Inhibition of HIV infection by bicyclams, highly potent and specific CXCR4 antagonists

European Cytokine Network

Volumn 10, Issue 2, 1999, Pages 281-285

  De Clercq, Erik ^a  

^a REGA INSTITUTE FOR MEDICAL RESEARCH   (Belgium)

Author keywords

[No Author keywords available]

Indexed keywords

1,1' [1,4 PHENYLENE BIS(METHYLENE)] BIS 1,4,8,11 TETRA AZACYCLOTETRADECANE; 1,1' PROPYLENE BIS 1,4,8,11 TETRA AZACYCLOTETRADECANE; ANTIVIRUS AGENT; CHEMOKINE; CHEMOKINE RECEPTOR CXCR4; RANTES; UNCLASSIFIED DRUG;

ANTIGEN BINDING; ANTIVIRAL ACTIVITY; CHEMOTAXIS; CONFERENCE PAPER; CONTROLLED STUDY; DRUG MECHANISM; DRUG STRUCTURE; HUMAN; HUMAN CELL; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; NONHUMAN; SIGNAL TRANSDUCTION; STRUCTURE ACTIVITY RELATION; T LYMPHOCYTE;

EID: 0032782311     PISSN: 11485493     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Conference Paper

References (25)

1. 1. De Clercq E. 1995. Antiviral therapy for human immunodeficiency virus infections. Clin. Microbiol. Rev. 8: 200.
2. 2. De Clercq E, Yamamoto N, Pauwels R, Baba M, Schols D, Nakashima H, Balzarini J, Debyser Z, Murrer B A, Schwartz D, Thornton D, Bridger G, Fricker S, Henson G, Abrams M, Picker D. 1992. Potent and selective inhibition of human immunodeficiency virus (HIV)-1 and HIV-2 replication by a class of bicyclams interacting with a viral uncoating event. Proc. Natl. Acad. Sci. USA 89: 5286.
3. 3. De Clercq E, Yamamoto N, Pauwels R, Balzarini J, Witvrouw M, de Vreese K, Debyser Z, Rosenwirth B, Peichl P, Datema R, Thornton D, Skerlj R, Gaul F, Padmanabhan S, Bridger G, Henson G, Abrams M. 1994. Highly potent and selective inhibition of human immunodeficiency virus by the bicyclam derivative JM3100. Antimicrob. Agents Chemother. 38: 668.
4. 4. Schols D, de Clercq E. 1998. The simian immunodeficiency virus mnd(GB-1) strain uses CXCR4, not CCR5, as coreceptor for entry in human cells. J. Gen. Virol. 79: 2203.
5. 5. De Clercq E. 1992. Human immunodeficiency virus inhibitors targeted at virus-cell fusion and/or viral uncoating. Int. J. Immumother. 18: 115.
6. 6. De Vreese K, Reymen D, Griffin P, Steinkasserer A, Werner G, Bridger G J, Esté J, James W, Henson G W, Desmyter J, Anné J, de Clercq E. 1996. The bicyclams, a new class of potent human immunodeficiency virus inhibitors, block viral entry after binding. Antiviral Res. 29: 209.
7. 7. Esté J A, de Vreese K, Witvrouw M, Schmit J C, Vandamme A M, Anné J, DesmyterJ, Henson G W, Bridger G, de Clercq E. 1996. Antiviral activity of the bicyclam derivative JM3100 against drug-resistant strains of human immunodeficiency virus type I. Antiviral Res. 29: 297.
8. 8. De Vreese K, Kofler-Mongold V, Leutgeb C, Weber V, Vermeire K, Schacht S, Anné J, de Clercq E, Datema R, Werner G. 1996. The molecular target of bicyclams, potent inhibitors of human immunodeficiency virus replication. J. Virol. 70: 689.
9. 9. De Vreese K, van Nerum I, Vermeire K, Anné J, de Clercq E. 1997. Sensitivity of human immunodeficiency virus to bicyclam derivatives is influenced by the three-dimensional structure of gp120. Antimicrob. Agents Chemother. 41: 2616.
10. 10. Schols D, Struyf S, van Damme J, Esté J A, Henson G, de Clercq E. 1997. Inhibition of T-tropic HIV strains by selective antagonization of the chemokine receptor CXCR4. J. Exp. Med. 186: 1383.
11. 11. Schols D, Esté J A, Henson G, de Clercq E. 1997. Bicyclams, a class of potent anti-HIV agents, are targeted at the HIV coreceptor fusin/CXCR-4. Antiviral Res. 35: 147.
12. 12. 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, Moore J P. 1998. AMD3100, a small molecule inhibitor of HIV-1 entry via the CXCR4 co-receptor. Nature Medicine 4: 72.
