Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTVKILB)

• DTT Name: Prostaglandin G/H synthase 2 (COX-2)
• Synonyms: Prostaglandin-endoperoxide synthase 2; Prostaglandin H2 synthase 2; PHS II; PGHS-2; PGH synthase 2; Cyclooxygenase-2; COX2; COX-2
• Gene Name: PTGS2
• DTT Type: Successful target; [1]
• BioChemical Class: Paired donor oxygen oxidoreductase
• UniProt ID: PGH2_HUMAN
• TTD ID: T66665
• EC Number: EC 1.14.99.1
• Sequence:
  MLARALLLCAVLALSHTANPCCSHPCQNRGVCMSVGFDQYKCDCTRTGFYGENCSTPEFL
  TRIKLFLKPTPNTVHYILTHFKGFWNVVNNIPFLRNAIMSYVLTSRSHLIDSPPTYNADY
  GYKSWEAFSNLSYYTRALPPVPDDCPTPLGVKGKKQLPDSNEIVEKLLLRRKFIPDPQGS
  NMMFAFFAQHFTHQFFKTDHKRGPAFTNGLGHGVDLNHIYGETLARQRKLRLFKDGKMKY
  QIIDGEMYPPTVKDTQAEMIYPPQVPEHLRFAVGQEVFGLVPGLMMYATIWLREHNRVCD
  VLKQEHPEWGDEQLFQTSRLILIGETIKIVIEDYVQHLSGYHFKLKFDPELLFNKQFQYQ
  NRIAAEFNTLYHWHPLLPDTFQIHDQKYNYQQFIYNNSILLEHGITQFVESFTRQIAGRV
  AGGRNVPPAVQKVSQASIDQSRQMKYQSFNEYRKRFMLKPYESFEELTGEKEMSAELEAL
  YGDIDAVELYPALLVEKPRPDAIFGETMVEVGAPFSLKGLMGNVICSPAYWKPSTFGGEV
  GFQIINTASIQSLICNNVKGCPFTSFSVPDPELIKTVTINASSSRSGLDDINPTVLLKER
  STEL
• Function: Converts arachidonate to prostaglandin H2 (PGH2), a committed step in prostanoid synthesis. Constitutively expressed in some tissues in physiological conditions, such as the endothelium, kidney and brain, and in pathological conditions, such as in cancer. PTGS2 is responsible for production of inflammatory prostaglandins. Up-regulation of PTGS2 is also associated with increased cell adhesion, phenotypic changes, resistance to apoptosis and tumor angiogenesis. In cancer cells, PTGS2 is a key step in the production of prostaglandin E2 (PGE2), which plays important roles in modulating motility, proliferation and resistance to apoptosis. During neuroinflammation, plays a role in neuronal secretion of specialized preresolving mediators (SPMs), especially 15-R-lipoxin A4, that regulates phagocytic microglia (By similarity).
• KEGG Pathway:
  Arachidonic acid metabolism (hsa00590)
  Metabolic pathways (hsa01100)
  NF-kappa B signaling pathway (hsa04064)
  VEGF signaling pathway (hsa04370)
  TNF signaling pathway (hsa04668)
  Retrograde endocannabinoid signaling (hsa04723)
  Serotonergic synapse (hsa04726)
  Ovarian steroidogenesis (hsa04913)
  Oxytocin signaling pathway (hsa04921)
  Regulation of lipolysis in adipocytes (hsa04923)
  Leishmaniasis (hsa05140)
  Pathways in cancer (hsa05200)
  Chemical carcinogenesis (hsa05204)
  MicroRNAs in cancer (hsa05206)
  Small cell lung cancer (hsa05222)
• Reactome Pathway:
  Synthesis of 15-eicosatetraenoic acid derivatives (R-HSA-2142770)
  Synthesis of Prostaglandins (PG) and Thromboxanes (TX) (R-HSA-2162123)
  Interleukin-10 signaling (R-HSA-6783783)
  Interleukin-4 and Interleukin-13 signaling (R-HSA-6785807)
  Biosynthesis of DHA-derived SPMs (R-HSA-9018677)
  Biosynthesis of EPA-derived SPMs (R-HSA-9018679)
  Biosynthesis of DPAn-3 SPMs (R-HSA-9025094)
  Biosynthesis of electrophilic Omega-3 PUFA oxo-derivatives (R-HSA-9027604)
  Nicotinamide salvaging (R-HSA-197264)
• BioCyc Pathway: MetaCyc:HS01115-MON

Molecular Interaction Atlas (MIA) of This DTT

27 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Aminosalicylic Acid	DMENSL5	Crohn disease	DD70	Approved	[2]
Carprofen	DMHMP05	Pain	MG30-MG3Z	Approved	[3]
Celecoxib	DM6LOQU	Dysmenorrhea	GA34.3	Approved	[4]
Diflunisal	DM7EN8I	Osteoarthritis	FA00-FA05	Approved	[1]
Eicosapentaenoic acid/docosa-hexaenoic acid	DMMUCG4	Hypertriglyceridemia	5C80.1	Approved	[5]
Etodolac	DM6WJO9	Osteoarthritis	FA00-FA05	Approved	[6]
Etoricoxib	DM6A4NW	Rheumatoid arthritis	FA20	Approved	[7]
FENBUFEN	DMXGDFK	Arthritis	FA20	Approved	[8]
Flufenamic Acid	DMC8VNH	Dysmenorrhea	GA34.3	Approved	[9]
Flurbiprofen	DMGN4BY	Osteoarthritis	FA00-FA05	Approved	[10]
Ibuprofen	DM8VCBE	Dysmenorrhea	GA34.3	Approved	[11]
Indomethacin	DMSC4A7	Bursitis		Approved	[2]
Ketoprofen	DMRKXPT	Bursitis		Approved	[12]
Lumiracoxib	DM1S4AG	Chronic renal failure	GB61.Z	Approved	[13]
Meclofenamate Sodium	DMNL98G	Arthritis	FA20	Approved	[14]
Mefenamic acid	DMK7HFI	Dysmenorrhea	GA34.3	Approved	[15]
Meloxicam	DM2AR7L	Arthritis	FA20	Approved	[16]
Nabumetone	DMAT2XH	Osteoarthritis	FA00-FA05	Approved	[17]
Naproxen	DMZ5RGV	Bursitis		Approved	[18]
Niflumic Acid	DMJ3I1Q	Rheumatoid arthritis	FA20	Approved	[19]
Phenylbutazone	DMAYL0T	Chronic pain	MG30	Approved	[20]
Rofecoxib	DM3P5DA	Osteoarthritis	FA00-FA05	Approved	[21]
Tenoxicam	DMVAZP9	Rheumatoid arthritis	FA20	Approved	[22]
Tiaprofenic acid	DM23D7J	Osteoarthritis	FA00-FA05	Approved	[23]
Tolmetin	DMWUIJE	Osteoarthritis	FA00-FA05	Approved	[11]
Valdecoxib	DMAY7H4	Osteoarthritis	FA00-FA05	Approved	[24]
IMRECOXIB	DMVXLOD	N. A.	N. A.	Phase 4	[25]

