simtuzumab   Click here for help

GtoPdb Ligand ID: 8412

Synonyms: AB0024 | GS 6624 | GS-6624
Compound class: Antibody
Comment: Simtuzumab is an investigational monoclonal antibody targeting lysyl oxidase-like 2 (LOXL2). The antibody is reported to be an allosteric modulator of LOXL2 enzymatic activity [6-7].
Peptide sequence information for this antibody is available from its IMGT/mAb-DB record. Peptide sequence matches reveal that US8461303 is the covering patent [7]. The heavy chain variable domain sequence of simtuzumab (from IMGT) matches the sequence for the AB0023 M20 variant 3 clone in US8461303.
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Ligand Activity Visualisation Charts

These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.

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View interactive charts of activity data across species
References
1. Adamali HI, Maher TM. (2012)
Current and novel drug therapies for idiopathic pulmonary fibrosis.
Drug Des Devel Ther, 6: 261-72. [PMID:23055696]
2. Cano A, Santamaría PG, Moreno-Bueno G. (2012)
LOXL2 in epithelial cell plasticity and tumor progression.
Future Oncol, 8 (9): 1095-108. [PMID:23030485]
3. Chien JW, Richards TJ, Gibson KF, Zhang Y, Lindell KO, Shao L, Lyman SK, Adamkewicz JI, Smith V, Kaminski N et al.. (2014)
Serum lysyl oxidase-like 2 levels and idiopathic pulmonary fibrosis disease progression.
Eur Respir J, 43 (5): 1430-8. [PMID:24177001]
4. Martin A, Salvador F, Moreno-Bueno G, Floristán A, Ruiz-Herguido C, Cuevas EP, Morales S, Santos V, Csiszar K, Dubus P et al.. (2015)
Lysyl oxidase-like 2 represses Notch1 expression in the skin to promote squamous cell carcinoma progression.
EMBO J, 34 (8): 1090-109. [PMID:25759215]
5. Nishioka T, Eustace A, West C. (2012)
Lysyl oxidase: from basic science to future cancer treatment.
Cell Struct Funct, 37 (1): 75-80. [PMID:22453058]
6. Rodriguez HM, Vaysberg M, Mikels A, McCauley S, Velayo AC, Garcia C, Smith V. (2010)
Modulation of lysyl oxidase-like 2 enzymatic activity by an allosteric antibody inhibitor.
J Biol Chem, 285 (27): 20964-74. [PMID:20439985]
7. 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.
8. Tadmor T, Bejar J, Attias D, Mischenko E, Sabo E, Neufeld G, Vadasz Z. (2013)
The expression of lysyl-oxidase gene family members in myeloproliferative neoplasms.
Am J Hematol, 88 (5): 355-8. [PMID:23494965]
9. Van Bergen T, Marshall D, Van de Veire S, Vandewalle E, Moons L, Herman J, Smith V, Stalmans I. (2013)
The role of LOX and LOXL2 in scar formation after glaucoma surgery.
Invest Ophthalmol Vis Sci, 54 (8): 5788-96. [PMID:23821193]