclic acid Drug Info Approved Acne vulgaris; Dermatitis [11], [12], [1]
Salsalate Drug Info Approved Rheumatold arthritis; Osteoarthritis [13], [1]
Suprofen Drug Info Approved Miosis during ocular surgery; Dysmenorrhea [14], [15], [1]
IMRECOXIB Drug Info Phase 4 Discovery agent [16]
Curcumin Drug Info Phase 3 Cancer [17], [18]
diclofenac sodium patch Drug Info Phase 3 Unspecified [19]
DOCOSAHEXAENOIC ACID Drug Info Phase 3 Alzheimer disease [20]
ThermoProfen Drug Info Phase 3 Pain [21]
EPICATECHIN Drug Info Phase 2 Discovery agent [22]
Naproxen Drug Info Phase 2 Pain [23], [24]
EXO-230 Drug Info Phase 1/2 Diabetic neuropathy [25]
Bromfenac Drug Info Withdrawn from market Inflammatory disease [4], [1]
INDOPROFEN Drug Info Withdrawn from market Gout [1]
CRx-401 Drug Info Discontinued in Phase 2 Type 2 diabetes [26]
R-KETOPROFEN Drug Info Discontinued in Phase 2 Discovery agent [27]
SRT501 Drug Info Discontinued in Phase 2 Colorectal cancer [28]
TEBUFELONE Drug Info Discontinued in Phase 2 Pain [29]
ATLIPROFEN METHYL ESTER Drug Info Terminated Inflammation [30]
SC-58451 Drug Info Terminated Discovery agent [31]
Inhibitor (-)-3-O-acetylspectaline Drug Info [32]
(11H-Dibenzo[b,e][1,4]dioxepin-2-yl)-acetic acid Drug Info [33]
(11H-Dibenzo[b,e][1,4]dioxepin-7-yl)-acetic acid Drug Info [33]
(11H-Dibenzo[b,e][1,4]dioxepin-8-yl)-acetic acid Drug Info [33]
(3-Chloro-4-Propoxy-Phenyl)-Acetic Acid Drug Info [34]
(R)-2-(4-Isobutyl-phenyl)-N-phenyl-propionamide Drug Info [35]
(S)-FLURBIPROFEN Drug Info [35]
(Z)-2'-des-methyl sulindac sulfide Drug Info [36]
1,2-dihydro-3-(2,3,4-trimethoxyphenyl)naphthalene Drug Info [37]
1-(4-(methylsulfonyl)phenyl)-3-p-tolylurea Drug Info [38]
1-(4-(methylsulfonyl)phenyl)-3-phenylurea Drug Info [38]
1-(4-aminosulfonylphenyl)-2-(2-pyridyl)acetylene Drug Info [39]
1-(4-aminosulfonylphenyl)-2-(4-pyridyl)acetylene Drug Info [39]
2'-epi-guianin Drug Info [40]
2,4'-Dimethoxy-5,3'-di-(2-propenyl)-biphenyl Drug Info [41]
2-(1,1'-Biphenyl-4-Yl)Propanoic Acid Drug Info [34]
2-(2,3,4-trimethoxyphenyl)-1H-indene Drug Info [37]
2-(2-(2,6-dimethylphenylamino)phenyl)acetic acid Drug Info [42]
2-(2-methoxyphenyl)-1H-indene Drug Info [37]
2-(2-Methylpropanoyl)-1,3,5-benzenetriol Drug Info [43]
2-(3'-Allyl-biphenyl-4-yl)-propionic acid Drug Info [44]
2-(3'-Ethyl-biphenyl-4-yl)-propionic acid Drug Info [44]
2-(3'-Ethylsulfanyl-biphenyl-4-yl)-propionic acid Drug Info [44]
2-(3'-Vinyl-biphenyl-4-yl)-propionic acid Drug Info [44]
2-(3-Phenyl-propyl)-1,2-dihydro-indazol-3-one Drug Info [45]
2-(N-(2-Ffuorophenyl)pyrrol-3-yl) acetic acid Drug Info [46]
2-(N-(2-fluorophenyl)pyrrol-2-yl) acetic acid Drug Info [46]
2-(p-Methylsulfonylbenzoyl)furan Drug Info [47]
2-Benzyl-1,2-dihydro-indazol-3-one Drug Info [45]
2-Bromoacetyl Group Drug Info [48]
2-Furan-2-ylmethyl-1,2-dihydro-indazol-3-one Drug Info [45]
2-Methyl-1,2-dihydro-indazol-3-one Drug Info [45]
2-Naphthalen-2-ylmethyl-1,2-dihydro-indazol-3-one Drug Info [45]
2-Phenethyl-1,2-dihydro-indazol-3-one Drug Info [45]
