Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTSJ6Q4)

• DTT Name: LOX-5 messenger RNA (ALOX5 mRNA)
• Synonyms: LOG5 (mRNA); 5-lipoxygenase (mRNA); 5-LO (mRNA)
• Gene Name: ALOX5
• DTT Type: Discontinued target; [1]
• BioChemical Class: mRNA target
• UniProt ID: LOX5_HUMAN
• TTD ID: T93566
• EC Number: EC 1.13.11.34
• Sequence:
  MPSYTVTVATGSQWFAGTDDYIYLSLVGSAGCSEKHLLDKPFYNDFERGAVDSYDVTVDE
  ELGEIQLVRIEKRKYWLNDDWYLKYITLKTPHGDYIEFPCYRWITGDVEVVLRDGRAKLA
  RDDQIHILKQHRRKELETRQKQYRWMEWNPGFPLSIDAKCHKDLPRDIQFDSEKGVDFVL
  NYSKAMENLFINRFMHMFQSSWNDFADFEKIFVKISNTISERVMNHWQEDLMFGYQFLNG
  CNPVLIRRCTELPEKLPVTTEMVECSLERQLSLEQEVQQGNIFIVDFELLDGIDANKTDP
  CTLQFLAAPICLLYKNLANKIVPIAIQLNQIPGDENPIFLPSDAKYDWLLAKIWVRSSDF
  HVHQTITHLLRTHLVSEVFGIAMYRQLPAVHPIFKLLVAHVRFTIAINTKAREQLICECG
  LFDKANATGGGGHVQMVQRAMKDLTYASLCFPEAIKARGMESKEDIPYYFYRDDGLLVWE
  AIRTFTAEVVDIYYEGDQVVEEDPELQDFVNDVYVYGMRGRKSSGFPKSVKSREQLSEYL
  TVVIFTASAQHAAVNFGQYDWCSWIPNAPPTMRAPPPTAKGVVTIEQIVDTLPDRGRSCW
  HLGAVWALSQFQENELFLGMYPEEHFIEKPVKEAMARFRKNLEAIVSVIAERNKKKQLPY
  YYLSPDRIPNSVAI
• Function: Catalyzes the first step in leukotriene biosynthesis, and thereby plays a role in inflammatory processes.
• KEGG Pathway:
  Arachidonic acid metabolism (hsa00590)
  Metabolic pathways (hsa01100)
  Serotonergic synapse (hsa04726)
  Ovarian steroidogenesis (hsa04913)
  Toxoplasmosis (hsa05145)
• Reactome Pathway:
  Synthesis of Leukotrienes (LT) and Eoxins (EX) (R-HSA-2142691)
  Synthesis of Lipoxins (LX) (R-HSA-2142700)
  Interleukin-4 and Interleukin-13 signaling (R-HSA-6785807)
  Neutrophil degranulation (R-HSA-6798695)
  Interleukin-18 signaling (R-HSA-9012546)
  Biosynthesis of D-series resolvins (R-HSA-9018676)
  Biosynthesis of maresins (R-HSA-9018682)
  Biosynthesis of E-series 18(S)-resolvins (R-HSA-9018896)
  Biosynthesis of aspirin-triggered D-series resolvins (R-HSA-9020265)
  Biosynthesis of E-series 18(R)-resolvins (R-HSA-9023661)
  Biosynthesis of DPAn-3-derived protectins and resolvins (R-HSA-9026286)
  Biosynthesis of DPAn-3-derived maresins (R-HSA-9026290)
  Biosynthesis of DPAn-3-derived 13-series resolvins (R-HSA-9026403)
  Biosynthesis of electrophilic Omega-3 PUFA oxo-derivatives (R-HSA-9027604)
  Synthesis of 5-eicosatetraenoic acids (R-HSA-2142688)
• BioCyc Pathway: MetaCyc:HS00336-MON

Molecular Interaction Atlas (MIA) of This DTT

3 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
TEBUFELONE	DMMUE8P	Pain	MG30-MG3Z	Discontinued in Phase 2	[2]
ZD-2138	DMVFCX7	Asthma	CA23	Discontinued in Phase 2	[3]
BW A4C	DMNUMDG	Arthritis	FA20	Terminated	[4]

