- Advanced search
- Immuno Portal
- Malaria Portal
Compound class: Synthetic organic
Comment: VBY-825 is a reversible cysteine protease inhibitor with high potency against cathepsins B, L, S and V . Human cysteinyl cathepsins are required for proteolytic processing of virally encoded proteins during infection [2-3,5], including a likely requirement for proper processing of the SARS-CoV-2 S protein within the endosome (activating its fusogenic acitivity) . Experimental evidence indicates that VBY-825 has some antiviral activity against SARS-CoV-2 . In in vitro experiments VBY-825 inhibits SARS-CoV-2 entry. It does not inhibit the viral 3C-like protease (3CLpro) or papain-like protease (PLpro), which suggests that its antiviral activity is associated with inhibition of host proteases.
In the oncology setting, a pre-clinical model of pancreatic islet cancer revealed that VBY-825 exhibits significant anti-tumour 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. Elie BT, Gocheva V, Shree T, Dalrymple SA, Holsinger LJ, Joyce JA. (2010)
Identification and pre-clinical testing of a reversible cathepsin protease inhibitor reveals anti-tumor efficacy in a pancreatic cancer model.
Biochimie, 92 (11): 1618-24. [PMID:20447439]
2. Marzi A, Reinheckel T, Feldmann H. (2012)
Cathepsin B & L are not required for ebola virus replication.
PLoS Negl Trop Dis, 6 (12): e1923. [PMID:23236527]
3. Mori Y, Yamashita T, Tanaka Y, Tsuda Y, Abe T, Moriishi K, Matsuura Y. (2007)
Processing of capsid protein by cathepsin L plays a crucial role in replication of Japanese encephalitis virus in neural and macrophage cells.
J Virol, 81 (16): 8477-87. [PMID:17553875]
4. Riva L, Yuan S, Yin X, Martin-Sancho L, Matsunaga N, Pache L, Burgstaller-Muehlbacher S, De Jesus PD, Teriete P, Hull MV et al.. (2020)
Discovery of SARS-CoV-2 antiviral drugs through large-scale compound repurposing.
Nature, [Epub ahead of print]. DOI: 10.1038/s41586-020-2577-1
5. Simmons G, Gosalia DN, Rennekamp AJ, Reeves JD, Diamond SL, Bates P. (2005)
Inhibitors of cathepsin L prevent severe acute respiratory syndrome coronavirus entry.
Proc Natl Acad Sci USA, 102 (33): 11876-81. [PMID:16081529]