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15-LOX-1

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Target id: 1388

Nomenclature: 15-LOX-1

Family: Lipoxygenases

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 662 17p13.2 ALOX15 arachidonate 15-lipoxygenase
Mouse - 663 11 42.99 cM Alox15 arachidonate 15-lipoxygenase
Rat - 663 10q24 Alox15 arachidonate 15-lipoxygenase
Previous and Unofficial Names Click here for help
arachidonate ω-6 lipoxygenase | 12/15-LOX | 12-LOX | Alox12 | Alox12l | arachidonate 12-lipoxygenase, leukocyte-type | arachidonate 15-lipoxygenase | 12-LO
Database Links Click here for help
Alphafold P16050 (Hs), P39654 (Mm), Q02759 (Rn)
BRENDA 1.13.11.33
CATH/Gene3D 2.60.60.20
ChEMBL Target CHEMBL2903 (Hs), CHEMBL3259476 (Mm), CHEMBL2741 (Rn)
Ensembl Gene ENSG00000161905 (Hs), ENSMUSG00000018924 (Mm), ENSRNOG00000019183 (Rn)
Entrez Gene 246 (Hs), 11687 (Mm), 81639 (Rn)
Human Protein Atlas ENSG00000161905 (Hs)
KEGG Enzyme 1.13.11.33
KEGG Gene hsa:246 (Hs), mmu:11687 (Mm), rno:81639 (Rn)
OMIM 152392 (Hs)
Pharos P16050 (Hs)
UniProtKB P16050 (Hs), P39654 (Mm), Q02759 (Rn)
Wikipedia ALOX15 (Hs)
Enzyme Reaction Click here for help
EC Number: 1.13.11.33 Arachidonic acid + O2 = 15S-HPETE
Description Reaction Reference
Linoleic acid + O2 => 13S-HPODE

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
compound 34 [PMID: 20866075] Small molecule or natural product Primary target of this compound Hs Inhibition >8.0 pKi 3
⤷ pKi >8.0 (Ki <1x10-8 M) [3]
PD-146176 Small molecule or natural product Hs Inhibition 6.7 pKi 4
⤷ pKi 6.7 [4]
ML351 Small molecule or natural product Hs Inhibition 6.7 pIC50 2
⤷ pIC50 6.7 (IC50 2x10-7 M) [2]
Allosteric Modulators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
PKUMDL_MH_1001 Small molecule or natural product Immunopharmacology Ligand Hs Positive 5.4 pKd 1
⤷ pKd 5.4 (Kd 3.9x10-6 M) [1]
Description: Determined by surface plasmon resonance (SPR)
Immuno Process Associations
Immuno Process:  Inflammation
Immuno Process:  Antigen presentation
Immuno Process:  T cell (activation)
Immuno Process:  B cell (activation)
Immuno Process:  Immune regulation
Immuno Process:  Cytokine production & signalling

References

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1. Meng H, McClendon CL, Dai Z, Li K, Zhang X, He S, Shang E, Liu Y, Lai L. (2016) Discovery of Novel 15-Lipoxygenase Activators To Shift the Human Arachidonic Acid Metabolic Network toward Inflammation Resolution. J Med Chem, 59 (9): 4202-9. [PMID:26290290]

2. Rai G, Joshi N, Perry S, Yasgar A, Schultz L, Jung JE, Liu Y, Terasaki Y, Diaz G, Kenyon V et al.. (2010) Discovery of ML351, a Potent and Selective Inhibitor of Human 15-Lipoxygenase-1. Probe Reports from the NIH Molecular Libraries Program,. [PMID:24672829]

3. Rai G, Kenyon V, Jadhav A, Schultz L, Armstrong M, Jameson JB, Hoobler E, Leister W, Simeonov A, Holman TR et al.. (2010) Discovery of potent and selective inhibitors of human reticulocyte 15-lipoxygenase-1. J Med Chem, 53 (20): 7392-404. [PMID:20866075]

4. Sendobry SM, Cornicelli JA, Welch K, Bocan T, Tait B, Trivedi BK, Colbry N, Dyer RD, Feinmark SJ, Daugherty A. (1997) Attenuation of diet-induced atherosclerosis in rabbits with a highly selective 15-lipoxygenase inhibitor lacking significant antioxidant properties. Br J Pharmacol, 120 (7): 1199-206. [PMID:9105693]

Contributors

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