10 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(S)-FLURBIPROFEN	DMF2O4T	Myalgia	FB56.2	Preregistration	[26]
CG-100649	DMIKMA9	Arthritis	FA20	Phase 3	[27]
Curcumin	DMQPH29	Solid tumour/cancer	2A00-2F9Z	Phase 3	[28]
ThermoProfen	DMPGH7N	Pain	MG30-MG3Z	Phase 3	[29]
Darbufelone	DMYVKM5	Asthma	CA23	Phase 2/3	[30]
CIMICOXIB	DMTKSVA	Pain	MG30-MG3Z	Phase 2	[31]
FK-3311	DML5AE4	Rheumatoid arthritis	FA20	Phase 2	[32]
SC-75416	DM58HR7	Pain	MG30-MG3Z	Phase 2	[33]
CA102N	DMYDNQ2	Solid tumour/cancer	2A00-2F9Z	Phase 1	[34]
RWJ-67657	DM6YAGE	Arthritis	FA20	Phase 1	[35]

2 Patented Agent(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Carbamate derivative 2	DMEWPQ6	N. A.	N. A.	Patented	[36]
PMID29130358-Compound-LonimacranthoideVI	DMTJEU5	N. A.	N. A.	Patented	[37]

32 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
INDOPROFEN	DM5QSKN	Gout	FA25	Withdrawn from market	[26]
GW-406381	DMJ4KQS	Neuropathic pain	8E43.0	Discontinued in Phase 3	[38]
PMI-001	DMDZBIQ	Lupus	4A40	Discontinued in Phase 3	[39]
PRINOMIDE TROMETHAMINE	DMI02PF	Inflammation	1A00-CA43.1	Discontinued in Phase 3	[40]
Apricoxib	DMR3Q82	Non-small-cell lung cancer	2C25.Y	Discontinued in Phase 2	[41]
CRx-401	DM39N7W	Type-2 diabetes	5A11	Discontinued in Phase 2	[42]
GSK-644784	DMUC9OS	Neuropathic pain	8E43.0	Discontinued in Phase 2	[38]
R-ketoprofen	DMHSUQ1	N. A.	N. A.	Discontinued in Phase 2	[26]
RQ-00317076	DM4GVZ9	Pain	MG30-MG3Z	Discontinued in Phase 2	[43]
S-2474	DMMSZ1A	Rheumatoid arthritis	FA20	Discontinued in Phase 2	[44]
TEBUFELONE	DMMUE8P	Pain	MG30-MG3Z	Discontinued in Phase 2	[45]
Tilmacoxib	DMPWSRA	Colon polyp	DB35	Discontinued in Phase 2	[46]
DUP 697	DMUMAHC	Pain	MG30-MG3Z	Discontinued in Phase 1	[47]
E-6087	DM79MI4	Pain	MG30-MG3Z	Discontinued in Phase 1	[48]
GR-253035	DMWY2F6	Alzheimer disease	8A20	Discontinued in Phase 1	[49]
SC-57666	DMIVRWS	Rheumatoid arthritis	FA20	Discontinued in Phase 1	[45]
ATLIPROFEN METHYL ESTER	DMS2FB3	Inflammation	1A00-CA43.1	Terminated	[2]
Flosulide	DM6OIJ1	Pain	MG30-MG3Z	Terminated	[50]
FR-123826	DM0582D	Rheumatoid arthritis	FA20	Terminated	[51]
L-745337	DMOQIWH	Asthma	CA23	Terminated	[52]
L-768277	DM7J6QH	Hyperthermia	MG26	Terminated	[53]
Nimesulide	DMR1NMD	Metastatic colorectal cancer	2B91	Terminated	[54]
NMI-150	DMX6DNZ	Pain	MG30-MG3Z	Terminated	[55]
NS398	DMINUWH	Endometriosis	GA10	Terminated	[56]
ON-09300	DMMLXRG	Solid tumour/cancer	2A00-2F9Z	Terminated	[2]
RPR 200765A	DM1U0TB	Rheumatoid arthritis	FA20	Terminated	[57]
RWJ-63556	DMUDE1T	Arthritis	FA20	Terminated	[58]
S-33516	DMF710M	Arthritis	FA20	Terminated	[59]
SB 203580	DMAET6F	N. A.	N. A.	Terminated	[60]
SC-236	DMO1URE	Solid tumour/cancer	2A00-2F9Z	Terminated	[61]
SC-58125	DM874YU	N. A.	N. A.	Terminated	[62]
SC-58451	DMVGK24	N. A.	N. A.	Terminated	[63]