48 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(+)-3,3'-bisdemethyltanegool	DMNUWVB	Discovery agent	N.A.	Investigative	[5]
(-)-3,3'-bisdemethylpinoresinol	DMGC7F5	Discovery agent	N.A.	Investigative	[5]
(-)-pinoresinol	DM4INSG	Discovery agent	N.A.	Investigative	[5]
(N-(3-phenoxycinnamyl)-acetohydroxamic acid	DM9ATZ8	Discovery agent	N.A.	Investigative	[6]
1-(4-methoxyphenyl)-3-(1,3,4-thiadiazol-2-yl)urea	DMNJ2CS	Discovery agent	N.A.	Investigative	[7]
1-(4-methoxyphenyl)-3-(4-methylthiazol-2-yl)urea	DMYPC0W	Discovery agent	N.A.	Investigative	[7]
1-(4-methoxyphenyl)-3-(5-methylthiazol-2-yl)urea	DMVWIE5	Discovery agent	N.A.	Investigative	[7]
2,4'-Diacetoxy-5,3'-di-(2-propenyl)-biphenyl	DMVPWML	Discovery agent	N.A.	Investigative	[8]
2,4'-Dimethoxy-5,3'-di-(2-propenyl)-biphenyl	DMWNJ84	Discovery agent	N.A.	Investigative	[8]
2,4,5-Triarylimidazole analogue	DMSJBEH	Discovery agent	N.A.	Investigative	[9]
2-(4-methoxyphenyl)-N-(thiazol-2-yl)acetamide	DM1N08O	Discovery agent	N.A.	Investigative	[7]
2-(benzyloxy)naphthalene	DME50RZ	Discovery agent	N.A.	Investigative	[10]
2-phenyl-N-(1,3,4-thiadiazol-2-yl)acetamide	DMFC3B5	Discovery agent	N.A.	Investigative	[7]
2-phenyl-N-(thiazol-2-yl)acetamide	DMP0NW3	Discovery agent	N.A.	Investigative	[7]
3,4,5-trimethoxy-N-(thiazol-2-yl)benzamide	DMU5NRA	Discovery agent	N.A.	Investigative	[7]
3-methoxy-N-(1,3,4-thiadiazol-2-yl)benzamide	DMFEL39	Discovery agent	N.A.	Investigative	[7]
3-methoxy-N-(4-methylthiazol-2-yl)benzamide	DM4WJX3	Discovery agent	N.A.	Investigative	[7]
4'-Methoxy-5,3'-dipropyl-biphenyl-2ol	DM5FRV2	Discovery agent	N.A.	Investigative	[8]
4-(dimethylamino)-N-(thiazol-2-yl)benzamide	DMJP5YH	Discovery agent	N.A.	Investigative	[7]
4-methoxy-N-(thiazol-2-yl)benzamide	DMPQKGY	Discovery agent	N.A.	Investigative	[7]
5,3'-Dipropyl-biphenyl-2,4'-diol	DMJRXLD	Discovery agent	N.A.	Investigative	[8]
HONOKIOL	DMJWT3X	Discovery agent	N.A.	Investigative	[8]
ISAINDIGOTONE	DMD6U4F	Discovery agent	N.A.	Investigative	[11]
ISIS 1820	DMQ5A4Y	Discovery agent	N.A.	Investigative	[12]
ISIS 1821	DMUG2PN	Discovery agent	N.A.	Investigative	[12]
ISIS 1822	DMLJBU8	Discovery agent	N.A.	Investigative	[12]
ISIS 1827	DMPHWMO	Discovery agent	N.A.	Investigative	[12]
ISIS 1831	DM1LWGI	Discovery agent	N.A.	Investigative	[12]
ISIS 2177	DM4VZPU	Discovery agent	N.A.	Investigative	[12]
Isojaspic acid	DMHTBDN	Discovery agent	N.A.	Investigative	[13]
JASPAQUINOL	DMJAEMT	Discovery agent	N.A.	Investigative	[13]
KAEMPFEROL	DMHEMUB	Discovery agent	N.A.	Investigative	[5]
L-689065	DM42BGX	Discovery agent	N.A.	Investigative	[14]
L-702-539	DM92X5T	Discovery agent	N.A.	Investigative	[15]
L-746530	DMUY8MP	Discovery agent	N.A.	Investigative	[16]
Methyl 2-(Benzylamino)-1H-indole-3-carboxylate	DMB1PXR	Discovery agent	N.A.	Investigative	[6]
Methyl 2-(Diallylamino)-1H-indole-3-carboxylate	DMB74WP	Discovery agent	N.A.	Investigative	[6]
METHYLHONOKIOL	DM9YE6K	Discovery agent	N.A.	Investigative	[8]
N-(1,3,4-thiadiazol-2-yl)benzamide	DMWP6OZ	Discovery agent	N.A.	Investigative	[7]
N-(4-methylthiazol-2-yl)-2-phenylacetamide	DM03VXN	Discovery agent	N.A.	Investigative	[7]
N-(4-methylthiazol-2-yl)benzamide	DMTCA2Z	Discovery agent	N.A.	Investigative	[7]
N-(5-methylthiazol-2-yl)-2-phenylacetamide	DM8PNKC	Discovery agent	N.A.	Investigative	[7]
N-(5-methylthiazol-2-yl)benzamide	DMFI057	Discovery agent	N.A.	Investigative	[7]
N-(thiazol-2-yl)benzamide	DM1N7AG	Discovery agent	N.A.	Investigative	[7]
N-hydroxy-N-[1-(4-isobutylphenyl)ethyl]urea	DM4E8NJ	Discovery agent	N.A.	Investigative	[17]
PD-169316	DM1Z3D7	Discovery agent	N.A.	Investigative	[9]
PUUPEHEDIONE	DMF28IU	Discovery agent	N.A.	Investigative	[13]
PUUPEHENONE	DMF3BCK	Discovery agent	N.A.	Investigative	[13]

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	9.43E-03	0.14	0.28

References

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• [14] Substituted thiopyrano[2,3,4-c,d]indoles as potent, selective, and orally active inhibitors of 5-lipoxygenase. Synthesis and biological evaluation ... J Med Chem. 1993 Sep 17;36(19):2771-87.
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