The DOI matches its Crossref record.
Viracept (Nelfinavir Mesylate, AG1343): A Potent, Orally Bioavailable Inhibitor of HIV-1 Protease
Open accessAbstract
Using a combination of iterative structure-based design and an analysis of oral pharmacokinetics and antiviral activity, AG1343 (Viracept, nelfinavir mesylate), a nonpeptidic inhibitor of HIV-1 protease, was identified. AG1343 is a potent enzyme inhibitor (Ki = 2 nM) and antiviral agent (HIV-1 ED50 = 14 nM). An X-ray cocrystal structure of the enzyme-AG1343 complex reveals how the novel thiophenyl ether and phenol-amide substituents of the inhibitor interact with the S1 and S2 subsites of HIV-1 protease, respectively. In vivo studies indicate that AG1343 is well absorbed orally in a variety of species and possesses favorable pharmacokinetic properties in humans. AG1343 (Viracept) has recently been approved for marketing for the treatment of AIDS.
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Citations
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Smith, A. J. T., Zhang, X., Leach, A. G., & Houk, K. N. (2009) · Journal of Medicinal Chemistry · doi:10.1021/jm800498e · Cited by 193
Bardsley-Elliot (2000) · doi:10.2165/00003495-200059030-00014 · Cited by 127
Metadata
- Authors
- Kaldor, S. W., Kalish, V. J., Davies, J. F., Shetty, B. V., Fritz, J. E., Appelt, K., Burgess, J. A., Campanale, K. M., Chirgadze, N. Y., Clawson, D. K., Dressman, B. A., Hatch, S. D., Khalil, D. A., Kosa, M. B., Lubbehusen, P. P., Muesing, M. A., Patick, A. K., Reich, S. H., Su, K. S., & Tatlock, J. H.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 1997-11-01
- Volume
- 40
- Issue
- 24
- Pages
- 3979-3985
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W2027095884
- Cited by
- 618
- References
- 0
- FWCI
- 8.88
- Type
- journal article
- Language
- en
- Open access
- green
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