andecaliximab   Click here for help

GtoPdb Ligand ID: 9510

Synonyms: GS-5745 | GS5745
Immunopharmacology Ligand
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 [1].
Click here for help
References
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]