A small-molecule, nonpeptide CCR5 antagonist with highly potent and selective anti-HIV-1 activity

Proceedings of the National Academy of Sciences of the United States of America

Volumn 96, Issue 10, 1999, Pages 5698-5703

  Baba, Masanori ^a,b   Nishimura, Osamu ^a,b   Kanzaki, Naoyuki ^b   Okamoto, Mika ^a   Sawada, Hidekazu ^b   Iizawa, Yuji ^b   Shiraishi, Mitsuru ^b   Aramaki, Yoshio ^b   Okonogi, Kenji ^b   Ogawa, Yasuaki ^b   Meguro, Kanji ^b   Fujino, Masahiko ^b  

^a KAGOSHIMA UNIVERSITY   (Japan)

^b TAKEDA PHARMACEUTICAL COMPANY LIMITED   (Japan)

Author keywords

[No Author keywords available]

Indexed keywords

ANTIVIRUS AGENT; CHEMOKINE RECEPTOR CCR5; CHEMOKINE RECEPTOR CCR5 ANTAGONIST; CHEMOKINE RECEPTOR CXCR4; N [4 [[[6,7 DIHYDRO 2 (4 METHYLPHENYL) 5H BENZOCYCLOHEPTEN 8 YL]CARBONYL]AMINO]BENZYL] N,N DIMETHYL 2H TETRAHYDROPYRAN 4 AMINIUM CHLORIDE; N,N DIMETHYL N [ [[[2 (4 METHYLPHENYL) 6,7 DIHYDRO 5H BENZOCYCLOHEPTEN 8 YL]CARBONYL]AMINO]BENZYL]TETRAHYDRO 2H PYRAN 4 AMINIUM CHLORIDE; RANTES; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; CHO CELL; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG POTENCY; DRUG SELECTIVITY; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS 1; NONHUMAN; PRIORITY JOURNAL; VIRUS INHIBITION; VIRUS REPLICATION;

AMIDES; ANIMALS; ANTI-HIV AGENTS; BINDING, COMPETITIVE; CHO CELLS; CRICETINAE; HIV-1; HUMANS; JURKAT CELLS; LEUKOCYTES, MONONUCLEAR; MOLECULAR STRUCTURE; PROTEIN BINDING; QUATERNARY AMMONIUM COMPOUNDS; RANTES; RECEPTORS, CCR5; TRANSFECTION; VIRUS REPLICATION;

ANIMALIA; CRICETINAE; CRICETULUS GRISEUS; HUMAN IMMUNODEFICIENCY VIRUS; HUMAN IMMUNODEFICIENCY VIRUS 1;

EID: 13044256383     PISSN: 00278424     EISSN: None     Source Type: Journal    
DOI: 10.1073/pnas.96.10.5698     Document Type: Article

References (35)