2-Phenyl-1,2-dihydro-indazol-3-one Drug Info [45]
2-[4-(1H-Indol-5-yl)-phenyl]-propionic acid Drug Info [44]
3 beta-O-acetyloleanolic acid Drug Info [49]
3-(4-Methanesulfonyl-phenyl)-1-phenyl-propynone Drug Info [50]
4'-Methoxy-5,3'-dipropyl-biphenyl-2ol Drug Info [41]
4,5-Bis(4-chlorophenyl)-1,2-selenazole Drug Info [51]
4,5-Bis(4-chlorophenyl)isothiazole Drug Info [52]
4,5-Bis(4-methoxyphenyl)-1,2-selenazole Drug Info [51]
4,5-Bis(4-methoxyphenyl)-3H-1,2-dithiol-3-one Drug Info [52]
4,5-Bis(4-methoxyphenyl)-3H-1,2-dithiole-3-thione Drug Info [52]
4,5-Bis(4-methoxyphenyl)isothiazole Drug Info [52]
4-(4-Chlorophenyl)-5-(4-methoxyphenyl)isothiazole Drug Info [52]
4-(4-Chlorophenyl)-5-p-tolyl-1,2-selenazole Drug Info [51]
4-(4-Chlorophenyl)-5-p-tolyl-3H-1,2-dithiol-3-one Drug Info [52]
4-(4-Chlorophenyl)-5-p-tolylisothiazole Drug Info [52]
4-(5-(4-Hydroxyphenyl)isothiazol-4-yl)phenol Drug Info [52]
4-amino-N-(2-chlorophenyl)benzenesulfonamide Drug Info [53]
4-amino-N-(4-chlorophenyl)benzenesulfonamide Drug Info [53]
4-amino-N-p-tolylbenzenesulfonamide Drug Info [53]
5,3'-Dipropyl-biphenyl-2,4'-diol Drug Info [41]
5-(2-1H-indenyl)-1,3-benzodioxole Drug Info [37]
5-(2-Imidazol-1-yl-ethyl)-7,8-dihydro-quinoline Drug Info [54]
5-(4-Chlorophenyl)-4-(4-methoxyphenyl)isothiazole Drug Info [52]
5-(4-Chlorophenyl)-4-p-tolyl-1,2-selenazole Drug Info [51]
5-(4-Chlorophenyl)-4-p-tolyl-3H-1,2-dithiol-3-one Drug Info [52]
5-(4-Chlorophenyl)-4-p-tolylisothiazole Drug Info [52]
5-(4-Methoxyphenyl)-4-p-tolyl-1,2-selenazole Drug Info [51]
5-(4-Methoxyphenyl)-4-p-tolylisothiazole Drug Info [52]
5-Ethyl-3,4-diphenyl-isoxazole Drug Info [55]
5-Methyl-3,4-diphenyl-isoxazole Drug Info [55]
5-Phenyl-pentanoic acid benzyl-hydroxy-amide Drug Info [56]
Acetic acid 2-hept-2-ynylsulfanyl-phenyl ester Drug Info [57]
Acetic acid 2-hept-3-ynylsulfanyl-phenyl ester Drug Info [57]
Acetic acid 2-heptylselanyl-phenyl ester Drug Info [57]
Acetic acid 2-heptylsulfanyl-phenyl ester Drug Info [57]
Acetic acid 2-hex-2-ynylsulfanyl-phenyl ester Drug Info [57]
Acetic acid 2-hexylsulfanyl-phenyl ester Drug Info [57]
Acetic acid 2-pentylsulfanyl-phenyl ester Drug Info [57]
Acetic Acid Salicyloyl-Amino-Ester Drug Info [34]
Alpha-D-Mannose Drug Info [48]
Alpha-Methyl-4-biphenyl-acetic acid Drug Info [58]
Arachidonic Acid Drug Info [48]
B-Octylglucoside Drug Info [48]
Balsalazide Drug Info [59]
Beta-D-Glucose Drug Info [48]
Beta-D-Mannose Drug Info [48]
Bromfenac Drug Info [60]
CATECHIN Drug Info [61]
CRx-401 Drug Info [62]
Curcumin Drug Info [63]
DEMETHOXYCURCUMIN Drug Info [63]
DOCOSAHEXAENOIC ACID Drug Info [64]
EPICATECHIN Drug Info [61]
FENBUFEN Drug Info [65]
Flufenamic Acid Drug Info [66]
FR122047 Drug Info [67]
Gamma-Homolinolenic acid Drug Info [68], [69], [70]
Heme Drug Info [34]
HONOKIOL Drug Info [41]
Hyperforin Drug Info [71]
IMRECOXIB Drug Info [72]
INDOPROFEN Drug Info [35]
IODOINDOMETHACIN Drug Info [58]
IODOSUPROFEN Drug Info [58]
Mesalazine Drug Info [73]
