A mutation in human immunodeficiency virus type 1 protease at position 88, located outside the active site, confers resistance to the hydroxyethylurea inhibitor SC-55389A

Antimicrobial Agents and Chemotherapy

Volumn 41, Issue 3, 1997, Pages 515-522

  Smidt, Mary L ^a,b   Potts, Karen E ^a,c   Tucker, Simon P ^a,d   Blystone, Lisa ^a   Stiebel Jr , Thomas R ^a   Stallings, William C ^a   McDonald, Joseph J ^a   Pillay, Deenan ^e,f   Richman, Douglas D ^e   Bryant, Martin L ^a,g  

^a PFIZER INC   (United States)

^b Mail Zone AA5C ^*  (United States)

^c AGOURON PHARMACEUTICALS INC   (United States)

^d UNIVERSITY OF GLASGOW   (United Kingdom)

^e UNIVERSITY OF CALIFORNIA   (United States)

^f BIRMINGHAM HEARTLANDS HOSPITAL   (United Kingdom)

^g MEDIMMUNE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ANTIVIRUS AGENT; DROXINAVIR; HYDROXYETHYLUREA INHIBITOR; MUTANT PROTEIN; PROTEINASE; SAQUINAVIR; TELINAVIR; UNCLASSIFIED DRUG; ZIDOVUDINE;

ANTIBIOTIC RESISTANCE; ARTICLE; ENZYME ACTIVE SITE; ENZYME STRUCTURE; GENE MUTATION; HUMAN; HUMAN CELL; HUMAN IMMUNODEFICIENCY VIRUS 1; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; PRIORITY JOURNAL; PROTEINASE INHIBITION; STRAIN DIFFERENCE;

EID: 0031035963     PISSN: 00664804     EISSN: None     Source Type: Journal    
DOI: 10.1128/aac.41.3.515     Document Type: Article

References (27)