126 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(11H-Dibenzo[b,e][1,4]dioxepin-2-yl)-acetic acid	DMSUPVE	Discovery agent	N.A.	Investigative	[64]
(11H-Dibenzo[b,e][1,4]dioxepin-7-yl)-acetic acid	DM5ZTXL	Discovery agent	N.A.	Investigative	[64]
(11H-Dibenzo[b,e][1,4]dioxepin-8-yl)-acetic acid	DMBY623	Discovery agent	N.A.	Investigative	[64]
(E)-2-(4-(methylsulfonyl)styryl)furan	DMH2U4Z	Discovery agent	N.A.	Investigative	[65]
(E)-2-(4-(methylsulfonyl)styryl)thiophene	DMDFE1R	Discovery agent	N.A.	Investigative	[65]
(E)-3-(4-(methylsulfonyl)styryl)thiophene	DMUS0D8	Discovery agent	N.A.	Investigative	[65]
(E)-4-(2-(furan-2-yl)vinyl)benzenesulfonamide	DMDF7M4	Discovery agent	N.A.	Investigative	[65]
(E)-4-(2-(thiophen-2-yl)vinyl)benzenesulfonamide	DM7204O	Discovery agent	N.A.	Investigative	[65]
(E)-4-(2-(thiophen-3-yl)vinyl)benzenesulfonamide	DMTAB8W	Discovery agent	N.A.	Investigative	[65]
(R)-2-(4-Isobutyl-phenyl)-N-phenyl-propionamide	DMAD4JY	Discovery agent	N.A.	Investigative	[26]
(Z)-2'-des-methyl sulindac sulfide	DM0OEQJ	Discovery agent	N.A.	Investigative	[66]
1,2-dihydro-3-(2,3,4-trimethoxyphenyl)naphthalene	DMST60D	Discovery agent	N.A.	Investigative	[67]
1,3-bis(nitrooxy)propan-2-yl 2-acetoxybenzoate	DMIK7XV	Discovery agent	N.A.	Investigative	[68]
1-(2-hydroxyphenyl)-3-p-tolylprop-2-en-1-one	DMAFS7J	Discovery agent	N.A.	Investigative	[69]
1-(4-(methylsulfonyl)phenyl)-1H-indole	DMCE7G0	Discovery agent	N.A.	Investigative	[70]
1-(4-(methylsulfonyl)phenyl)-1H-pyrrole	DMYFBRQ	Discovery agent	N.A.	Investigative	[70]
1-(4-(methylsulfonyl)phenyl)-3-p-tolylurea	DMMSQLC	Discovery agent	N.A.	Investigative	[71]
1-(4-(methylsulfonyl)phenyl)-3-phenylurea	DMH7RY0	Discovery agent	N.A.	Investigative	[71]
1-(4-aminosulfonylphenyl)-2-(2-pyridyl)acetylene	DMWA6G1	Discovery agent	N.A.	Investigative	[72]
2'-hydroxy-3,4,5-trimethoxychalcone	DM5ACNU	Discovery agent	N.A.	Investigative	[69]
2'-Hydroxychalcone	DM8RTBS	Discovery agent	N.A.	Investigative	[69]
2,3-dimethoxy-2'-hydroxychalcone	DML92OK	Discovery agent	N.A.	Investigative	[69]
2,4'-Dimethoxy-5,3'-di-(2-propenyl)-biphenyl	DMWNJ84	Discovery agent	N.A.	Investigative	[73]
2,4'-Dimethoxy-5,3'-dipropyl-biphenyl	DM94NM7	Discovery agent	N.A.	Investigative	[73]
2,4-dimethoxy-2'-hydroxychalcone	DMP9BZU	Discovery agent	N.A.	Investigative	[69]
2,6-dihydroxy-1,7-dimethoxyxanthone	DM5QEUC	Discovery agent	N.A.	Investigative	[74]
2-(2,3,4-trimethoxyphenyl)-1H-indene	DMFU1PK	Discovery agent	N.A.	Investigative	[67]
2-(2-(2,6-dimethylphenylamino)phenyl)acetic acid	DMJ2DE4	Discovery agent	N.A.	Investigative	[75]
2-(3-Phenyl-propyl)-1,2-dihydro-indazol-3-one	DMIQBXD	Discovery agent	N.A.	Investigative	[76]
2-(4-(methylsulfonyl)phenyl)-3-phenylquinoline	DMVD6HE	Discovery agent	N.A.	Investigative	[77]
2-(4-(methylsulfonyl)phenyl)pyridine	DM1TZNK	Discovery agent	N.A.	Investigative	[70]
2-(N-(2-Ffuorophenyl)pyrrol-3-yl) acetic acid	DMRNOM6	Discovery agent	N.A.	Investigative	[78]
2-(N-(2-fluorophenyl)pyrrol-2-yl) acetic acid	DMCL9E6	Discovery agent	N.A.	Investigative	[78]
2-(p-Methylsulfonylbenzoyl)furan	DMLT635	Discovery agent	N.A.	Investigative	[70]
2-Benzyl-1,2-dihydro-indazol-3-one	DM1CB5J	Discovery agent	N.A.	Investigative	[76]
2-Furan-2-ylmethyl-1,2-dihydro-indazol-3-one	DMQIRY7	Discovery agent	N.A.	Investigative	[76]
2-Methyl-1,2-dihydro-indazol-3-one	DMDJHFQ	Discovery agent	N.A.	Investigative	[76]
2-Naphthalen-2-ylmethyl-1,2-dihydro-indazol-3-one	DM1EJ6W	Discovery agent	N.A.	Investigative	[76]
2-Phenethyl-1,2-dihydro-indazol-3-one	DM0WMBC	Discovery agent	N.A.	Investigative	[76]
2-Phenyl-1,2-dihydro-indazol-3-one	DM28CLZ	Discovery agent	N.A.	Investigative	[76]
3 beta-O-acetyloleanolic acid	DM1L5IJ	Discovery agent	N.A.	Investigative	[79]
3,4-dibenzyloxy-2'-hydroxychalcone	DMBUT8A	Discovery agent	N.A.	Investigative	[69]
3,4-dihydroxyxanthone	DMTQX92	Discovery agent	N.A.	Investigative	[74]
3-(4-Methanesulfonyl-phenyl)-1-phenyl-propynone	DMSR2O3	Discovery agent	N.A.	Investigative	[80]
3-benzyloxy-4-methoxy-2'-hydroxychalcone	DMKD874	Discovery agent	N.A.	Investigative	[69]
3-Bromo-2'-hydroxy-4-methoxychalcone	DM1BALV	Discovery agent	N.A.	Investigative	[69]
4,5-Bis(4-chlorophenyl)-1,2-selenazole	DMIO254	Discovery agent	N.A.	Investigative	[81]
4,5-Bis(4-chlorophenyl)isothiazole	DMENLFY	Discovery agent	N.A.	Investigative	[82]
4,5-Bis(4-methoxyphenyl)-1,2-selenazole	DMKHD1M	Discovery agent	N.A.	Investigative	[81]
4,5-Bis(4-methoxyphenyl)-3H-1,2-dithiol-3-one	DMI39QT	Discovery agent	N.A.	Investigative	[82]
4,5-Bis(4-methoxyphenyl)isothiazole	DM90DV6	Discovery agent	N.A.	Investigative	[82]
4-((4-methoxyphenyl)diazenyl)benzenesulfonamide	DMNAT1D	Discovery agent	N.A.	Investigative	[83]
4-(3-hydroxy-benzylideneamino)-benzenesulfonamide	DMY2OVL	Discovery agent	N.A.	Investigative	[84]
4-(3-methoxy-benzylideneamino)-benzenesulfonamide	DMO8SQA	Discovery agent	N.A.	Investigative	[84]
4-(3-nitro-benzylideneamino)-benzenesulfonamide	DMD94OB	Discovery agent	N.A.	Investigative	[84]
4-(4-Chlorophenyl)-5-p-tolyl-1,2-selenazole	DMZBEYO	Discovery agent	N.A.	Investigative	[81]
4-(4-fluoro-benzylideneamino)-benzenesulfonamide	DMRJD75	Discovery agent	N.A.	Investigative	[84]
