General Information of Drug Therapeutic Target (DTT) (ID: TTDMBF5)

DTT Name Arachidonate 5-lipoxygenase activating protein (FLAP)
Synonyms MK-886-binding protein; FLAP; ALOX5AP
Gene Name ALOX5AP
DTT Type
Discontinued target
[1]
UniProt ID
AL5AP_HUMAN
TTD ID
T46642
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MDQETVGNVVLLAIVTLISVVQNGFFAHKVEHESRTQNGRSFQRTGTLAFERVYTANQNC
VDAYPTFLAVLWSAGLLCSQVPAAFAGLMYLFVRQKYFVGYLGERTQSTPGYIFGKRIIL
FLFLMSVAGIFNYYLIFFFGSDFENYIKTISTTISPLLLIP
Function
Required for leukotrienebiosynthesis by ALOX5 (5- lipoxygenase). Anchors ALOX5 to the membrane. Binds arachidonic acid, and could play an essential role in the transfer of arachidonic acid to ALOX5. Binds to MK-886, a compound that blocks the biosynthesis of leukotrienes.
KEGG Pathway
Fc epsilon RI signaling pathway (hsa04664 )
Reactome Pathway
Synthesis of Leukotrienes (LT) and Eoxins (EX) (R-HSA-2142691 )
Synthesis of Lipoxins (LX) (R-HSA-2142700 )
Synthesis of 5-eicosatetraenoic acids (R-HSA-2142688 )
BioCyc Pathway
MetaCyc:ENSG00000132965-MON

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DTT
6 Discontinued Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
DG031 DMO3AJS Asthma CA23 Discontinued in Phase 3 [1]
AM103 DMAQNBW Cardiovascular disease BA00-BE2Z Discontinued in Phase 2 [2]
GSK2190914 DMHZQ0T Asthma CA23 Discontinued in Phase 2 [3]
GSK2190915 DM89AV2 Asthma CA23 Discontinued in Phase 2 [4]
AZD4769 DMA3OWI Solid tumour/cancer 2A00-2F9Z Discontinued in Phase 1 [5]
A-93178 DM1KBAY Allergy 4A80-4A85 Terminated [6]
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⏷ Show the Full List of 6 Discontinued Drug(s)
2 Investigative Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
L-671,480 DMP4QCJ Discovery agent N.A. Investigative [7]
L-689,037 DMCH3ZK Discovery agent N.A. Investigative [5]
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Molecular Expression Atlas (MEA) of This DTT

Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This DTT
Disease Name ICD 11 Studied Tissue p-value Fold-Change Z-score
Asthma CA23 Nasal and bronchial airway 9.89E-01 -0.06 -0.05
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References

1 BAY x 1005 attenuates atherosclerosis in apoE/LDLR - double knockout mice. J Physiol Pharmacol. 2007 Sep;58(3):583-8.
2 AM103 Experimental Treatment for Respiratory Diseases. Amira Pharmaceuticals/GSK. 2009.
3 FLAP inhibitors for the treatment of inflammatory diseases. Curr Opin Investig Drugs. 2009 Nov;10(11):1163-72.
4 Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
5 5-Lipoxygenase-activating protein is the target of a novel hybrid of two classes of leukotriene biosynthesis inhibitors. Mol Pharmacol. 1992 Feb;41(2):267-72.
6 Characterization of A-93178, an iminoxy-quinoline inhibitor of leukotriene biosynthesis. Adv Exp Med Biol. 1997;433:91-4.
7 5-Lipoxygenase-activating protein is the target of a quinoline class of leukotriene synthesis inhibitors. Mol Pharmacol. 1991 Jul;40(1):22-7.