1. Havlir, D. V. & Richman, D. D. (1996) Ann. Intern. Med. 124, 984-994.
2. Carpenter, C. C. J., Fischl, M. A., Hammer, S. M., Hirsch, M. S. Jacobsen, D. M., Katzenstein, D. A., Montaner, J. S. G., Richman, D. D., Saag, M. S., Schooley, R. T., et al. (1998) J. Am. Med. Assoc. 280, 78-86.
3. Deeks, S. G., Smith, M., Holodniy, M. & Kahn, J. O. (1997) J. Am. Med. Assoc. 277, 145-153.
4. Deng, H., Liu, R., Ellmeier, W., Choe, S., Unutmaz, D., Burkhart, M., Di Marzio, P., Marmon, S., Sutton, R. E., Hill, C. M., et al. (1996) Nature (London) 381, 661-666.
5. Dragic, T., Litwin, V., Allaway, G. P., Martin, S. R., Huang, Y., Nagashima, K. A., Cayanan, C., Maddon, P. J., Koup, R. A., Moore, J. P., et al. (1996) Nature (London) 381, 667-673.
6. Alkhatib, G., Combadiere, C., Broder, C. C., Feng, Y., Kennedy, P. E., Murphy, P. M. & Berger, E. A. (1996) Science 272, 1955-1958.
7. Choe, H., Farzan, M., Sun, Y., Sullivan, N., Rollins, B., Ponath, P. D., Wu, L., Mackay, C. R., LaRosa, G., Newman, W., et al. (1996) Cell 85, 1135-1148.
8. Doranz, B. J., Rucker, J., Yi, Y., Smyth, R. J., Samson, M., Peiper, S. C., Parmentier, M., Collman, R. G. & Doms, R. W. (1996) Cell 85, 1149-1158.
9. Schuitemaker, H., Koot, M., Kootstra, N. A., Dercksen, M. W., de Goede, R. E., van Steenwijk, R. P., Lange, J. M., Schattenkerk, J. K., Miedema, F. & Tersmette, M. (1992) J. Virol. 66, 1354-1360.
10. Richman, D. D. & Bozzette, S. A. (1994) J. Infect. Dis. 169, 968-974.
11. Conner, R. I., Sheridan, K. E., Caradini, D., Choe, S. & Landau, N. L. (1997) J. Exp. Med. 185, 621-628.
12. Liu, R., Paxton, W. A., Choe, S., Ceradini, D., Martin, S. R., Horuk, R., MacDonald, M. E., Stuhlmann, H., Koup, R. A. & Landau, N. R. (1996) Cell 86, 367-377.
13. Samson, M., Libert, F., Doranz, B. J., Rucker, J., Liesnard, C., Farber, C.-M., Saragosti, S., Lapouméroulie, C., Cognaux, J., Forceille, C., et al. (1996) Nature (London) 382, 722-725.
14. Bjorndal, A., Deng, H., Jansson, M., Fiore, J. R., Colognesi, C., Karlsson, A., Albert, J., Scarlatti, G., Littman, D. R. & Fenyo, E. M. (1997) J. Virol. 71, 7478-7487.
15. Scarlatti, G., Tresoldi, E., Bjorndal, A., Fredriksson, R., Colognesi, C., Deng, H. K., Malnati, M. S., Plebani, A., Siccardi, A. G., Littman, D. R., et al. (1997) Nat. Med. 3, 1259-1265.
16. Cocchi, F., DeVico, A. L., Garzino-Demo, A., Arya, S. K., Gallo, R. C. & Lusso, P. (1995) Science 270, 1811-1815.
17. Proudfoot, A. E. I., Power, C. A., Hoogewerf, A. J., Montjovent, M. O., Borlat, F., Offord, R. E. & Wells, T. N. C. (1996) J. Biol. Chem. 271, 2599-2603.
18. Simmons, G., Clapham, P. R., Picard, L., Offord, R. E., Rosenkilde, M. M., Schwartz, T. W., Buser, R., Wells, T. N. C. & Proudfoot, A. E. I. (1997) Science 276, 276-279.
19. Schols, D., Struyf, S., Van Damme, J., Esté, J. A., Henson, G. & De Clercq, E. (1997) J. Exp. Med. 186, 1383-1388.
20. Donzella, G. A., Schols, D., Lin, S. W., Esté, J. A., Nagashima, K. A. Maddon, P. J., Allaway, G. P., Sakmar, T. P., Henson, G., De Clercq, E. et al. (1998) Nat. Med. 4, 72-77.
21. Chackerian, B., Long, E. M., Luciw, P. A. & Overbaugh, J. (1997) J. Virol. 71, 3932-3939.
22. Miyoshi, I., Taguchi, H., Kubonishi, I., Yoshimoto, S., Ohtsuki, Y., Shiraishi, Y. & Akagi, T. (1982) Gann Monogr. 28, 219-228.
23. Samson, M., Labbe, O., Mollereau, C., Vassart, G. & Parmentier, M. (1996) Biochemistry 35, 3362-3367.
24. Raport, C. J., Gosling J., Schweickart, V. L., Gray, P. W. & Charo, I. F. (1996) J. Biol. Chem. 271, 17161-17166.
25. Kimpton, J. & Emerman, M. (1992) J. Virol. 66, 2232-2239 (1992).
26. Baba, M., De Clercq, E., Tanaka, H., Ubasawa, M., Takashima, H., Sekiya, K., Nitta, I., Umezu, K., Nakashima, H., Mori, S., et al. (1991) Proc. Natl. Acad. Sci. USA 88, 2356-2360.
27. Pauwels, R., Balzarini, J., Baba, M., Snoeck, R., Schols, D., Herdewijn, P., Desmyter, J. & De Clercq, E. (1988) J. Virol. Methods 20, 309-321.
28. Hesselgesser, J., Liang, M., Hoxie, J., Greenberg, M., Brass, L. F., Orsini, M. J., Taub, D. & Horuk, R. (1998) J. Immunol. 160, 877-883.
29. Luster, A. D. (1998) N. Engl. J. Med. 338, 436-445.
30. He, J., Chen, Y., Farzan, M., Choe, H., Ohagen, A., Gartner, S., Busciglio, J., Yang, X., Hofman, W., Newman, W., et al. (1997) Nature (London) 385, 645-649.
31. Ghorpade, A., Xia, M. Q., Hyman, B. T., Persidsky, Y., Nukuna, A., Bock, P., Che, M., Limoges, J., Gendelman, H. E. & Mackay, C. R. (1998) J. Virol. 72, 3351-3361.
32. Mack, M., Luckow, B., Nelson, P. J., Cihak, J., Simmons, G., Clapham, P. R., Signoret, N., Marsh, M., Stangassinger, M., Borlat, F., et al. (1998) J. Exp. Med. 187, 1215-1224.
33. Wu, L., LaRosa, G., Kassam, N., Gordon, C. J., Heath, H., Ruffing, N., Chen, H., Humblias, J., Samson, M., Parmentier, M., et al. (1997) J. Exp. Med. 186, 1373-1381.
34. Schols, D., Esté, J. A., Cabrera, C. & De Clercq, E. (1998) J. Virol. 72, 4032-4037.
35. Cheng, Y.-C. & Prusoff, H. R. (1973) Biochem. Pharmacol. 22, 3099-3108.