4-(4-fluoro-phenyliminomethyl)-benzenesulfonamide	DMK8DCF	Discovery agent	N.A.	Investigative	[84]
4-(4-hydroxy-benzylideneamino)-benzenesulfonamide	DMNY0I5	Discovery agent	N.A.	Investigative	[84]
4-(4-methoxy-benzylideneamino)-benzenesulfonamide	DM2OR8E	Discovery agent	N.A.	Investigative	[84]
4-(4-methyl-benzylideneamino)-benzenesulfonamide	DMZSQ04	Discovery agent	N.A.	Investigative	[84]
4-(4-methyl-phenyliminomethyl)-benzenesulfonamide	DMV0S4U	Discovery agent	N.A.	Investigative	[84]
4-(4-nitro-benzylideneamino)-benzenesulfonamide	DMM86YK	Discovery agent	N.A.	Investigative	[84]
4-(benzylideneamino)benzenesulfonamide	DM03BQD	Discovery agent	N.A.	Investigative	[84]
4-amino-N-(4-chlorophenyl)benzenesulfonamide	DMCUSD4	Discovery agent	N.A.	Investigative	[85]
4-amino-N-(4-iodophenyl)benzenesulfonamide	DMN19QP	Discovery agent	N.A.	Investigative	[85]
4-benzyloxy-2'-hydroxychalcone	DMDC7TL	Discovery agent	N.A.	Investigative	[69]
4-fluoro-N-(4-(methylsulfonyl)phenyl)aniline	DMV6M5U	Discovery agent	N.A.	Investigative	[70]
4-phenyliminomethyl-benzenesulfonamide	DM9J5TZ	Discovery agent	N.A.	Investigative	[84]
5,3'-Dipropyl-biphenyl-2,4'-diol	DMJRXLD	Discovery agent	N.A.	Investigative	[73]
5-(2-Imidazol-1-yl-ethyl)-7,8-dihydro-quinoline	DMCP5U8	Discovery agent	N.A.	Investigative	[86]
5-(4-Chlorophenyl)-4-p-tolyl-1,2-selenazole	DMY0P86	Discovery agent	N.A.	Investigative	[81]
5-(4-Methoxyphenyl)-4-p-tolyl-1,2-selenazole	DMEV8WS	Discovery agent	N.A.	Investigative	[81]
5-Ethyl-3,4-diphenyl-isoxazole	DMRIGXA	Discovery agent	N.A.	Investigative	[87]
5-methoxy-2-(4-(methylsulfonyl)phenyl)-1H-indole	DMG2HSU	Discovery agent	N.A.	Investigative	[88]
5-Methyl-3,4-diphenyl-isoxazole	DM0G2N5	Discovery agent	N.A.	Investigative	[87]
5-Phenyl-pentanoic acid benzyl-hydroxy-amide	DM3B6A8	Discovery agent	N.A.	Investigative	[89]
5-thia-8,11,14,17-eicosatetraenoic acid	DMF4RGW	Discovery agent	N.A.	Investigative	[5]
6,7'-oxybis(2-phenyl-4H-chromen-4-one)	DMT09YC	Discovery agent	N.A.	Investigative	[90]
8alpha,19-dihydroxylabd-13 E-en-15-oic acid	DM7K2DN	Discovery agent	N.A.	Investigative	[91]
alpha-linolenic acid	DMY64HE	Discovery agent	N.A.	Investigative	[5]
B-Octylglucoside	DMMO75G	Discovery agent	N.A.	Investigative	[92]
Bimetopyrole	DMPR14J	Pain	MG30-MG3Z	Investigative	[47]
C-myb	DMA5Z2G	Pain	MG30-MG3Z	Investigative	[93]
CLEMATOMANDSHURICA SAPONIN A	DM4SKYA	Discovery agent	N.A.	Investigative	[94]
CLEMATOMANDSHURICA SAPONIN B	DMNWXOC	Discovery agent	N.A.	Investigative	[94]
CR-4174	DM3M5AW	Inflammation	1A00-CA43.1	Investigative	[95]
CX-9051	DM526C9	Solid tumour/cancer	2A00-2F9Z	Investigative	[95]
DFU	DMUM84K	Pain	MG30-MG3Z	Investigative	[96]
Firocoxib	DMP6GNY	Discovery agent	N.A.	Investigative	[97]
Fluoro loxoprofen	DMJS62X	Discovery agent	N.A.	Investigative	[98]
Furan-3-yl(4-(methylsulfonyl)phenyl)methanone	DMPC6YL	Discovery agent	N.A.	Investigative	[70]
GW-637185X	DMX59A0	Discovery agent	N.A.	Investigative	[99]
Heme	DMGC287	Discovery agent	N.A.	Investigative	[100]
HONOKIOL	DMJWT3X	Discovery agent	N.A.	Investigative	[73]
L-748780	DMJZXAF	Discovery agent	N.A.	Investigative	[101]
L-761000	DM0A2MG	Discovery agent	N.A.	Investigative	[101]
LM-4108	DMWLMTD	Discovery agent	N.A.	Investigative	[102]
METHYLHONOKIOL	DM9YE6K	Discovery agent	N.A.	Investigative	[73]
Microxine	DM7Y9AD	Pain	MG30-MG3Z	Investigative	[103]
N-(1H-indazol-5-yl)acetamide	DMIMJNU	Discovery agent	N.A.	Investigative	[104]
N-(3-(phenylthio)pyridin-4-yl)methanesulfonamide	DMSJX1H	Discovery agent	N.A.	Investigative	[105]
N-(3-phenoxy-4-pyridinyl)ethanesulfonamide	DMXF46V	Discovery agent	N.A.	Investigative	[106]
N-(3-phenylamino-4-pyridinyl)methanesulfonamide	DMJB7SE	Discovery agent	N.A.	Investigative	[105]
Nectamazin C	DMO0Q1F	Discovery agent	N.A.	Investigative	[107]
NEOLIGNAN 9-NOR-7,8-DEHYDRO-ISOLICARIN B	DMKFPA9	Discovery agent	N.A.	Investigative	[107]
Nitroflurbiprofen	DMWCV48	Discovery agent	N.A.	Investigative	[108]
NSC-27236	DMANZIE	Discovery agent	N.A.	Investigative	[83]
OCOPHYLLALS A	DMT59UG	Discovery agent	N.A.	Investigative	[107]
Ocophyllals b	DMEUPVF	Discovery agent	N.A.	Investigative	[107]
Oxametacin	DMWVLG1	Discovery agent	N.A.	Investigative	[109]
Oxindole 94	DMPFD6Y	Pain	MG30-MG3Z	Investigative	[110]
PAC-10649	DMKL6IC	Arthritis	FA20	Investigative	[111]
PHENIDONE	DMJD8XN	Discovery agent	N.A.	Investigative	[76]
Prifelone	DMLI4RF	Discovery agent	N.A.	Investigative	[112]
Primary alcohol metabolite of celecoxib	DMA8GI6	Discovery agent	N.A.	Investigative	[113]
Prostaglandin G2	DME74SP	Discovery agent	N.A.	Investigative	[100]
Resveratrol Potassium3-Sulfate	DMN1RLA	Discovery agent	N.A.	Investigative	[114]
Resveratrol Potassium4,-Sulfate	DMMFP57	Discovery agent	N.A.	Investigative	[114]
SB 239063	DM201Q7	Pain	MG30-MG3Z	Investigative	[115]
SC-558	DMAZLKX	Discovery agent	N.A.	Investigative	[116]
Silicon-modified indomethacin	DM5ZILV	Arthritis	FA20	Investigative	[95]
TENOSAL	DMMLSZ4	Rheumatoid arthritis	FA20	Investigative	[117]
THIOCTIC ACID	DMNFCXW	Discovery agent	N.A.	Investigative	[81]
Wogonin	DMGCF51	Discovery agent	N.A.	Investigative	[69]
XGP-110	DM96FTS	Arthritis	FA20	Investigative	[95]

