The DOI matches its Crossref record; 5 of the 5 references it cites were found in a registry or an index.
The Challenge of Drugging Undruggable Targets in Cancer: Lessons Learned from Targeting BCL-2 Family Members
Abstract
The genomic and proteomic revolutions have provided us with an ever-increasing number of mechanistic insights into cancer pathogenesis. Mutated genes and pathologic protein products have emerged as the basis for modern anticancer drug development. With the increasing realization of the importance of disrupting oncogenic protein-protein interaction, new challenges have emerged for classical small molecule and protein-based drug modalities, i.e., the critical need to target flat and extended protein surfaces. Here, we highlight two distinct technologies that are being used to bridge the pharmacologic gap between small molecules and protein therapeutics. With the BCL-2 family of survival proteins as their substrate for intracellular targeting, we conclude that peptide stapling and fragment-based drug discovery show promise to traverse the critical surface features of proteins that drive human cancer.
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Hopkins, A. L., & Groom, C. R. (2002) · Nature Reviews Drug Discovery · doi:10.1038/nrd892 · Cited by 3,305
Chen, L., Willis, S. N., Wei, A., Smith, B. J., Fletcher, J. I., Hinds, M. G., Colman, P. M., Day, C. L., Adams, J. M., & Huang, D. C. S. (2005) · Molecular Cell · doi:10.1016/j.molcel.2004.12.030 · Cited by 1,816
Small-molecule inhibitors of protein–protein interactions: progressing towards the dream
Arkin, M. R., & Wells, J. A. (2004) · Nature Reviews Drug Discovery · doi:10.1038/nrd1343 · Cited by 1,705
Activation of Apoptosis in Vivo by a Hydrocarbon-Stapled BH3 Helix
Walensky, L. D., Kung, A. L., Escher, I., Malia, T. J., Barbuto, S., Wright, R. D., Wagner, G., Verdine, G. L., & Korsmeyer, S. J. (2004) · Science · doi:10.1126/science.1099191 · Cited by 1,349
Self-citationSchafmeister, C. E., Po, J., & Verdine, G. L. (2000) · Journal of the American Chemical Society · doi:10.1021/ja000563a · Cited by 1,037
Self-citation
Cited by
Principles of cancer therapy: oncogene and non-oncogene addiction
Luo, J., Solimini, N. L., & Elledge, S. J. (2009) · Cell · doi:10.1016/j.cell.2009.02.024 · Cited by 1,765
The role of BCL-2 family proteins in regulating apoptosis and cancer therapy
Qian, S., Wei, Z., Yang, W., Huang, J., Yang, Y., & Wang, J. (2022) · Frontiers in Oncology · doi:10.3389/fonc.2022.985363 · Cited by 1,011
Drugging the ‘undruggable’ cancer targets
Dang, C. V., Reddy, E. P., Shokat, K. M., & Soucek, L. (2017) · Nature Reviews Cancer · doi:10.1038/nrc.2017.36 · Cited by 927
Advances in Biomaterials for Drug Delivery
Fenton, O. S., Olafson, K. N., Pillai, P. S., Mitchell, M. J., & Langer, R. (2018) · Advanced Materials · doi:10.1002/adma.201705328 · Cited by 855
MYC Activation Is a Hallmark of Cancer Initiation and Maintenance
Gabay, M., Li, Y., & Felsher, D. W. (2014) · Cold Spring Harbor Perspectives in Medicine · doi:10.1101/cshperspect.a014241 · Cited by 818
Metadata
- Authors
- Verdine, G. L., & Walensky, L. D.
- Venue
- Clinical Cancer Research
- Published
- 2007-12-15
- Volume
- 13
- Issue
- 24
- Pages
- 7264-7270
- ISSN
- 1078-0432 (ISSN-L)
- 1557-3265
- OpenAlex
- W2123196322
- Cited by
- 361
- References
- 5
- FWCI
- 4.31
- Type
- journal article
- Language
- en
- Open access
- closed
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- Verdine, G. L., & Walensky, L. D. (2007). The Challenge of Drugging Undruggable Targets in Cancer: Lessons Learned from Targeting BCL-2 Family Members. Clinical Cancer Research. https://doi.org/10.1158/1078-0432.ccr-07-2184
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