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Synonyms: GS-5745 | GS5745
Compound class: Antibody
Comment: Gilead Sciences designed andecaliximab (GS-5745), a humanized anti-MMP9 monoclonal antibody, for potential to treat solid tumours and inflammatory disorders [1-2]. GS-5745 inhibits MMP-9 activity by a combination of blocking proenzyme (zymogen) conversion to active enzyme, and allosterically inhibiting active MMP-9 catalytic activity .
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.✖
1. Appleby TC, Greenstein AE, Hung M, Liclican A, Velasquez M, Villaseñor AG, Wang R, Wong MH, Liu X, Papalia GA et al.. (2017)
Biochemical characterization and structure determination of a potent, selective antibody inhibitor of human MMP9.
J Biol Chem, 292 (16): 6810-6820. [PMID:28235803]
2. Marshall DC, Lyman SK, McCauley S, Kovalenko M, Spangler R, Liu C, Lee M, O'Sullivan C, Barry-Hamilton V, Ghermazien H et al.. (2015)
Selective Allosteric Inhibition of MMP9 Is Efficacious in Preclinical Models of Ulcerative Colitis and Colorectal Cancer.
PLoS ONE, 10 (5): e0127063. [PMID:25961845]