lysyl oxidase like 2 | 1.4.3.13 Lysyl oxidases | IUPHAR/BPS Guide to PHARMACOLOGY

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lysyl oxidase like 2

Target not currently curated in GtoImmuPdb

Target id: 2853

Nomenclature: lysyl oxidase like 2

Family: 1.4.3.13 Lysyl oxidases

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

Gene and Protein Information
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
LOR2 | WS9-14 | protein-lysine 6-oxidase | lysyl oxidase homolog 2 | lysyl oxidase-like 2
Database Links
BRENDA
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction
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 Hs Inhibition 7.2 pKi 4
pKi 7.2 (Ki 6.7x10-8 M) [4]
compound 21b [PMID: 31430136] Hs Inhibition 6.8 pIC50 5
pIC50 6.8 (IC50 1.51x10-7 M) [5]
CCT365623 Hs Inhibition 5.8 pIC50 3
pIC50 5.8 (IC50 1.5x10-6 M) [3]
Immuno Process Associations
Immuno Process:  Antigen presentation
GO Annotations:  Associated to 1 GO processes, IEA only
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GO:0005044 scavenger receptor activity IEA
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 12/07/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2853.