METHYLHONOKIOL Drug Info [41]
N-(1H-indazol-5-yl)acetamide Drug Info [74]
N-(3-(phenylthio)pyridin-4-yl)methanesulfonamide Drug Info [75]
N-(3-phenoxy-4-pyridinyl)ethanesulfonamide Drug Info [76]
N-(3-phenoxy-4-pyridinyl)propanesulfonamide Drug Info [76]
N-(3-phenoxypyridin-4-yl)methanesulfonamide Drug Info [75]
N-(3-phenylamino-4-pyridinyl)methanesulfonamide Drug Info [75]
Naproxen Drug Info [77]
O-Acetylserine Drug Info [48]
Oxametacin Drug Info [78]
P-(2'-Iodo-5'-Thenoyl)Hydrotropic Acid Drug Info [34]
PHENIDONE Drug Info [45]
Prifelone Drug Info [79]
Primary alcohol metabolite of celecoxib Drug Info [80]
Protoporphyrin Ix Containing Co Drug Info [48]
R-KETOPROFEN Drug Info [35]
RESORCINOL Drug Info [61]
Resveratrol Potassium3-Sulfate Drug Info [81]
Resveratrol Potassium4,-Sulfate Drug Info [81]
Salicyclic acid Drug Info [82]
Salsalate Drug Info [83], [84]
SC-560 Drug Info [85]
SC-58451 Drug Info [86]
Suprofen Drug Info [87]
TEBUFELONE Drug Info [88]
ThermoProfen Drug Info [89]
TRL-382 Drug Info [90]
Modulator Aminosalicylic Acid Drug Info [91]
ATLIPROFEN METHYL ESTER Drug Info [91]
diclofenac sodium patch Drug Info
Meclofenamate Sodium Drug Info
Nitroflurbiprofen Drug Info
Piroxicam Drug Info [91]
SRT501 Drug Info [92]
Agonist EXO-230 Drug Info [93]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
BioCyc Pathway C20 prostanoid biosynthesis
KEGG Pathway Arachidonic acid metabolism
Metabolic pathways
Platelet activation
Serotonergic synapse
NetPath Pathway TGF_beta_Receptor Signaling Pathway
PANTHER Pathway Inflammation mediated by chemokine and cytokine signaling pathway
PathWhiz Pathway Arachidonic Acid Metabolism
WikiPathways Prostaglandin Synthesis and Regulation
Arachidonic acid metabolism
Phase 1 - Functionalization of compounds
Eicosanoid Synthesis
Selenium Micronutrient Network
References
REF 1Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
REF 2FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 077806.
REF 3FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 021664.
REF 4(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: 7131).
REF 5(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: 2447).
REF 6Treatment of rheumatoid arthritis with gammalinolenic acid. Ann Intern Med. 1993 Nov 1;119(9):867-73.
REF 7(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: 4655).
REF 8BiDil: assessing a race-based pharmaceutical. Ann Fam Med. 2006 Nov-Dec;4(6):556-60.
REF 9FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 073535.
REF 10(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: 7273).
REF 11(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: 4306).
REF 12Drug information of Salicyclic acid, 2008. eduDrugs.
REF 13Drug information of Salsalate, 2008. eduDrugs.
REF 14(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: 7298).
REF 15Drug information of Suprofen, 2008. eduDrugs.
REF 16ClinicalTrials.gov (NCT01985165) A Phase 4 Study of Imrecoxib in Treatment of Knee Osteoarthritis. U.S. National Institutes of Health.
