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lysyl oxidase like 2

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Target not currently curated in GtoImmuPdb

Target id: 2853

Nomenclature: lysyl oxidase like 2

Family: 1.4.3.13 Lysyl oxidases

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 774 8p21.3 LOXL2 lysyl oxidase like 2
Mouse - 776 14 D2 Loxl2 lysyl oxidase-like 2
Rat - 776 15p11 Loxl2 lysyl oxidase-like 2
Previous and Unofficial Names Click here for help
LOR2 | WS9-14 | protein-lysine 6-oxidase | lysyl oxidase homolog 2 | lysyl oxidase-like 2
Database Links Click here for help
Alphafold Q9Y4K0 (Hs), P58022 (Mm), B5DF27 (Rn)
BRENDA 1.4.3.13
CATH/Gene3D 3.10.250.10
ChEMBL Target CHEMBL3714029 (Hs), CHEMBL4105831 (Mm), CHEMBL4105908 (Rn)
Ensembl Gene ENSG00000134013 (Hs), ENSMUSG00000034205 (Mm), ENSRNOG00000016758 (Rn)
Entrez Gene 4017 (Hs), 94352 (Mm), 290350 (Rn)
Human Protein Atlas ENSG00000134013 (Hs)
KEGG Enzyme 1.4.3.13
KEGG Gene hsa:4017 (Hs), mmu:94352 (Mm), rno:290350 (Rn)
OMIM 606663 (Hs)
Pharos Q9Y4K0 (Hs)
RefSeq Nucleotide NM_002318 (Hs), NM_033325 (Mm), NM_001106047 (Rn)
RefSeq Protein NP_002309 (Hs), NP_201582 (Mm), NP_001099517 (Rn)
UniProtKB Q9Y4K0 (Hs), P58022 (Mm), B5DF27 (Rn)
Wikipedia LOXL2 (Hs)
Enzyme Reaction Click here for help
EC Number: 1.4.3.13 H2O + L-lysyl-[protein] + O2 = [protein]-(S)-2-amino-6-oxohexanoate + H2O2 + NH4+
Description Reaction Reference
Reaction is required for collagen and elastin cross-linking in the biosynthesis of normal mature extracellular matrices. peptidyl-L-lysyl-peptide + O2 + H2O = peptidyl-allysyl-peptide + NH3 + H2O2 2

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Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
simtuzumab Peptide Primary target of this compound Hs Inhibition 7.2 pKi 4
⤷ pKi 7.2 (Ki 6.7x10-8 M) [4]
compound 21b [PMID: 31430136] Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 6.8 pIC50 5
⤷ pIC50 6.8 (IC50 1.51x10-7 M) [5]
CCT365623 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 5.8 pIC50 3
⤷ pIC50 5.8 (IC50 1.5x10-6 M) [3]
Immuno Process Associations
Immuno Process:  Antigen presentation
General Comments
Genetic, chemical or antibody-mediated inhibition of LOXL2 results in decreased metastasis in orthotopic and transgenic breast cancer models [1].

References

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1. Barker HE, Chang J, Cox TR, Lang G, Bird D, Nicolau M, Evans HR, Gartland A, Erler JT. (2011) LOXL2-mediated matrix remodeling in metastasis and mammary gland involution. Cancer Res, 71 (5): 1561-72. [PMID:21233336]

2. Harris ED, Gonnerman WA, Savage JE, O'Dell BL. (1974) Connective tissue amine oxidase. II. Purification and partial characterization of lysyl oxidase from chick aorta. Biochim Biophys Acta, 341 (2): 332-44. [PMID:4838158]

3. Leung L, Niculescu-Duvaz D, Smithen D, Lopes F, Callens C, McLeary R, Saturno G, Davies L, Aljarah M, Brown M et al.. (2019) Anti-metastatic Inhibitors of Lysyl Oxidase (LOX): Design and Structure-Activity Relationships. J Med Chem, 62 (12): 5863-5884. [PMID:31070916]

4. Smith V, Ogg S, Van Vlasselaer P, Barry VE, Marshall D, Holzer AK, Rodriguez H, Oyasu M, McCauley SA, Garcia CA et al.. (2013) LOX and LOXL2 inhibitors and uses thereof. Patent number: US8461303 B2. Assignee: Gilead Biologics, Inc.. Priority date: 02/08/2007. Publication date: 11/06/2013.

5. Smithen DA, Leung LMH, Challinor M, Lawrence R, Tang H, Niculescu-Duvaz D, Pearce SP, Mcleary R, Lopes F, Aljarah M et al.. (2020) 2-Aminomethylene-5-sulfonylthiazole Inhibitors of Lysyl Oxidase (LOX) and LOXL2 Show Significant Efficacy in Delaying Tumor Growth. J Med Chem, 63 (5): 2308-2324. [PMID:31430136]

How to cite this page

1.4.3.13 Lysyl oxidases: lysyl oxidase like 2. Last modified on 11/09/2019. Accessed on 19/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2853.