The DOI matches its Crossref record; 5 of the 5 references it cites were found in a registry or an index.
Allostery and population shift in drug discovery
Open accessAbstract
Proteins can exist in a large number of conformations around their native states that can be characterized by an energy landscape. The landscape illustrates individual valleys, which are the conformational substates. From the functional standpoint, there are two key points: first, all functionally relevant substates pre-exist; and second, the landscape is dynamic and the relative populations of the substates will change following allosteric events. Allosteric events perturb the structure, and the energetic strain propagates and shifts the population. This can lead to changes in the shapes and properties of target binding sites. Here we present an overview of dynamic conformational ensembles focusing on allosteric events in signaling. We propose that combining equilibrium fluctuation concepts with genomic screens could help drug discovery.
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Cites
Intrinsic Disorder in Cell-signaling and Cancer-associated Proteins
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Folding funnels and binding mechanisms
Ma, B., Kumar, S., Tsai, C.-J., & Nussinov, R. (1999) · Protein Engineering, Design and Selection · doi:10.1093/protein/12.9.713 · Cited by 594
Self-citationHuman Cancer Protein-Protein Interaction Network: A Structural Perspective
Kar, G., Gursoy, A., & Keskin, O. (2009) · PLoS Computational Biology · doi:10.1371/journal.pcbi.1000601 · Cited by 235
Self-citationBoehr, D. D., McElheny, D., Dyson, H. J., & Wright, P. E. (2010) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0914163107 · Cited by 142
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Cited by
Wei, G., Xi, W., Nussinov, R., & Ma, B. (2016) · Chemical Reviews · doi:10.1021/acs.chemrev.5b00562 · Cited by 436
Self-citationRas Conformational Ensembles, Allostery, and Signaling
Lu, S., Jang, H., Muratcioglu, S., Gursoy, A., Keskin, O., Nussinov, R., & Zhang, J. (2016) · Chemical Reviews · doi:10.1021/acs.chemrev.5b00542 · Cited by 355
Self-citationTuncbag, N., Gursoy, A., Nussinov, R., & Keskin, O. (2011) · Nature Protocols · doi:10.1038/nprot.2011.367 · Cited by 263
Self-citationControlling Allosteric Networks in Proteins
Dokholyan, N. V. (2016) · Chemical Reviews · doi:10.1021/acs.chemrev.5b00544 · Cited by 260
Dynamic Allostery: Linkers Are Not Merely Flexible
Ma, B., Tsai, C.-J., Haliloğlu, T., & Nussinov, R. (2011) · Structure · doi:10.1016/j.str.2011.06.002 · Cited by 222
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Metadata
- Authors
- Kar, G., Keskin, O., Gursoy, A., & Nussinov, R.
- Venue
- Current Opinion in Pharmacology
- Publisher
- Elsevier BV
- Published
- 2010-12
- Volume
- 10
- Issue
- 6
- Pages
- 715-722
- ISSN
- 1471-4892 (ISSN-L)
- OpenAlex
- W2164385498
- Cited by
- 187
- References
- 5
- FWCI
- 7.44
- Type
- journal article
- Language
- en
- Open access
- green
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