2-Glycineamide-5-chlorophenyl 2-pyrryl ketone, a non-benzodiazepin Tat antagonist, is effective against acute and chronic HIV-1 infections in vitro

Antiviral Research

Volumn 32, Issue 2, 1996, Pages 55-62

  Kira, Toshihiko ^a   Hashimoto, Koh Ichi ^a   Baba, Masanori ^b   Okamoto, Takashi ^c   Shigeta, Shiro ^a  

^a FUKUSHIMA MEDICAL UNIVERSITY   (Japan)

^b KAGOSHIMA UNIVERSITY   (Japan)

^c NAGOYA CITY UNIV MEDICAL SCHOOL   (Japan)

Author keywords

Anti HIV; Anti Tat; Chronic infection; GCPK; Ro24 7429; Ro5 3335

Indexed keywords

7 CHLORO 1,3 DIHYDRO 5 (2 PYRROLYL) 2H 1,4 BENZODIAZEPIN 2 ONE; ANTIVIRUS AGENT; PHOSPHOTRANSFERASE; TUMOR NECROSIS FACTOR ALPHA; [7 CHLORO 5 (1H PYRROL 2 YL) 3H BENZO[E][1,4]DIAZEPIN 2 YL]METHYLAMINE;

ANTIVIRAL ACTIVITY; ARTICLE; CONTROLLED STUDY; DOSE RESPONSE; DRUG EFFICACY; HUMAN; HUMAN CELL; HUMAN IMMUNODEFICIENCY VIRUS 1; IN VITRO STUDY; PRIORITY JOURNAL; STRUCTURE ACTIVITY RELATION; VIRUS INFECTION; VIRUS REPLICATION;

ALPHAVIRUS; HUMAN IMMUNODEFICIENCY VIRUS; HUMAN IMMUNODEFICIENCY VIRUS 1;

EID: 0030270635     PISSN: 01663542     EISSN: None     Source Type: Journal    
DOI: 10.1016/0166-3542(95)00980-9     Document Type: Article

References (30)