Molecular Expression Atlas (MEA) of This DTT

Disease Name	ICD 11	Studied Tissue	p-value	Fold-Change	Z-score
Asthma	CA23	Nasal and bronchial airway	1.50E-04	0.86	0.64
Alzheimer's disease	8A00.0	Entorhinal cortex	7.93E-04	-0.29	-0.34
Osteoarthritis	FA20	Synovial tissue	3.32E-01	1.67	0.74
Rheumatoid arthritis	FA20	Synovial tissue	9.92E-06	1.36	2.49
Endometriosis	GA10	Endometrium tissue	1.40E-01	-0.9	-0.5
Type 2 diabetes	5A11	Liver tissue	2.08E-01	1.68E-03	0.03
Rectal cancer	2C82	Rectal colon tissue	2.03E-07	1.68	3.86
Colon cancer	2C82	Colon tissue	1.64E-44	1.57	1.7

The Drug-Metabolizing Enzyme (DME) Role of This DTT

• DTT DME Name: Prostaglandin G/H synthase 2 (COX-2) DME Info
• Gene Name: PTGS2

6 Approved Drug(s) Metabolized by This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Dapsone	DM4LT8A	Acne vulgaris	ED80	Approved	[118]
Eicosapentaenoic acid/docosa-hexaenoic acid	DMMUCG4	Hypertriglyceridemia	5C80.1	Approved	[119]
Epanova	DMHEAGL	Hypertriglyceridemia	5C80.1	Approved	[120]
Etoposide	DMNH3PG	Acute myelogenous leukaemia	2A41	Approved	[121]
Gamma-Homolinolenic acid	DMSXKYG	Malnutrition	5B50-5B71	Approved	[119]
Gamolenic acid	DMQN30Z	Allergy	4A80-4A85	Approved	[119]

1 Clinical Trial Drug(s) Metabolized by This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Omega-6-FA	DMBWY8V	N. A.	N. A.	Phase 3	[122]

5 Investigative Drug(s) Metabolized by This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
alpha-linolenic acid	DMY64HE	Discovery agent	N.A.	Investigative	[119]
Arachidonic Acid	DMUOQZD	Discovery agent	N.A.	Investigative	[123]
BML3-C01	DMER2WS	N. A.	N. A.	Investigative	[119]
Eicosadienoic acid	DMVJK9W	N. A.	N. A.	Investigative	[119]
Icosapentum	DMF1CM7	N. A.	N. A.	Investigative	[119]