13. 13. Simmons G, Reeves J D, McKnight A, Dejucq N, Hibbits S, Power C A, Aarons E, Schols D, de Clercq E, Proudfoot A E I, Clapham P R. 1998. CXCR4 as a functional coreceptor for human immunodeficiency virus type I infection of primary macrophages. J. Virol. 72: 8453.
14. 14. Schols D, de Clercq E. Differential use of the chemokine receptor CXCR4 by different T-tropic human immunodeficiency virus type I strains. J. Virol. Submitted for publication.
15. 15. Schols D, Esté J A, Cabrera C, de Clercq E. 1998. T cell-line-tropic human immunodeficiency virus type I that is made resistant to stromal cell-derived factor 1α contains mutations in the envelope gp120 but does not show a switch in coreceptor use. J. Virol. 72: 4032.
16. 16. Labrosse B, Brelot A, Heveker N, Sol N, Schols D, de Clercq E, Alizon M. 1998. Determinants for sensitivity of human immunodeficiency virus coreceptor CXCR4 to the bicyclam AMD3100. J. Virol. 72: 6381.
17. 17. Bridger G J, Skerlj R T, Thornton D, Padmanabhan S, Martellucci S A, Henson G W, Abrams M J, Yamamoto N, de Vreese K, Pauwels R, de Clercq E, 1995. Synthesis and structure-activity relationships of phenylenebis(methylene)-linked bistetraazamacrocycles that inhibit HIV replication. Effects of macrocyclic ring size and substituents on the aromatic linker. J. Med. Chem. 38: 366.
18. 18. Bridger G J, Skerlj R T, Padmanabhan S, Martellucci S A, Henson G W, Abrams M J, Joao H C, Witvrouw M, de Vreese K, Pauwels R, de Clercq E. 1996. Synthesis and structure-activily relationships of phenylenebis(methylene)-linked bis-tetraaza-macrocycles that inhibit human immunodeficiency virus replication. 2. Effect of heteroaromatic linkers on the activity of bicyclams. J. Med. Chem. 39: 109.
19. 19. Joao H C, de Vreese K, Pauwels R, de Clercq E, Henson G W, Bridger G J. 1995. Quantitative structural activity relationship study of his-tetraazacyclic compounds. A novel series of HIV-1 and HIV-2 inhibitors. J. Med. Chem. 38: 3865.
20. 20. Esté JA, Cabrera C, de Clercq E, Struyf S, van Damme J, Bridger G, Skerlj R T, Abrams M J, Henson G, Gutierrez A, Clotet B, Schols D. 1998. Activity of different bicyclam derivatives against human immunodeficiency virus depends on their interaction with the CXCR4 chemokine receptor. Mol. Pharmacol. 55: 67.
21. 21. Esté J A, Schols D, Cabrera C, Blanco J, Gutierrez A, Bridger G, Henson G, Clotet B, de Clercq E. Outgrowth of RS HIV from clinical isolates through blockade of the CXCR4 receptor by the bicyclam AMD3100. J. Virol. Submitted for publication.
22. 22. Murakami T, Nakajima T, Koyanagi Y, Tachibana K, Fujii N, Tamamura H, Yoshida N, Waki M, Matsumuto A, Yoshie O, Kishimoto T, Yamamoto N, Nagasawa T. 1997. A small molecule CXCR4 inhibitor that blocks T tell line-tropic HIV-1 infection. J. Exp. Med. 186: 1389.
23. 23. Doran B J, Grovit-Ferbas K, Sharron M P, Mao S H, Goetz M B, Daar E S, Doms R W, O'Brien W A. 1997. A small-molecule inhibitor directed against the chemokine receptor CXCR4 prevents its use as an HIV-1 coreceptor. J. Exp. Med. 186: 1395.
24. 24. Daclemans D, Schols D, Witvrouw M, Pannecouque C, Van Dooren S, Hamy F, Klimkait T, de Clercq E, Vandamme A M. A second target for the peptoid Tat/TAR-inhibitor CGP64222: inhibition of HIV replication by blocking CXCR4-mediated virus entry. Mol. Pharmacol. Submitted for publication.
25. 25. Datema R, Rabin L, Hincenbergs M, Moreno M B, Warren S, Linguist V, Rosenwirth B, Seifert J, McCune J M. 1996. Antiviral efficacy in vivo of the anti-human immunodeficiency virus bicyclam SDZ SID 791 (JM 3100), an inhibitor of infectious cell entry. Antimicrob. Agents Chemother. 40: 750.