1. Aldenderfer, M. S., and R. K. Blashfield. 1984. Cluster analysis. Sage Publications, Beverly Hills, Calif.
2. Bryant, M. L., D. P. Getman, M. Smidt, J. J. Marr, M. Clare, R. Dillard, D. Lansky, G. DeCrescenzo, R. Heintz, K. Houseman, K. Reed, J. Stolzenbach, J. Talley, M. Vazquez, and R. Mueller. 1995. SC-52151, a novel inhibitor of the HIV protease. Antimicrob. Agents Chemother. 39:2229-2234.
3. Chen, Z., Y. Li, H. B. Schock, D. Hall, E. Chen, and L. C. Kuo. 1995. Three-dimensional structure of a mutant HIV-1 protease displaying cross-resistance to all protease inhibitors in clinical trials. J. Biol. Chem. 270: 21433-21436.
4. Coffin, J. M. 1995. HIV population dynamics in vivo: implications for genetic variation, pathogenesis, and therapy. Science 267:483-489.
5. Condra, J. 1995. Personal communication.
6. Condra, J. H., W. A. Schleif, O. M. Blahy, L. J. Gabryelski, D. J. Graham, J. C. Quintero, A. Rhodes, H. L. Robbins, E. Roth, M. Shivaprakash, D. L. Titus, T. Yang, H. Teppler, K. E. Squires, P. J. Deutsch, and E. A. Emini. 1995. In vivo selection by monotherapy of HIV-1 variants resistant to multiple protease inhibitors, abstr. 23. In Program and abstracts of the Eighth International Conference on Antiviral Research. Antivir. Res. 26:A238.
7. Condra, J. H., W. A. Schlief, O. M. Blahy, L. J. Gabryelski, D. J. Graham, J. C. Quintero, A. Rhodes, H. L. Robbins, E. Roth, M. Shivaprakash, D. Titus, T. Yang, H. Teppler, K. E. Squires, P. J. Deutsch, and E. A. Emini. 1995. In vivo emergence of HIV-1 variants resistant to multiple protease inhibitors. Nature 374:569-571.
8. DeLean, A., P. J. Munson, and D. Rodbard. 1978. Simultaneous analysis of families of sigmoidal curves: application to bioassay, radioligand assay, and physiological dose-response curves. Am. J. Physiol. 235:E97-E102.
9. Erickson, J. W. 1995. The not-so-great-escape. Nature Structural Biol. 2: 523-529.
10. Getman, D. P., D. Bertenshaw, G. DeCrescenzo, E. Doherty, J. Freskos, R. Heintz, J. Julien, K. Reed, J. Rogier, J. Talley, M. Vazquez, M. Bryant, K. Houseman, G. Kocan, N. Kishore, R. Mueller, K. Potts, S. P. Tucker, M. L. Smidt, M. Clare, H. Sheng-Shieh, W. Stallings, and R. Stegeman. 1995. HIV protease inhibitors. In Abstracts of the Gordon Research Conference: Chemotherapy of AIDS.
11. Getman, D. P., G. A. DeCrescenzo, R. M. Heintz, K. L. Reed, J. J. Talley, M. L. Bryant, M. Clare, K. A. Houseman, J. J. Marr, R. A. Mueller, M. L. Vazquez, H.-S. Shieh, W. C. Stallings, and R. A. Stegeman. 1993. Discovery of a novel class of potent HIV-1 protease inhibitors containing the (R)-(hydroxyethyl)urea isostere. J. Med. Chem. 36:288-291.
12. Guenet, C., R. A. Leppik, J. T. Pelton, K. Moelling, W. Lovenberg, and B. A. Harris. 1989. HIV-1 protease: mutagenesis of asparagine 88 indicates a domain required for dimer formation. Eur. J. Pharm. 172:443-451.
13. Holland, J., K. Spindler, F. Horodyski, E. Grabau, S. Nichol, and S. Vander-Pol. 1982. Rapid evolution of RNA genomes. Science 215:1577-1585.
14. Jacobsen, H., K. Yasargil, D. L. Winslow, J. D. Craig, A. Krohn, I. B. Duncan, and J. Mous. 1995. Characterization of human immunodeficiency virus type 1 mutants with decreased sensitivity to proteinase inhibitor Ro 31-8959. Virology 206:527-534.
15. Kozel, M. J., N. Shah, N. Shen, R. Yang, R. Fucini, T. C. Merigan, D. D. Richman, D. Morris, E. Hubbell, M. S. Chee, and T. R. Gingeras. 1996. Extensive polymorphisms observed in HIV-1 clade B protease gene using high density oligonucleotide arrays: implication for therapy. Nature Medicine 2:753-759.
16. Louis, J. M., C. A. D. Smith, E. M. Wondrak, P. T. Mora, and S. Oroszlan. 1989. Substitution mutations of the highly conserved arginine 87 of HIV-1 protease result in loss of proteolytic activity. Biochem. Biophys. Res. Commun. 164:30-38.
17. Markowitz, M., H. Mo, D. J. Kempf, D. W. Norbeck, T. N. Bhat, J. W. Erickson, and D. D. Ho. 1995. Selection and analysis of human immunodeficiency virus type 1 variants with increased resistance to ABT-538, a novel protease inhibitor. J. Virol. 69:701-700.
18. Mellors, J., B. Larder, and R. Schinazi. 1994. Mutations in HIV-1 reverse transeriptase and protease associated with drug resistance. Int. Antiviral News 2:1-5.
19. Patick, A. K., M. Duran, Y. Cao, T. Ho, Z. Pei, M. R. Keller, J. Peterkin, S. Chapman, B. Anderson, D. Ho, and M. Markowitz. 1996. Genotypic and phenotypic characterization of HIV-1 variants isolated from in vitro selection studies and from patients treated with the protease inhibitor, nelfinavir, p. 29. In Abstracts of the 5th International Workshop on HIV Drug Resistance.
20. Potts, B. J. 1990. "Mini" reverse transcriptase (RT) assay. In A. Aldovini and D. Walker (ed.), Techniques in HIV research. Stockton Press, New York, N.Y.
21. Potts, K., M. L. Smidt, S. P. Tucker, T. R. Stiebel, Jr., W. Stallings, J. J. McDonald, and M. L. Bryant. In vitro sequential selection of human immunodeficiency virus type 1 variants with reduced sensitivity to hydroxyethylurea protease inhibitors. Submitted for publication.
22. Powell, D. J., B. M. Dunn, and J. Kay. 1995. The proteinases of equine infectious anaemia virus and feline immunodeficiency virus: mimics of drug-resistant forms of HIV-1 proteinase?, abstr. 67. In Abstracts of the Fourth International Workshop on HIV Drug Resistance.
23. Richman, D. D., V. A. Johnson, D. L. Mayers, T. Shirasaka, M. C. O'Brien, and H. Mitsuya. 1993. In vitro evaluation of experimental agents for anti-HIV activity, p. 1-21. In J. E. Coligan, A. M. Kruisbeck, D. H. Margulies, E. M. Shevach, and W. Strober (ed.), Current protocols in immunology, vol. 12.9. John Wiley & Sons, Inc., Brooklyn, N.Y.
24. Sebaugh, J. L., and G. A. Milliken. 1980. Threshold point models: a SAS macro for estimation of parameters, p. 248-253. In SAS Users Group International: Proceedings of the Fifth Annual Conference. SAS Institute, Cary, N.C.
25. Tisdale, M., R. E. Myers, B. Maschera, N. R. Parry, N. M. Oliver, and E. D. Blair. 1995. Cross-resistance analysis of human immunodeficiency virus type 1 variants individually selected for resistance to five different protease inhibitors. Antimicrob. Agents Chemother. 39:1704-1710.
26. Weber, I. T. 1989. Structural alignment of retroviral protease sequences. Gene 85:565-566.
27. Wondrak, E. M., J. M. Louis, P. T. Mora, and S. Oroszlan. 1991. Purification of HIV-1 wild-type protease and characterization of proteolytically inactive HIV-1 protease mutants by pepstatin A affinity chromatography. FEBS Lett. 280:347-350.