References

• [1] Celecoxib and rofecoxib. The role of COX-2 inhibitors in dental practice. J Am Dent Assoc. 2001 Apr;132(4):451-6.
• [2] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [3] Scaffold of the cyclooxygenase-2 (COX-2) inhibitor carprofen provides Alzheimer gamma-secretase modulators. J Med Chem. 2006 Dec 28;49(26):7588-91.
• [4] Pfizer. Product Development Pipeline. March 31 2009.
• [5] Cox-2 inhibitory effects of naturally occurring and modified fatty acids. J Nat Prod. 2001 Jun;64(6):745-9.
• [6] Membranous nephropathy associated with the relatively selective cyclooxygenase-2 inhibitor, etodolac, in a patient with early rheumatoid arthritis. Intern Med. 2007;46(13):1055-8.
• [7] The effect of newer anti-rheumatic drugs on osteogenic cell proliferation: an in-vitro study. J Orthop Surg Res. 2009 May 26;4:17.
• [8] 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. Eur J Med Chem. 2009 Sep;44(9):3798-804.
• [9] Ouellet M, Percival MD: Effect of inhibitor time-dependency on selectivity towards cyclooxygenase isoforms. Biochem J. 1995 Feb 15;306 ( Pt 1):247-51.
• [10] Flurbiprofen, a cyclooxygenase inhibitor, protects mice from hepatic ischemia/reperfusion injury by inhibiting GSK-3 signaling and mitochondrial permeability transition.Mol Med.2012 Sep 25;18:1128-35.
• [11] Maternal toxicity of nonsteroidal anti-inflammatory drugs as an important factor affecting prenatal development. Reprod Toxicol. 2009 Sep;28(2):239-44.
• [12] Probing the skin permeation of fish oil/EPA and ketoprofen-3. Effects on epidermal COX-2 and LOX. Prostaglandins Leukot Essent Fatty Acids. 2007 Jun;76(6):357-62.
• [13] Dissociation of airway inflammation and hyperresponsiveness by cyclooxygenase inhibition in allergen challenged mice. Eur Respir J. 2009 Jul;34(1):200-8.
• [14] Role of COX-2-derived metabolites in regulation of the renal hemodynamic response to norepinephrine. Am J Physiol Renal Physiol. 2001 Nov;281(5):F975-82.
• [15] Systematic pharmacological approach to the characterization of NSAIDs. Prostaglandins Leukot Essent Fatty Acids. 1998 Jul;59(1):55-62.
• [16] Meloxicam: selective COX-2 inhibition in clinical practice. Semin Arthritis Rheum. 1997 Jun;26(6 Suppl 1):21-7.
• [17] Renal effects of nabumetone, a COX-2 antagonist: impairment of function in isolated perfused rat kidneys contrasts with preserved renal function in vivo. Exp Nephrol. 2001;9(6):387-96.
• [18] Comparative 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.
• [19] Rat ovulation, implantation and decidualization are severely compromised by COX-2 inhibitors. Front Biosci. 2007 May 1;12:3333-42.
• [20] COX-1 and COX-2 inhibition in horse blood by phenylbutazone, flunixin, carprofen and meloxicam: an in vitro analysis. Pharmacol Res. 2005 Oct;52(4):302-6.
• [21] Privileged structures: a useful concept for the rational design of new lead drug candidates. Mini Rev Med Chem. 2007 Nov;7(11):1108-19.
• [22] The use and safety profile of non-steroidal antiinflammatory drugs among Turkish patients with osteoarthritis. Turk J Gastroenterol. 2005 Sep;16(3):138-42.
• [23] Effects of tiaprofenic acid on the concentration and metabolism of proteoglycans in normal and degenerating canine articular cartilage. J Clin Pharmacol. 1990 Sep;30(9):808-14.
• [24] Biochemical mechanisms of New Molecular Entities (NMEs) approved by United States FDA during 2001-2004: mechanisms leading to optimal efficacy and ... Curr Top Med Chem. 2006;6(5):461-78.
• [25] Synthesis and anti-inflammatory activity of the major metabolites of imrecoxib. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2270-2.
• [26] 2-Arylpropionic CXC chemokine receptor 1 (CXCR1) ligands as novel noncompetitive CXCL8 inhibitors. J Med Chem. 2005 Jun 30;48(13):4312-31.
• [27] Pharmacokinetic, pharmacodynamic, and safety/tolerability profiles of CG100649, a novel COX-2 inhibitor: results of a phase i, randomized, multiple-dose study in healthy Korean men and women. Clin Ther. 2015 Jan 1;37(1):197-210.
• [28] Design, synthesis, biological evaluation and molecular docking of curcumin analogues as antioxidant, cyclooxygenase inhibitory and anti-inflammator... Bioorg Med Chem Lett. 2005 Apr 1;15(7):1793-7.
• [29] Topical NSAID therapy for musculoskeletal pain. Pain Med. 2010 Apr;11(4):535-49.
• [30] Novel 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.
• [31] Pharmacokinetic profiles of the novel COX-2 selective inhibitor cimicoxib in dogs.Vet J.2014 Apr;200(1):77-81.
• [32] Effects of the COX-2 inhibitor FK3311 on ischemia - reperfusion injury in the rat lung. J Invest Surg. 2007 May-Jun;20(3):175-80.
• [33] Modeling and simulation to support dose selection and clinical development of SC-75416, a selective COX-2 inhibitor for the treatment of acute and ... Clin Pharmacol Ther. 2008 Jun;83(6):857-66.
• [34] National Cancer Institute Drug Dictionary (drug name CA102N).
• [35] Monocyte intracellular cytokine production during human endotoxaemia with or without a second in vitro LPS challenge: effect of RWJ-67657, a p38 MAP-kinase inhibitor, on LPS-hyporesponsiveness. Clin Exp Immunol. 2002 Feb;127(2):337-43.
• [36] Fatty acid amide hydrolase inhibitors: a patent review (2009-2014).Expert Opin Ther Pat. 2015;25(11):1247-66.
• [37] Gelatinase inhibitors: a patent review (2011-2017).Expert Opin Ther Pat. 2018 Jan;28(1):31-46.
• [38] Emerging drugs in neuropathic pain. Expert Opin Emerg Drugs. 2007 Mar;12(1):113-26.
• [39] Development of a botanical anti-arthritis drug, PMI-001. SBIR.STTR America's Seed Fund.
• [40] Dexketoprofene, selective cox-1 inhibitor nsaids, without gastrointestinal injury in rats. Acta Gastroenterol Latinoam. 2002 May;32(1):17-20.
• [41] Apricoxib, a COX-2 inhibitor for the potential treatment of pain and cancer. IDrugs. 2009 Nov;12(11):711-22.
• [42] ClinicalTrials.gov (NCT00506298) Study of CRx-401 on Glucose Levels in Subjects With Type II Diabetes. U.S. National Institutes of Health.
• [43] Clinical pipeline report, company report or official report of raqualia.
