The DOI matches its Crossref record; 5 of the 5 references it cites were found in a registry or an index.
Design and Applications of Bifunctional Small Molecules: Why Two Heads Are Better Than One
Open accessAbstract
Induction of protein--protein interactions is a daunting challenge, but recent studies show promise for small molecules that specifically bring two or more protein molecules together for enhanced or novel biological effect. The first such bifunctional molecules were the rapamycin- and FK506-based "chemical inducers of dimerization", but the field has since expanded with new molecules and new applications in chemical genetics and cell biology. Examples include coumermycin-mediated gyrase B dimerization, proteolysis targeting chimeric molecules (PROTACs), drug hybrids, and strategies for exploiting multivalency in toxin binding and antibody recruitment. This Review discusses these and other advances in the design and use of bifunctional small molecules and potential strategies for future systems.
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Self-citationSmall-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
Schneekloth, A. R., Pucheault, M., Tae, H. S., & Crews, C. M. (2008) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2008.07.114 · Cited by 635
Self-citationMandel, S., Amit, T., Bar-Am, O., & Youdim, M. B. H. (2007) · Progress in Neurobiology · doi:10.1016/j.pneurobio.2007.06.001 · Cited by 164
Youdim, M. B. H., Fridkin, M., & Zheng, H. (2005) · Mechanisms of Ageing and Development · doi:10.1016/j.mad.2004.08.023 · Cited by 128
Cited by
Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4
Zengerle, M., Chan, K.-H., & Ciulli, A. (2015) · ACS Chemical Biology · doi:10.1021/acschembio.5b00216 · Cited by 1,056
Small‐Molecule PROTACS: New Approaches to Protein Degradation
Toure, M., & Crews, C. M. (2016) · Angewandte Chemie International Edition · doi:10.1002/anie.201507978 · Cited by 674
Self-citationProtein Degradation by In-Cell Self-Assembly of Proteolysis Targeting Chimeras
Lebraud, H., Wright, D. J., Johnson, C. N., & Heightman, T. D. (2016) · ACS Central Science · doi:10.1021/acscentsci.6b00280 · Cited by 413
Chemically Controlled Protein Assembly: Techniques and Applications
Fegan, A., White, B., Carlson, J. C. T., & Wagner, C. R. (2010) · Chemical Reviews · doi:10.1021/cr8002888 · Cited by 294
Crew, A. P., Raina, K., Dong, H., Qian, Y., Wang, J., Vigil, D., Serebrenik, Y. V., Hamman, B. D., Morgan, A., Ferraro, C., et al. (2018) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.7b00635 · Cited by 257
Self-citationManiaci, C., Hughes, S. J., Testa, A., Chen, W., Lamont, D. J., Rocha, S., Alessi, D. R., Romeo, R., & Ciulli, A. (2017) · Nature Communications · doi:10.1038/s41467-017-00954-1 · Cited by 245
Impact of linker length on the activity of PROTACs
Cyrus, K., Wehenkel, M., Choi, E.-Y., Han, H.-J., Lee, H., Swanson, H., & Kim, K.-B. (2010) · Molecular BioSystems · doi:10.1039/c0mb00074d · Cited by 232
Small‐Molecule‐Mediated Degradation of the Androgen Receptor through Hydrophobic Tagging
Gustafson, J. L., Neklesa, T. K., Cox, C. S., Roth, A. G., Buckley, D. L., Tae, H. S., Sundberg, T. B., Stagg, D. B., Hines, J., McDonnell, D. P., et al. (2015) · Angewandte Chemie International Edition · doi:10.1002/anie.201503720 · Cited by 206
Self-citationRNA‐PROTACs: Degraders of RNA‐Binding Proteins
Ghidini, A., Cléry, A., Halloy, F., Allain, F. H. T., & Hall, J. (2021) · Angewandte Chemie International Edition · doi:10.1002/anie.202012330 · Cited by 197
DeepPROTACs is a deep learning-based targeted degradation predictor for PROTACs
Li, F., Hu, Q., Zhang, X., Sun, R., Liu, Z., Wu, S., Tian, S., Ma, X., Dai, Z., Yang, X., et al. (2022) · Nature Communications · doi:10.1038/s41467-022-34807-3 · Cited by 159
Plasticity in designing PROTACs for selective and potent degradation of HDAC6
Yang, H., Lv, W., He, M., Deng, H., Li, H., Wu, W., & Rao, Y. (2019) · Chemical Communications · doi:10.1039/c9cc08509b · Cited by 108
Privileged Electrophile Sensors: A Resource for Covalent Drug Development
Long, M. J. C., & Aye, Y. (2017) · Cell Chemical Biology · doi:10.1016/j.chembiol.2017.05.023 · Cited by 81
Bifunctional Small‐Molecule Ligands of K‐Ras Induce Its Association with Immunophilin Proteins
Zhang, Z., & Shokat, K. M. (2019) · Angewandte Chemie International Edition · doi:10.1002/anie.201910124 · Cited by 66
Niedermolekulare PROTACs: neue Wege zum Abbau von Proteinen
Toure, M., & Crews, C. M. (2016) · Angewandte Chemie · doi:10.1002/ange.201507978 · Cited by 40
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Metadata
- Authors
- Corson, T. W., Aberle, N., & Crews, C. M.
- Venue
- ACS Chemical Biology
- Publisher
- American Chemical Society (ACS)
- Published
- 2008-10-24
- Volume
- 3
- Issue
- 11
- Pages
- 677-692
- ISSN
- 1554-8929 (ISSN-L)
- 1554-8937
- OpenAlex
- W1990350046
- Cited by
- 165
- References
- 5
- FWCI
- 3.10
- Type
- journal article
- Language
- en
- Open access
- green
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