1. Antoni, B.A., Stein, S.B. and Rabson, A.B. (1994) Regulation of human immuno-deficiency virus infection: implications for pathogenesis. Adv. Virus Res. 43, 53-145.
2. Arya, S.K., Guo, C., Josephs, S.F. and Wong-Staal, F. (1985) Trans-activator gene of human T-lymphotropic virus type III (HTLV-III). Science 229, 69-73.
3. Bawen, E.F., Atkins, M., Weller, I.V.D. and Johnson, M.A. (1995) In: D.J. Jeffries and E. De Clercq (Eds), Antiviral Chemotherapy, pp. 65-79. John Wiley & Sons, Chichester.
4. Berkhout, B.B., Gatignol, A., Rabson, A.B. and Jeang, K. (1990) TAR-independent activation of HIV-1 LTR: evidence that Tat requires specific regions of the promoter. Cell 62, 757-767.
5. Biswas, D.K., Ahlers, C.M., Dezube, B.J. and Pardee, A.B. (1993) Cooperative inhibition of NF-κB and Tat-induced superactivation human immunodeficiency virus type 1 long terminal repeat. Proc. Natl. Acad. Sci. USA 90, 11044-11048.
6. Braddock, M., Cannon, P., Muckenthaler, M., Kingsman, A.J. and Kingsman, S.M. (1994) Inhibition of human immunodeficiency virus type 1 Tat-dependent activation of translation in Xenopus oocytes by the benzodiazepine Ro24-7429 requires trans-activation response element loop sequence. J. Virol. 68, 25-33.
7. + cell model of chronic infection. J. Virol. 65, 4645-4653.
8. Chandra, A., Demirhan, I., Arya, S.K. and Chandra, P. (1988) D-Penicillamine inhibits trans activation of human immunodeficiency virus type-1 (HIV-1) LTR by transactivator protein. FEBS Lett. 29, 282-286.
9. Condra, J.H., Schleif, W.A., Blahy, O.M., Gabryelski, L.J., Graham, D.J., Quintero, J., Rhodes, A., Robbins, H.L., Roth, E., Shivaprakash, M., Titus, D., Yang, T., Teppler, H., Squires, K.E., Deutsch, P.J. and Emini, E.A. (1995) In vivo emergence of HIV-1 variants resistant to multiple protease inhibitors. Nature 374, 569-571.
10. Feinberg, M.B., Baltimore, D. and Frankel, A.D. (1991) The role of Tat in the human immunodeficiency virus life cycle indicates a primary effect on transcriptional elongation. Proc. Natl. Acad. Sci. USA 88, 4045-4049.
11. Feorino, P.M., Butera, S.T., Folks, T.M. and Schinazi, R.F. (1993) Prevention of activation of HIV-1 by antiviral agents in OM-10.1 cells. Antiviral Chem. Chemother. 4, 55-63.
12. Geleziunas, R., Bour, S., Boulerice, F., Hiscott, J. and Wainberg, M.A. (1991) Diminution of CD4 surface protein but not CD4 messenger RNA level in monocytic cells infected by HIV-1. AIDS 5, 29-33.
13. Hoxie, J. A., Haggarty, B.S. and Rackowski, J. (1985) Persistent noncytopathic infection of normal human T lymphocyte with AIDS-associated retro viruses. Science 229, 1400-1402.
14. Hoxie, J.A., Alpers, J.D., Rackowski, J.L., Huebner, K., Haggarty, B.S., Cedarbaum, A.J. and Reed, J.C. (1986) Alteration in T4 (CD4) protein and mRNA synthesis in cells infected with HIV. Science 234, 1123-1127.
15. Hsu, M., Schutt, A.D., Holly, M., Slice, L.W., Shertnan, M.I., Richman, D.D., Potash, M.J. and Volsky, D.J. (1991) Inhibition of HIV replication in acute and chronic infections in vitro by a Tat antagonist. Science 254, 1799-1802.
16. Hsu, M., Dhingra, U., Earley, J.V., Holly, M., Keith, D., Nalin, C.M., Richou, A.R., Schutt, A.D., Tam, S.Y., Potash, M.J., Volsky, D.J. and Richman, D.D. (1993) Inhibition of type 1 human immunodeficiency virus replication by a Tat antagonist to which the virus remains sensitive after prolonged exposure in vitro. Proc. Natl. Acad. Sci. USA 90, 6395-6399.
17. Kira, T., Merin. J.P., Shigeta, S., Baba, M. and Okamoto, T. (1995) Anti-Tat MTT assay: a novel anti-HIV drug screening system using the viral regulatory network of replication. AIDS Res. Hum. Retrovir. 11, 1359-1366.
18. Laspia, M.F., Rice, A.P. and Mathews, M.B. (1989) HIV-1 Tat protein increases transcriptional initiation and stabilizes elongation. Cell 59, 283-292.
19. Li, C.J., Wang, C. and Pardee, A.B. (1994) Camptothecin inhibits Tat-mediated transactivation of type 1 human immunodeficiency virus. J. Biol. Chem. 269, 7051-7054.
20. Luznik, L., Kraus, G., Guatelli, J., Richman, D.D. and Wong-Staal, F. (1995) Tat-independent replication of human immunodeficiency viruses. J. Clin. Invest. 95, 328-332.
21. Marciniak, R. and Sharp, P. (1991) HIV-1 Tat protein promotes formation of more-processive elongation complexes. EMBO J. 10, 4189-4196.
22. Okamoto, T. and Wong-Staal, F. (1986) Demonstration of virus-specific transcriptional activator(s) in cells infected with HTLV-III by an in vitro cell-free system. Cell 47, 29-35.
23. Pauwels, R., Balzarini, J., Baba, M., Snoeck, R., Schols, D., Herdewijn, P., Desmyter, J. and De Clercq, E. (1988) Rapid and automated tetrazolium-based colorimetric assay for the detection of anti-HIV compounds. J. Virol. Methods 20, 309-321.
24. Popik, W. and Pitha, P. (1993) Role of tumor necrosis factor alpha in activation and replication of the tat-defective human immunodeficiency virus type 1. J. Virol. 67, 1094-1099.
25. Popik, W. and Pitha, P. (1994) Differential effect of tumor necrosis factor-α and herpes simplex virus type 1 on the Tat-targeted inhibition of human immunodeficiency virus type 1 replication. Virology 202, 521-529.
26. Rosen, C.A., Sodroski, J.G. and Haseltine, W.A. (1985) The location of cis-acting regulatory sequences in the human T cell lymphotropic virus type III (HTLV-III/LAV) long terminal repeat. Cell 41, 813-823.
27. Shahabuddin, M., Volsky, B., Hsu, M. and Volsky, D.J. (1992) Restoration of cell surface CD4 expression in human immunodeficiency virus type 1-infected cells by treatment with a Tat antagonist. J. Virol. 66, 6802-6805.
28. Sharp, P.A. and Marciniak, R.A. (1989) HIV TAR: an RNA enhancer? Cell 59, 229-230.
29. Sodroski, J., Patarca, R. and Rosen, C. (1985) Location of the trans-activating region on the genome of human T-cell lymphotropic virus type III. Science 229, 74-77.
30. Witvrouw, M., Pauwels, R., Vandamme, A., Schols, D., Reymen, D., Yamamoto, N., Desmyter, J. and De Clercq, E. (1992) Cell type-specific human immuno-deficiency virus type 1 activity of the transactivation inhibitor Ro5-3335. Antimicrob. Agents Chemother. 36, 2628-2633.