The DOI matches its Crossref record; 3 of the 3 references it cites were found in a registry or an index.
Potent D-peptide inhibitors of HIV-1 entry
Open accessAbstract
During HIV-1 entry, the highly conserved gp41 N-trimer pocket region becomes transiently exposed and vulnerable to inhibition. Using mirror-image phage display and structure-assisted design, we have discovered protease-resistant D-amino acid peptides (D-peptides) that bind the N-trimer pocket with high affinity and potently inhibit viral entry. We also report high-resolution crystal structures of two of these D-peptides in complex with a pocket mimic that suggest sources of their high potency. A trimeric version of one of these peptides is the most potent pocket-specific entry inhibitor yet reported by three orders of magnitude (IC 50= 250 pM). These results are the first demonstration that D-peptides can form specific and high-affinity interactions with natural protein targets and strengthen their promise as therapeutic agents. The D-peptides described here address limitations associated with current L-peptide entry inhibitors and are promising leads for the prevention and treatment of HIV/AIDS.
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Harris, J. M., & Chess, R. B. (2003) · Nature Reviews Drug Discovery · doi:10.1038/nrd1033 · Cited by 3,431
Wei, X., Decker, J. M., Liu, H., Zhang, Z., Arani, R. B., Kilby, J. M., Saag, M. S., Wu, X., Shaw, G. M., & Kappes, J. C. (2002) · Antimicrobial Agents and Chemotherapy · doi:10.1128/aac.46.6.1896-1905.2002 · Cited by 1,569
Sadowski, M., Pankiewicz, J., Scholtzova, H., Ripellino, J. A., Li, Y., Schmidt, S. D., Mathews, P. M., Fryer, J. D., Holtzman, D. M., Sigurdsson, E. M., et al. (2004) · The American Journal of Pathology · doi:10.1016/s0002-9440(10)63355-x · Cited by 154
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White, J. M., Delos, S. E., Brecher, M., & Schornberg, K. (2008) · Critical Reviews in Biochemistry and Molecular Biology · doi:10.1080/10409230802058320 · Cited by 892
Wilen, C. B., Tilton, J. C., & Doms, R. W. (2012) · Cold Spring Harbor Perspectives in Medicine · doi:10.1101/cshperspect.a006866 · Cited by 654
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Bird, G. H., Madani, N., Perry, A. F., Princiotto, A. M., Supko, J. G., He, X., Gavathiotis, E., Sodroski, J. G., & Walensky, L. D. (2010) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1002713107 · Cited by 347
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Kopeček, J., & Yang, J. (2012) · Angewandte Chemie International Edition · doi:10.1002/anie.201201040 · Cited by 313
Structural and biological mimicry of protein surface recognition by α/β-peptide foldamers
Horne, W. S., Johnson, L. M., Ketas, T. J., Klasse, P. J., Lu, M., Moore, J. P., & Gellman, S. H. (2009) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0902663106 · Cited by 275
Metadata
- Authors
- Welch, B. D., VanDemark, A. P., Heroux, A., Hill, C. P., & Kay, M. S.
- Venue
- Proceedings of the National Academy of Sciences
- Published
- 2007-10-23
- Volume
- 104
- Issue
- 43
- Pages
- 16828-16833
- ISSN
- 0027-8424 (ISSN-L)
- 1091-6490
- OpenAlex
- W1969552295
- Cited by
- 250
- References
- 3
- FWCI
- 5.37
- Type
- journal article
- Language
- en
- Open access
- green
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