The DOI matches its Crossref record; 32 of the 32 references it cites were found in a registry or an index.
In Vitro Antiretroviral Properties of S/GSK1349572, a Next-Generation HIV Integrase Inhibitor
Open accessAbstract
S/GSK1349572 is a next-generation HIV integrase (IN) inhibitor designed to deliver potent antiviral activity with a low-milligram once-daily dose requiring no pharmacokinetic (PK) booster. In addition, S/GSK1349572 demonstrates activity against clinically relevant IN mutant viruses and has potential for a high genetic barrier to resistance. S/GSK1349572 is a two-metal-binding HIV integrase strand transfer inhibitor whose mechanism of action was established through in vitro integrase enzyme assays, resistance passage experiments, activity against viral strains resistant to other classes of anti-HIV agents, and mechanistic cellular assays. In a variety of cellular antiviral assays, S/GSK1349572 inhibited HIV replication with low-nanomolar or subnanomolar potency and with a selectivity index of 9,400. The protein-adjusted half-maximal effective concentration (PA-EC 50) extrapolated to 100% human serum was 38 nM. When virus was passaged in the presence of S/GSK1349572, highly resistant mutants were not selected, but mutations that effected a low fold change (FC) in the EC 50(up to 4.1 fold) were identified in the vicinity of the integrase active site. S/GSK1349572 demonstrated activity against site-directed molecular clones containing the raltegravir-resistant signature mutations Y143R, Q148K, N155H, and G140S/Q148H (FCs, 1.4, 1.1, 1.2, and 2.6, respectively), while these mutants led to a high FC in the EC 50 of raltegravir (11- to >130-fold). Either additive or synergistic effects were observed when S/GSK1349572 was tested in combination with representative approved antiretroviral agents; no antagonistic effects were seen. These findings demonstrate that S/GSK1349572 would be classified as a next-generation drug in the integrase inhibitor class, with a resistance profile markedly different from that of first-generation integrase inhibitors.
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Cites
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Cited by
Tsiang, M., Jones, G. S., Goldsmith, J., Mulato, A., Hansen, D., Kan, E., Tsai, L., Bam, R. A., Stepan, G., Stray, K. M., et al. (2016) · Antimicrobial Agents and Chemotherapy · doi:10.1128/aac.01474-16 · Cited by 290
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Self-citationNew Class of HIV-1 Integrase (IN) Inhibitors with a Dual Mode of Action
Tsiang, M., Jones, G. S., Niedziela-Majka, A., Kan, E., Lansdon, E. B., Huang, W., Hung, M., Samuel, D., Novikov, N., Xu, Y., et al. (2012) · Journal of Biological Chemistry · doi:10.1074/jbc.m112.347534 · Cited by 167
“Although the introduction into the clinic of a secondgeneration INSTI represented by dolutegravir is expected in the near future (13), all INSTIs function with essentially the samemode of action, through binding to the catalytic site of IN.”
BackgroundBalakrishnan, M., Yant, S. R., Tsai, L., O’Sullivan, C., Bam, R. A., Tsai, A., Niedziela-Majka, A., Stray, K. M., Sakowicz, R., & Cihlar, T. (2013) · PLoS ONE · doi:10.1371/journal.pone.0074163 · Cited by 126
Metadata
- Authors
- Kobayashi, M., Yoshinaga, T., Seki, T., Wakasa-Morimoto, C., Brown, K. W., Ferris, R., Foster, S. A., Hazen, R. J., Miki, S., Suyama-Kagitani, A., Kawauchi-Miki, S., Taishi, T., Kawasuji, T., Johns, B. A., Underwood, M. R., Garvey, E. P., Sato, A., & Fujiwara, T.
- Venue
- Antimicrobial Agents and Chemotherapy
- Publisher
- American Society for Microbiology
- Published
- 2011-02
- Volume
- 55
- Issue
- 2
- Pages
- 813-821
- ISSN
- 0066-4804 (ISSN-L)
- 1098-6596
- OpenAlex
- W2152880150
- Cited by
- 382
- References
- 32
- FWCI
- 18.06
- Type
- journal article
- Language
- en
- Open access
- green
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- Kobayashi, M., Yoshinaga, T., Seki, T., Wakasa-Morimoto, C., Brown, K. W., Ferris, R., Foster, S. A., Hazen, R. J., Miki, S., Suyama-Kagitani, A., Kawauchi-Miki, S., Taishi, T., Kawasuji, T., Johns, B. A., Underwood, M. R., Garvey, E. P., Sato, A., & Fujiwara, T. (2011). In Vitro Antiretroviral Properties of S/GSK1349572, a Next-Generation HIV Integrase Inhibitor. Antimicrobial Agents and Chemotherapy. https://doi.org/10.1128/aac.01209-10
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