The DOI matches its Crossref record; 3 of the 3 references it cites were found in a registry or an index.
Emerging principles in protease-based drug discovery
Open accessAbstract
Proteases have an important role in many signalling pathways, and represent potential drug targets for diseases ranging from cardiovascular disorders to cancer, as well as for combating many parasites and viruses. Although inhibitors of well-established protease targets such as angiotensin-converting enzyme and HIV protease have shown substantial therapeutic success, developing drugs for new protease targets has proved challenging in recent years. This in part could be due to issues such as the difficulty of achieving selectivity when targeting protease active sites. This Perspective discusses the general principles in protease-based drug discovery, highlighting the lessons learned and the emerging strategies, such as targeting allosteric sites, which could help harness the therapeutic potential of new protease targets.
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Cites
The apoptosome: Signalling platform of cell death
Riedl, S. J., & Salvesen, G. S. (2007) · Nature Reviews Molecular Cell Biology · doi:10.1038/nrm2153 · Cited by 1,097
Self-citationAllosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders
Jeffrey Conn, P., Christopoulos, A., & Lindsley, C. W. (2009) · Nature Reviews Drug Discovery · doi:10.1038/nrd2760 · Cited by 1,063
Human inhibitor of apoptosis proteins: why XIAP is the black sheep of the family
Eckelman, B. P., Salvesen, G. S., & Scott, F. L. (2006) · The EMBO Reports · doi:10.1038/sj.embor.7400795 · Cited by 813
Self-citation
Cited by
Rut, W., Lv, Z., Zmudzinski, M., Patchett, S., Nayak, D., Snipas, S. J., El Oualid, F., Huang, T. T., Bekes, M., Drag, M., et al. (2020) · Science Advances · doi:10.1126/sciadv.abd4596 · Cited by 459
Self-citationDiscovery of specific inhibitors of human USP7/HAUSP deubiquitinating enzyme.
Reverdy, C., Conrath, S., Lopez, R., Planquette, C., Atmanene, C., Collura, V., Harpon, J., Battaglia, V., Vivat, V., Sippl, W., et al. (2012) · Chemistry & Biology · doi:10.1016/j.chembiol.2012.02.007 · Cited by 270
Bacterial proteases, untapped antimicrobial drug targets
Culp, E., & Wright, G. D. (2017) · The Journal of Antibiotics · doi:10.1038/ja.2016.138 · Cited by 244
Kasperkiewicz, P., Poreba, M., Snipas, S. J., Parker, H., Winterbourn, C. C., Salvesen, G. S., & Drag, M. (2014) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1318548111 · Cited by 189
Self-citationDruggable Orthosteric and Allosteric Hot Spots to Target Protein-protein Interactions
Ma, B., & Nussinov, R. (2014) · Current Pharmaceutical Design · doi:10.2174/13816128113199990073 · Cited by 45
Metadata
- Authors
- Drag, M., & Salvesen, G. S.
- Venue
- Nature Reviews Drug Discovery
- Published
- 2010-09
- Volume
- 9
- Issue
- 9
- Pages
- 690-701
- ISSN
- 1474-1776 (ISSN-L)
- 1474-1784
- OpenAlex
- W2017871159
- Cited by
- 601
- References
- 3
- FWCI
- 1.70
- Type
- journal article
- Language
- en
- Open access
- green
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