REF 17Nanocurcumin: a promising therapeutic advancement over native curcumin. Crit Rev Ther Drug Carrier Syst. 2013;30(4):331-68.
REF 18(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: 7000).
REF 19Diclofenac: an update on its mechanism of action and safety profile.Curr Med Res Opin.2010 Jul;26(7):1715-31.
REF 20(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: 1051).
REF 21ClinicalTrials.gov (NCT00488267) Efficacy of ThermoProfen in Patients With Mild to Moderate Pain Associated With Osteoarthritis of the Knee. U.S. National Institutes of Health.
REF 22ClinicalTrials.gov (NCT01690676) Effect of an Apple Polyphenol Extract on Brachial Artery Flow-mediated Vasodilatory Function. U.S. National Institutes of Health.
REF 23(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: 5230).
REF 24ClinicalTrials.gov (NCT01139190) Clinical Trial Evaluating Gastrointestinal Damage Following Administration PL3100 or Naproxen in At-Risk Adults. U.S. National Institutes of Health.
REF 25ClinicalTrials.gov (NCT00544934) Multiple Dose Trial of Anti-glycation Agent GLY-230 in Healthy and Diabetic Subjects. U.S. National Institutes of Health.
REF 26Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018957)
REF 27Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007136)
REF 28Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018787)
REF 29Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002346)
REF 30Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000964)
REF 31Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006812)
REF 32J Nat Prod. 2007 Dec;70(12):2026-8. Epub 2007 Nov 30.Lipoperoxidation and cyclooxygenase enzyme inhibitory piperidine alkaloids from Cassia spectabilis green fruits.
REF 33J Med Chem. 1986 Aug;29(8):1436-41.Synthesis and antiinflammatory/analgesic activities of 11H-dibenzo[b, e,][1,4]dioxepinacetic acids.
REF 34The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
REF 35J Med Chem. 2005 Jun 30;48(13):4312-31.2-Arylpropionic CXC chemokine receptor 1 (CXCR1) ligands as novel noncompetitive CXCL8 inhibitors.
REF 36Bioorg Med Chem Lett. 2009 Jun 15;19(12):3271-4. Epub 2009 Apr 23.The influence of double bond geometry in the inhibition of cyclooxygenases by sulindac derivatives.
REF 37Bioorg Med Chem. 2007 Sep 15;15(18):6109-18. Epub 2007 Jun 20.'Bridged' stilbene derivatives as selective cyclooxygenase-1 inhibitors.
REF 38Bioorg Med Chem Lett. 2008 Feb 15;18(4):1336-9. Epub 2008 Jan 11.Design and synthesis of 1,3-diarylurea derivatives as selective cyclooxygenase (COX-2) inhibitors.
REF 39Bioorg Med Chem. 2008 Feb 15;16(4):1948-56. Epub 2007 Nov 5.Synthesis and cyclooxygenase inhibitory activities of linear 1-(methanesulfonylphenyl or benzenesulfonamido)-2-(pyridyl)acetylene regioisomers.
REF 40Bioorg Med Chem Lett. 2009 Dec 15;19(24):6922-5. Epub 2009 Oct 20.COX, LOX and platelet aggregation inhibitory properties of Lauraceae neolignans.
REF 41Bioorg 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 42J Biol Chem. 2007 Jun 1;282(22):16379-90. Epub 2007 Apr 12.Molecular determinants for the selective inhibition of cyclooxygenase-2 by lumiracoxib.
REF 43J Nat Prod. 2005 Oct;68(10):1545-8.Anti-inflammatory acylphloroglucinol derivatives from Hops (Humulus lupulus).
REF 44Bioorg Med Chem Lett. 1999 Feb 8;9(3):307-12.Structure-based design of COX-2 selectivity into flurbiprofen.
REF 45J 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 46Bioorg Med Chem. 2007 Jul 15;15(14):4876-90. Epub 2007 May 3.Synthesis and biological activity of new anti-inflammatory compounds containing the 1,4-benzodioxine and/or pyrrole system.
REF 47J Med Chem. 2010 Sep 23;53(18):6560-71.Synthesis, anti-inflammatory activity, and in vitro antitumor effect of a novel class of cyclooxygenase inhibitors: 4-(aryloyl)phenyl methyl sulfones.
REF 48How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
REF 49J Nat Prod. 2006 Jun;69(6):887-90.Nitrogen-containing phorbol esters from Croton ciliatoglandulifer and their effects on cyclooxygenases-1 and -2.
