15-LOX-1 | Lipoxygenases | IUPHAR/BPS Guide to PHARMACOLOGY

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15-LOX-1

Target not currently curated in GtoImmuPdb

Target id: 1388

Nomenclature: 15-LOX-1

Family: Lipoxygenases

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

Contents:

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - - ALOX15 arachidonate 15-lipoxygenase
Mouse - - Alox15 arachidonate 15-lipoxygenase
Rat - - Alox15 arachidonate 15-lipoxygenase
Previous and Unofficial Names
arachidonate ω-6 lipoxygenase | 12/15-LOX | 12-LOX | Alox12 | Alox12l | arachidonate 12-lipoxygenase, leukocyte-type | arachidonate 15-lipoxygenase | 12-LO
Database Links
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)
UniProtKB P16050 (Hs), P39654 (Mm), Q02759 (Rn)
Wikipedia ALOX15 (Hs)
Enzyme Reaction
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

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] Hs Inhibition >8.0 pKi 3
⤷ pKi >8.0 (Ki <1x10-8 M) [3]
ML351 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 Hs Positive 5.4 pKd 1
⤷ pKd 5.4 (Kd 3.9x10-6 M) [1]
Description: Determined by surface plasmon resonance (SPR)

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]

Contributors

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