The DOI matches its Crossref record; 2 of the 2 references it cites were found in a registry or an index.
Discovery of Raltegravir, a Potent, Selective Orally Bioavailable HIV-Integrase Inhibitor for the Treatment of HIV-AIDS Infection
Open accessAbstract
Human immunodeficiency virus type-1 (HIV-1) integrase is one of the three virally encoded enzymes required for replication and therefore a rational target for chemotherapeutic intervention in the treatment of HIV-1 infection. We report here the discovery of Raltegravir, the first HIV-integrase inhibitor approved by FDA for the treatment of HIV infection. It derives from the evolution of 5,6-dihydroxypyrimidine-4-carboxamides and N-methyl-4-hydroxypyrimidinone-carboxamides, which exhibited potent inhibition of the HIV-integrase catalyzed strand transfer process. Structural modifications on these molecules were made in order to maximize potency as HIV-integrase inhibitors against the wild type virus, a selection of mutants, and optimize the selectivity, pharmacokinetic, and metabolic profiles in preclinical species. The good profile of Raltegravir has enabled its progression toward the end of phase III clinical trials for the treatment of HIV-1 infection and culminated with the FDA approval as the first HIV-integrase inhibitor for the treatment of HIV-1 infection.
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Cites
Inhibitors of Strand Transfer That Prevent Integration and Inhibit HIV-1 Replication in Cells
Hazuda, D. J., Felock, P., Witmer, M., Wolfe, A., Stillmock, K., Grobler, J. A., Espeseth, A., Gabryelski, L., Schleif, W., Blau, C., et al. (2000) · Science · doi:10.1126/science.287.5453.646 · Cited by 1,131
Self-citationGrobler, J. A., Stillmock, K., Hu, B., Witmer, M., Felock, P., Espeseth, A. S., Wolfe, A., Egbertson, M., Bourgeois, M., Melamed, J., et al. (2002) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.092056199 · Cited by 399
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Cited by
How were new medicines discovered?
Swinney, D. C., & Anthony, J. (2011) · Nature Reviews Drug Discovery · doi:10.1038/nrd3480 · Cited by 1,812
Retroviral intasome assembly and inhibition of DNA strand transfer
Hare, S., Gupta, S. S., Valkov, E., Engelman, A., & Cherepanov, P. (2010) · Nature · doi:10.1038/nature08784 · Cited by 678
Christ, F., Voet, A., Marchand, A., Nicolet, S., Desimmie, B. A., Marchand, D., Bardiot, D., Van der Veken, N. J., Van Remoortel, B., Strelkov, S. V., et al. (2010) · Nature Chemical Biology · doi:10.1038/nchembio.370 · Cited by 479
Protein Binding Pocket Dynamics
Stank, A., Kokh, D. B., Fuller, J. C., & Wade, R. C. (2016) · Accounts of Chemical Research · doi:10.1021/acs.accounts.5b00516 · Cited by 445
Molecular mechanisms of retroviral integrase inhibition and the evolution of viral resistance
Hare, S., Vos, A. M., Clayton, R. F., Thuring, J. W., Cummings, M. D., & Cherepanov, P. (2010) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1010246107 · Cited by 305
Metadata
- Authors
- Summa, V., Petrocchi, A., Bonelli, F., Crescenzi, B., Donghi, M., Ferrara, M., Fiore, F., Gardelli, C., Gonzalez Paz, O., Hazuda, D. J., Jones, P., Kinzel, O., Laufer, R., Monteagudo, E., Muraglia, E., Nizi, E., Orvieto, F., Pace, P., Pescatore, G., Scarpelli, R., Stillmock, K., Witmer, M. V., & Rowley, M.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2008-09-03
- Volume
- 51
- Issue
- 18
- Pages
- 5843-5855
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W2068095506
- Cited by
- 633
- References
- 2
- FWCI
- 28.88
- Type
- journal article
- Language
- en
- Open access
- green
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- Summa, V., Petrocchi, A., Bonelli, F., Crescenzi, B., Donghi, M., Ferrara, M., Fiore, F., Gardelli, C., Gonzalez Paz, O., Hazuda, D. J., Jones, P., Kinzel, O., Laufer, R., Monteagudo, E., Muraglia, E., Nizi, E., Orvieto, F., Pace, P., Pescatore, G., . . . Rowley, M. (2008). Discovery of Raltegravir, a Potent, Selective Orally Bioavailable HIV-Integrase Inhibitor for the Treatment of HIV-AIDS Infection. Journal of Medicinal Chemistry. https://doi.org/10.1021/jm800245z
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Bibliographic data: Semantic Scholar, OpenAlex, Crossref.
Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