REF 50Bioorg Med Chem Lett. 2005 Nov 1;15(21):4842-5.Synthesis and biological evaluation of 1,3-diphenylprop-2-yn-1-ones as dual inhibitors of cyclooxygenases and lipoxygenases.
REF 51Eur J Med Chem. 2008 Jun;43(6):1152-9. Epub 2007 Sep 22.Investigations concerning the COX/5-LOX inhibiting and hydroxyl radical scavenging potencies of novel 4,5-diaryl isoselenazoles.
REF 52Bioorg Med Chem. 2009 Jan 15;17(2):558-68. Epub 2008 Dec 6.Diaryl-dithiolanes and -isothiazoles: COX-1/COX-2 and 5-LOX-inhibitory, *OH scavenging and anti-adhesive activities.
REF 53Bioorg Med Chem. 2007 Jan 15;15(2):1014-21. Epub 2006 Oct 18.Analgesic agents without gastric damage: design and synthesis of structurally simple benzenesulfonanilide-type cyclooxygenase-1-selectiveinhibitors.
REF 54J Med Chem. 2000 May 4;43(9):1841-51.1-imidazolyl(alkyl)-substituted di- and tetrahydroquinolines and analogues: syntheses and evaluation of dual inhibitors of thromboxane A(2) synthase and aromatase.
REF 55J Med Chem. 2004 Sep 23;47(20):4881-90.Novel synthesis of 3,4-diarylisoxazole analogues of valdecoxib: reversal cyclooxygenase-2 selectivity by sulfonamide group removal.
REF 56J Med Chem. 1989 Aug;32(8):1836-42.Differential effects of a series of hydroxamic acid derivatives on 5-lipoxygenase and cyclooxygenase from neutrophils and 12-lipoxygenase from platelets and their in vivo effects on inflammation and anaphylaxis.
REF 57J Med Chem. 1998 Nov 19;41(24):4800-18.Covalent modification of cyclooxygenase-2 (COX-2) by 2-acetoxyphenyl alkyl sulfides, a new class of selective COX-2 inactivators.
REF 58Bioorg Med Chem. 2010 Mar 15;18(6):2204-18. Epub 2010 Feb 8.In silico search for multi-target anti-inflammatories in Chinese herbs and formulas.
REF 59Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.
REF 60Comparison of cyclooxygenase inhibitory activity and ocular anti-inflammatory effects of ketorolac tromethamine and bromfenac sodium. Curr Med Res Opin. 2006 Jun;22(6):1133-40.
REF 61J Nat Prod. 2004 Nov;67(11):1777-82.Mechanism-based inactivation of COX-1 by red wine m-hydroquinones: a structure-activity relationship study.
REF 62ClinicalTrials.gov (NCT00506298) Study of CRx-401 on Glucose Levels in Subjects With Type II Diabetes. U.S. National Institutes of Health.
REF 63Bioorg Med Chem Lett. 2005 Apr 1;15(7):1793-7.Design, synthesis, biological evaluation and molecular docking of curcumin analogues as antioxidant, cyclooxygenase inhibitory and anti-inflammatory agents.
REF 64J Nat Prod. 2001 Jun;64(6):745-9.Cox-2 inhibitory effects of naturally occurring and modified fatty acids.
REF 65Eur J Med Chem. 2009 Sep;44(9):3798-804. Epub 2009 Apr 14.Fenbufen based 3-[5-(substituted aryl)-1,3,4-oxadiazol-2-yl]-1-(biphenyl-4-yl)propan-1-ones as safer antiinflammatory and analgesic agents.
REF 66Ouellet M, Percival MD: Effect of inhibitor time-dependency on selectivity towards cyclooxygenase isoforms. Biochem J. 1995 Feb 15;306 ( Pt 1):247-51.
REF 67The analgesic effect profile of FR122047, a selective cyclooxygenase-1 inhibitor, in chemical nociceptive models. Eur J Pharmacol. 2000 Mar 10;391(1-2):49-54.
REF 68Mutational and X-ray crystallographic analysis of the interaction of dihomo-gamma -linolenic acid with prostaglandin endoperoxide H synthases. J Biol Chem. 2001 Mar 30;276(13):10358-65. Epub 2000 Dec 19.
REF 69Structure of eicosapentaenoic and linoleic acids in the cyclooxygenase site of prostaglandin endoperoxide H synthase-1. J Biol Chem. 2001 Oct 5;276(40):37547-55. Epub 2001 Jul 27.