• [44] Effects of S-2474, a novel nonsteroidal anti-inflammatory drug, on amyloid beta protein-induced neuronal cell death. Br J Pharmacol. 2001 Oct;134(3):673-81.
• [45] New cyclooxygenase-2/5-lipoxygenase inhibitors. 2. 7-tert-butyl-2,3-dihydro-3,3-dimethylbenzofuran derivatives as gastrointestinal safe antiinflamm... J Med Chem. 1998 Mar 26;41(7):1124-37.
• [46] 4-(4-cycloalkyl/aryl-oxazol-5-yl)benzenesulfonamides as selective cyclooxygenase-2 inhibitors: enhancement of the selectivity by introduction of a ... J Med Chem. 2002 Mar 28;45(7):1511-7.
• [47] Current status of COX-2 inhibitors. Mini Rev Med Chem. 2008 Jan;8(1):73-90.
• [48] Enantioselective HPLC determination of E-6087, a new COX-2 inhibitor, in human plasma: Validation and pharmacokinetic application. Chirality. 2004 May 15;16(5):302-8.
• [49] Role of cyclooxygenases 1 and 2 in the modulation of neuromuscular functions in the distal colon of humans and mice. Gut. 2005 May; 54(5): 608-616.
• [50] Effect of flosulide, a selective cyclooxygenase 2 inhibitor, on passive heymann nephritis in the rat. Kidney Int. 1999 Nov;56(5):1770-8.
• [51] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007983)
• [52] Pharmacology of a selective cyclooxygenase-2 inhibitor, L-745,337: a novel nonsteroidal anti-inflammatory agent with an ulcerogenic sparing effect ... J Pharmacol Exp Ther. 1995 Sep;274(3):1531-7.
• [53] Characterization of the in vitro oxidative metabolites of the COX-2 selective inhibitor L-766,112. Bioorganic & Medicinal Chemistry Letters Volume 7, Issue 1, 7 January 1997, Pages 53-56.
• [54] Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5.
• [55] Selective COX-2 Inhibitors: A Review of Their Structure-Activity Relationships. Iran J Pharm Res. 2011 Autumn; 10(4): 655-683.
• [56] New drugs in development for the treatment of endometriosis. Expert Opin Investig Drugs. 2008 Aug;17(8):1187-202.
• [57] The discovery of RPR 200765A, a p38 MAP kinase inhibitor displaying a good oral anti-arthritic efficacy. Bioorg Med Chem. 2001 Feb;9(2):537-54.
• [58] Evaluation 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.
• [59] S 33516 Servier preclinical data. R & D Focus Drug News. July 12, 1999.
• [60] Inhibition of p38 MAP kinase as a therapeutic strategy. Immunopharmacology. 2000 May;47(2-3):185-201.
• [61] Cyclooxygenase (COX)-2-dependent effects of the inhibitor SC236 when combined with ionizing radiation in mammary tumor cells derived from HER-2/neu mice. Mol Cancer Ther. 2004 Apr;3(4):417-24.
• [62] Identification and optimisation of a novel series of pyrimidine based cyclooxygenase-2 (COX-2) inhibitors. Utilisation of a biotransformation appro... Bioorg Med Chem Lett. 2009 Aug 1;19(15):4509-14.
• [63] Novel 1,2-diarylcyclobutenes: Selective and orally active cox-2 inhibitors, Bioorg. Med. Chem. Lett. 6(22):2677-2682 (1996).
• [64] Synthesis and antiinflammatory/analgesic activities of 11H-dibenzo[b, e,][1,4]dioxepinacetic acids. J Med Chem. 1986 Aug;29(8):1436-41.
• [65] Sulfonamide derivatives of styrylheterocycles as a potent inhibitor of COX-2-mediated prostaglandin E2 production. Bioorg Med Chem Lett. 2010 Dec 1;20(23):6938-41.
• [66] The influence of double bond geometry in the inhibition of cyclooxygenases by sulindac derivatives. Bioorg Med Chem Lett. 2009 Jun 15;19(12):3271-4.
• [67] 'Bridged' stilbene derivatives as selective cyclooxygenase-1 inhibitors. Bioorg Med Chem. 2007 Sep 15;15(18):6109-18.
• [68] Dinitroglyceryl and diazen-1-ium-1,2-diolated nitric oxide donor ester prodrugs of aspirin, indomethacin and ibuprofen: synthesis, biological evalu... Bioorg Med Chem Lett. 2009 Jun 1;19(11):3014-8.
• [69] Inhibitory activity of prostaglandin E2 production by the synthetic 2'-hydroxychalcone analogues: Synthesis and SAR study. Bioorg Med Chem Lett. 2009 Mar 15;19(6):1650-3.
• [70] Synthesis, anti-inflammatory activity, and in vitro antitumor effect of a novel class of cyclooxygenase inhibitors: 4-(aryloyl)phenyl methyl sulfones. J Med Chem. 2010 Sep 23;53(18):6560-71.
• [71] Design and synthesis of 1,3-diarylurea derivatives as selective cyclooxygenase (COX-2) inhibitors. Bioorg Med Chem Lett. 2008 Feb 15;18(4):1336-9.
• [72] Synthesis and cyclooxygenase inhibitory activities of linear 1-(methanesulfonylphenyl or benzenesulfonamido)-2-(pyridyl)acetylene regioisomers. Bioorg Med Chem. 2008 Feb 15;16(4):1948-56.
• [73] 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.
• [74] Selective cyclooxygenase-2 inhibitors from Calophyllum membranaceum. J Nat Prod. 2005 Oct;68(10):1514-8.
• [75] Molecular determinants for the selective inhibition of cyclooxygenase-2 by lumiracoxib. J Biol Chem. 2007 Jun 1;282(22):16379-90.
• [76] Indazolinones, a new series of redox-active 5-lipoxygenase inhibitors with built-in selectivity and oral activity. J Med Chem. 1991 Mar;34(3):1028-36.
• [77] Design, synthesis and biological evaluation of new 2,3-diarylquinoline derivatives as selective cyclooxygenase-2 inhibitors. Bioorg Med Chem. 2010 Feb;18(3):1029-33.
• [78] Synthesis and biological activity of new anti-inflammatory compounds containing the 1,4-benzodioxine and/or pyrrole system. Bioorg Med Chem. 2007 Jul 15;15(14):4876-90.
• [79] Nitrogen-containing phorbol esters from Croton ciliatoglandulifer and their effects on cyclooxygenases-1 and -2. J Nat Prod. 2006 Jun;69(6):887-90.
• [80] Synthesis and biological evaluation of 1,3-diphenylprop-2-yn-1-ones as dual inhibitors of cyclooxygenases and lipoxygenases. Bioorg Med Chem Lett. 2005 Nov 1;15(21):4842-5.
• [81] Investigations concerning the COX/5-LOX inhibiting and hydroxyl radical scavenging potencies of novel 4,5-diaryl isoselenazoles. Eur J Med Chem. 2008 Jun;43(6):1152-9.
• [82] Diaryl-dithiolanes and -isothiazoles: COX-1/COX-2 and 5-LOX-inhibitory, *OH scavenging and anti-adhesive activities. Bioorg Med Chem. 2009 Jan 15;17(2):558-68.
• [83] Selective COX-2 inhibitors. Part 1: synthesis and biological evaluation of phenylazobenzenesulfonamides. Bioorg Med Chem Lett. 2006 Sep 1;16(17):4440-3.
• [84] Selective COX-2 inhibitors. Part 2: synthesis and biological evaluation of 4-benzylideneamino- and 4-phenyliminomethyl-benzenesulfonamides. Bioorg Med Chem. 2008 Mar 1;16(5):2697-706.
