Target Information

Target General Infomation
Target ID
T46642
Former ID
TTDC00062
Target Name
Arachidonate 5-lipoxygenaseactivating protein
Gene Name
ALOX5AP
Synonyms
FLAP; MK-886-binding protein; ALOX5AP
Target Type
Discontinued
Disease Asthma [ICD10: J45]
Allergy [ICD9: 995.3; ICD10: T78.4]
Cardiovascular disorder [ICD10: I00-I99]
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.
BioChemical Class
Membrane-associated metabolism proteins
Target Validation
T46642
UniProt ID
P20292
Sequence
MDQETVGNVVLLAIVTLISVVQNGFFAHKVEHESRTQNGRSFQRTGTLAFERVYTANQNC
VDAYPTFLAVLWSAGLLCSQVPAAFAGLMYLFVRQKYFVGYLGERTQSTPGYIFGKRIIL
FLFLMSVAGIFNYYLIFFFGSDFENYIKTISTTISPLLLIP
Drugs and Mode of Action
Drug(s) DG031 Drug Info Discontinued in Phase 3 Asthma [1], [2]
AM103 Drug Info Discontinued in Phase 2 Cardiovascular disorder [3]
GSK2190914 Drug Info Discontinued in Phase 2 Asthma [3]
GSK2190915 Drug Info Discontinued in Phase 2 Asthma [4]
A-93178 Drug Info Terminated Allergy [5]
Modulator A-93178 Drug Info [5]
Inhibitor AM103 Drug Info [6]
DG031 Drug Info [7], [8]
GSK2190914 Drug Info [2]
GSK2190915 Drug Info [9]
L-671,480 Drug Info [10]
L-674,573 Drug Info [11]
L-689,037 Drug Info [11]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
NetPath Pathway IL4 Signaling Pathway
TGF_beta_Receptor Signaling Pathway
Leptin Signaling Pathway
PANTHER Pathway Inflammation mediated by chemokine and cytokine signaling pathway
WikiPathways Nuclear Receptors Meta-Pathway
Arachidonic acid metabolism
Eicosanoid Synthesis
Selenium Micronutrient Network
References
REF 1(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: 5148).
REF 2FLAP inhibitors for the treatment of inflammatory diseases. Curr Opin Investig Drugs. 2009 Nov;10(11):1163-72.
REF 3Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026047)
REF 4Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027280)
REF 5Characterization of A-93178, an iminoxy-quinoline inhibitor of leukotriene biosynthesis. Adv Exp Med Biol. 1997;433:91-4.
REF 6AM103 Experimental Treatment for Respiratory Diseases. Amira Pharmaceuticals/GSK. 2009.
REF 7Effects of a 5-lipoxygenase-activating protein inhibitor on biomarkers associated with risk of myocardial infarction: a randomized trial. JAMA. 2005 May 11;293(18):2245-56.
REF 8BAY x 1005 attenuates atherosclerosis in apoE/LDLR - double knockout mice. J Physiol Pharmacol. 2007 Sep;58(3):583-8.
REF 9Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
REF 105-Lipoxygenase-activating protein is the target of a quinoline class of leukotriene synthesis inhibitors. Mol Pharmacol. 1991 Jul;40(1):22-7.
REF 115-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.

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