REF 70Differential metabolism of dihomo-gamma-linolenic acid and arachidonic acid by cyclo-oxygenase-1 and cyclo-oxygenase-2: implications for cellular synthesis of prostaglandin E1 and prostaglandin E2. Biochem J. 2002 Jul 15;365(Pt 2):489-96.
REF 71Hyperforin is a dual inhibitor of cyclooxygenase-1 and 5-lipoxygenase. Biochem Pharmacol. 2002 Dec 15;64(12):1767-75.
REF 72Bioorg Med Chem Lett. 2009 Apr 15;19(8):2270-2. Epub 2009 Feb 27.Synthesis and anti-inflammatory activity of the major metabolites of imrecoxib.
REF 73How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
REF 74J Med Chem. 2008 Dec 25;51(24):7800-5.New analgesics synthetically derived from the paracetamol metabolite N-(4-hydroxyphenyl)-(5Z,8Z,11Z,14Z)-icosatetra-5,8,11,14-enamide.
REF 75J Med Chem. 2009 Oct 8;52(19):5864-71.Pyridine analogues of nimesulide: design, synthesis, and in vitro and in vivo pharmacological evaluation as promising cyclooxygenase 1 and 2 inhibitors.
REF 76J Med Chem. 2004 Dec 30;47(27):6749-59.Design, synthesis, and pharmacological evaluation of pyridinic analogues of nimesulide as cyclooxygenase-2 selective inhibitors.
REF 77Comparative inhibitory activity of rofecoxib, meloxicam, diclofenac, ibuprofen, and naproxen on COX-2 versus COX-1 in healthy volunteers. J Clin Pharmacol. 2000 Oct;40(10):1109-20.
REF 78J Med Chem. 2007 Dec 13;50(25):6367-82. Epub 2007 Nov 10.Structure-based design, synthesis, and biological evaluation of indomethacin derivatives as cyclooxygenase-2 inhibiting nitric oxide donors.
REF 79J Med Chem. 2005 Oct 20;48(21):6523-43.Designed multiple ligands. An emerging drug discovery paradigm.
REF 80Bioorg Med Chem. 2008 Nov 15;16(22):9694-8. Epub 2008 Oct 5.Diazen-1-ium-1,2-diolated nitric oxide donor ester prodrugs of 5-(4-hydroxymethylphenyl)-1-(4-aminosulfonylphenyl)-3-trifluoromethyl-1H-pyrazole and its methanesulfonyl analog: synthesis, biological evaluation and nitric oxide release studies.
REF 81J Med Chem. 2010 Jul 8;53(13):5033-43.Selective synthesis and biological evaluation of sulfate-conjugated resveratrol metabolites.
REF 82The C50T polymorphism of the cyclooxygenase-1 gene and the risk of thrombotic events during low-dose therapy with acetyl salicylic acid. Thromb Haemost. 2008 Jul;100(1):70-5.
REF 83Aspirin and NSAID sensitivity. Immunol Allergy Clin North Am. 2004 Aug;24(3):491-505, vii.
REF 84New non-steroidal anti-rheumatic drugs: selective inhibitors of inducible cyclooxygenase. Med Klin (Munich). 1998 Jul 15;93(7):407-15.
REF 85J Med Chem. 2005 Oct 6;48(20):6400-8.Synthesis and antiinflammatory activity of coumarin derivatives.
REF 86Novel 1,2-diarylcyclobutenes: Selective and orally active cox-2 inhibitors, Bioorg. Med. Chem. Lett. 6(22):2677-2682 (1996).
REF 87Differential binding mode of diverse cyclooxygenase inhibitors. J Mol Graph Model. 2002 Mar;20(5):359-71.
REF 88J 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 89Topical NSAID therapy for musculoskeletal pain. Pain Med. 2010 Apr;11(4):535-49.
REF 90(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. (Target id: 1375).
REF 91Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
REF 92Resveratrol is a peroxidase-mediated inactivator of COX-1 but not COX-2: a mechanistic approach to the design of COX-1 selective agents. J Biol Chem. 2004 May 21;279(21):22727-37. Epub 2004 Mar 12.
REF 93Inhibiting Amadori-modified albumin formation improves biomarkers of podocyte damage in diabetic rats. Physiol Rep. 2013 September; 1(4): e00083.

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.