The DOI matches its Crossref record.
Potent Inhibition of HIV-1 Infectivity in Macrophages and Lymphocytes by a Novel CCR5 Antagonist
Abstract
The chemokine receptors CXCR4 and CCR5 have recently been shown to act as coreceptors, in concert with CD4, for human immunodeficiency virus–type 1 (HIV-1) infection. RANTES and other chemokines that interact with CCR5 and block infection of peripheral blood mononuclear cell cultures inhibit infection of primary macrophages inefficiently at best. If used to treat HIV-1–infected individuals, these chemokines could fail to influence HIV replication in nonlymphocyte compartments while promoting unwanted inflammatory side effects. A derivative of RANTES that was created by chemical modification of the amino terminus, aminooxypentane (AOP)–RANTES, did not induce chemotaxis and was a subnanomolar antagonist of CCR5 function in monocytes. It potently inhibited infection of diverse cell types (including macrophages and lymphocytes) by nonsyncytium-inducing, macrophage-tropic HIV-1 strains. Thus, activation of cells by chemokines is not a prerequisite for the inhibition of viral uptake and replication. Chemokine receptor antagonists like AOP-RANTES that achieve full receptor occupancy at nanomolar concentrations are strong candidates for the therapy of HIV-1–infected individuals.
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Cited by
The Biology of Chemokines and their Receptors
Rossi, D., & Zlotnik, A. (2000) · Annual Review of Immunology · doi:10.1146/annurev.immunol.18.1.217 · Cited by 2,410
Chemokine receptors as HIV-1 coreceptors: roles in viral entry, tropism, and disease
Berger, E. A., Murphy, P. M., & Farber, J. M. (1999) · Annual Review of Immunology · doi:10.1146/annurev.immunol.17.1.657 · Cited by 2,180
Lambeir, A.-M., Durinx, C., Scharpé, S., & De Meester, I. (2003) · Critical Reviews in Clinical Laboratory Sciences · doi:10.1080/713609354 · Cited by 955
Structure, Function, and Inhibition of Chemokines
Fernandez, E. J., & Lolis, E. (2002) · Annual Review of Pharmacology and Toxicology · doi:10.1146/annurev.pharmtox.42.091901.115838 · Cited by 609
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Zhang, X., Brann, T. W., Zhou, M., Yang, J., Oguariri, R. M., Lidie, K. B., Imamichi, H., Huang, D.-W., Lempicki, R. A., Baseler, M. W., et al. (2011) · The Journal of Immunology · doi:10.4049/jimmunol.1003389 · Cited by 249
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Shiraishi, M., Aramaki, Y., Seto, M., Imoto, H., Nishikawa, Y., Kanzaki, N., Okamoto, M., Sawada, H., Nishimura, O., Baba, M., et al. (2000) · Journal of Medicinal Chemistry · doi:10.1021/jm9906264 · Cited by 185
Hamdan, F. F., Audet, M., Garneau, P., Pelletier, J., & Bouvier, M. (2005) · SLAS Discovery · doi:10.1177/1087057105275344 · Cited by 183
Kenakin, T. P. (2017) · Pharmacology in Drug Discovery and Development · doi:10.1016/b978-0-12-803752-2.00001-6 · Cited by 1
Huang, M., Celniker, A. F., Chitsazi, R., Dyer, D. P., Jansma, A. L., Kufareva, I., Salanga, C. L., & Handel, T. M. (2025) · Journal of Biological Chemistry · doi:10.1016/j.jbc.2025.110736 · Cited by 1
Metadata
- Authors
- Simmons, G., Clapham, P. R., Picard, L., Offord, R. E., Rosenkilde, M. M., Schwartz, T. W., Buser, R., Wells, T. N. C., & Proudfoot, A. E. I.
- Venue
- Science
- Published
- 1997-04-11
- Volume
- 276
- Issue
- 5310
- Pages
- 276-279
- ISSN
- 0036-8075 (ISSN-L)
- 1095-9203
- OpenAlex
- W2067964854
- Cited by
- 608
- References
- 0
- FWCI
- 31.36
- Type
- journal article
- Language
- en
- Open access
- closed
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