• [85] Analgesic agents without gastric damage: design and synthesis of structurally simple benzenesulfonanilide-type cyclooxygenase-1-selective inhibitors. Bioorg Med Chem. 2007 Jan 15;15(2):1014-21.
• [86] 1-imidazolyl(alkyl)-substituted di- and tetrahydroquinolines and analogues: syntheses and evaluation of dual inhibitors of thromboxane A(2) synthas... J Med Chem. 2000 May 4;43(9):1841-51.
• [87] Novel synthesis of 3,4-diarylisoxazole analogues of valdecoxib: reversal cyclooxygenase-2 selectivity by sulfonamide group removal. J Med Chem. 2004 Sep 23;47(20):4881-90.
• [88] Synthesis and biological evaluation of new 4-carboxyl quinoline derivatives as cyclooxygenase-2 inhibitors. Bioorg Med Chem. 2009 Jul 15;17(14):5312-7.
• [89] Differential effects of a series of hydroxamic acid derivatives on 5-lipoxygenase and cyclooxygenase from neutrophils and 12-lipoxygenase from plat... J Med Chem. 1989 Aug;32(8):1836-42.
• [90] Synthesis of biflavones having a 6-O-7'' linkage and effects on cyclooxygenase-2 and inducible nitric oxide synthase. Bioorg Med Chem Lett. 2009 Jan 1;19(1):74-6.
• [91] Cyclooxygenase (COX)-1 and -2 inhibitory labdane diterpenes from Crassocephalum mannii. J Nat Prod. 2008 Jun;71(6):1070-3.
• [92] How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
• [93] Cyclooxygenase-2, a colorectal cancer nonsteroidal anti-inflammatory drug target, is regulated by c-MYB. Cancer Res. 2000 Apr 1;60(7):1805-9.
• [94] Triterpene saponins from clematis mandshurica. J Nat Prod. 2006 Nov;69(11):1591-5.
• [95] URL: 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: 1376).
• [96] Inhibition of cyclooxygenase-2 improves cardiac function in myocardial infarction. Biochem Biophys Res Commun. 2000 Jul 5;273(2):772-5.
• [97] SAR in the alkoxy lactone series: the discovery of DFP, a potent and orally active COX-2 inhibitor. Bioorg Med Chem Lett. 1999 Aug 2;9(15):2207-12.
• [98] Properties and synthesis of 2-{2-fluoro (or bromo)-4-[(2-oxocyclopentyl)methyl]phenyl}propanoic acid: nonsteroidal anti-inflammatory drugs with low... J Med Chem. 2010 Nov 11;53(21):7879-82.
• [99] Identification of [4-[4-(methylsulfonyl)phenyl]-6-(trifluoromethyl)-2-pyrimidinyl] amines and ethers as potent and selective cyclooxygenase-2 inhib... Bioorg Med Chem Lett. 2009 Aug 1;19(15):4504-8.
• [100] The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
• [101] From indomethacin to a selective COX-2 inhibitor: Development of indolalkanoic acids as potent and selective cyclooxygenase-2 inhibitors, Bioorg. Med. Chem. Lett. 6(6):725-730 (1996).
• [102] Discovery of 3-(4-bromophenyl)-6-nitrobenzo[1.3.2]dithiazolium ylide 1,1-dioxide as a novel dual cyclooxygenase/5-lipoxygenase inhibitor that also ... Bioorg Med Chem. 2010 Jan 15;18(2):597-604.
• [103] Inhibition of cell cycle oscillation of DNA replication by a selective inhibitor of the cdc2 kinase family, butyrolactone I, in Xenopus egg extracts. Biochem Biophys Res Commun. 1994 Jan 28;198(2):536-45.
• [104] New analgesics synthetically derived from the paracetamol metabolite N-(4-hydroxyphenyl)-(5Z,8Z,11Z,14Z)-icosatetra-5,8,11,14-enamide. J Med Chem. 2008 Dec 25;51(24):7800-5.
• [105] Pyridine analogues of nimesulide: design, synthesis, and in vitro and in vivo pharmacological evaluation as promising cyclooxygenase 1 and 2 inhibi... J Med Chem. 2009 Oct 8;52(19):5864-71.
• [106] Design, synthesis, and pharmacological evaluation of pyridinic analogues of nimesulide as cyclooxygenase-2 selective inhibitors. J Med Chem. 2004 Dec 30;47(27):6749-59.
• [107] COX, LOX and platelet aggregation inhibitory properties of Lauraceae neolignans. Bioorg Med Chem Lett. 2009 Dec 15;19(24):6922-5.
• [108] The cyclooxygenase inhibitor flurbiprofen reduces radiation-induced angiogenic growth factor secretion of squamous cell carcinoma cell lines. Ann N Y Acad Sci. 2004 Dec;1030:37-42.
• [109] Structure-based design, synthesis, and biological evaluation of indomethacin derivatives as cyclooxygenase-2 inhibiting nitric oxide donors. J Med Chem. 2007 Dec 13;50(25):6367-82.
• [110] A selective inhibitor of p38 MAP kinase, SB202190, induced apoptotic cell death of a lipopolysaccharide-treated macrophage-like cell line, J774.1. Biochim Biophys Acta. 2000 Oct 18;1502(2):207-23.
• [111] PAC 10649 Pacific licensing offer, Worldwide excluding South Korea. R & D Focus Drug News. September 22, 2003.
• [112] Designed multiple ligands. An emerging drug discovery paradigm. J Med Chem. 2005 Oct 20;48(21):6523-43.
• [113] Diazen-1-ium-1,2-diolated nitric oxide donor ester prodrugs of 5-(4-hydroxymethylphenyl)-1-(4-aminosulfonylphenyl)-3-trifluoromethyl-1H-pyrazole an... Bioorg Med Chem. 2008 Nov 15;16(22):9694-8.
• [114] Selective synthesis and biological evaluation of sulfate-conjugated resveratrol metabolites. J Med Chem. 2010 Jul 8;53(13):5033-43.
• [115] SB-239063, a potent and selective inhibitor of p38 map kinase: preclinical pharmacokinetics and species-specific reversible isomerization. Pharm Res. 2001 Sep;18(9):1336-44.
• [116] In silico search for multi-target anti-inflammatories in Chinese herbs and formulas. Bioorg Med Chem. 2010 Mar 15;18(6):2204-2218.
• [117] US patent application no. 6,274,627, Conjugates of dithiocarbamate disulfides with pharmacologically active agents and uses therefor.
• [118] Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.
• [119] Divergent cyclooxygenase responses to fatty acid structure and peroxide level in fish and mammalian prostaglandin H synthases. FASEB J. 2006 Jun;20(8):1097-108.
• [120] Structural basis of fatty acid substrate binding to cyclooxygenase-2. J Biol Chem. 2010 Jul 16;285(29):22152-63.
• [121] Peroxidative free radical formation and O-demethylation of etoposide(VP-16) and teniposide(VM-26). Biochem Biophys Res Commun. 1986 Feb 26;135(1):215-20.
• [122] Health implications of high dietary omega-6 polyunsaturated Fatty acids. J Nutr Metab. 2012;2012:539426.
• [123] PharmGKB summary: very important pharmacogene information for PTGS2. Pharmacogenet Genomics. 2011 Sep;21(9):607-13.