Target Information
Target General Infomation | |||||
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Target ID |
T46642
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Former ID |
TTDC00062
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Target Name |
Arachidonate 5-lipoxygenaseactivating protein
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Gene Name |
ALOX5AP
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Synonyms |
FLAP; MK-886-binding protein; ALOX5AP
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Target Type |
Discontinued
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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.
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BioChemical Class |
Membrane-associated metabolism proteins
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Target Validation |
T46642
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UniProt ID | |||||
Sequence |
MDQETVGNVVLLAIVTLISVVQNGFFAHKVEHESRTQNGRSFQRTGTLAFERVYTANQNC
VDAYPTFLAVLWSAGLLCSQVPAAFAGLMYLFVRQKYFVGYLGERTQSTPGYIFGKRIIL FLFLMSVAGIFNYYLIFFFGSDFENYIKTISTTISPLLLIP |
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Drugs and Mode of Action | |||||
Drug(s) | DG031 | Drug Info | Discontinued in Phase 3 | Asthma | [468211], [530488] |
AM103 | Drug Info | Discontinued in Phase 2 | Cardiovascular disorder | [548500] | |
GSK2190914 | Drug Info | Discontinued in Phase 2 | Asthma | [548500] | |
GSK2190915 | Drug Info | Discontinued in Phase 2 | Asthma | [548641] | |
A-93178 | Drug Info | Terminated | Allergy | [534613] | |
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 468211 | (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 530488 | FLAP inhibitors for the treatment of inflammatory diseases. Curr Opin Investig Drugs. 2009 Nov;10(11):1163-72. | ||||
Ref 534613 | Characterization of A-93178, an iminoxy-quinoline inhibitor of leukotriene biosynthesis. Adv Exp Med Biol. 1997;433:91-4. | ||||
Ref 530488 | FLAP inhibitors for the treatment of inflammatory diseases. Curr Opin Investig Drugs. 2009 Nov;10(11):1163-72. | ||||
Ref 534613 | Characterization of A-93178, an iminoxy-quinoline inhibitor of leukotriene biosynthesis. Adv Exp Med Biol. 1997;433:91-4. | ||||
Ref 536008 | 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. | ||||
Ref 536080 | Effects 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 536517 | BAY x 1005 attenuates atherosclerosis in apoE/LDLR - double knockout mice. J Physiol Pharmacol. 2007 Sep;58(3):583-8. |
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