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Title: A second target for the peptoid Tat/transactivation response element inhibitor CGP64222: inhibition of human immunodeficiency virus replication by blocking CXC-chemokine receptor 4-mediated virus entry
Authors: Daelemans, Dirk ×
Schols, Dominique
Witvrouw, Myriam
Pannecouque, Christophe
Hatse, Sigrid
Van Dooren, Sonia
Hamy, F
Klimkait, T
De Clercq, Erik
Vandamme, Anne-Mieke #
Issue Date: Jan-2000
Series Title: Molecular Pharmacology vol:57 issue:1 pages:116-124
Abstract: The peptoid CGP64222 has been previously demonstrated to inhibit the human immunodeficiency virus (HIV) Tat/transactivation response element complex formation. It has previously been shown that CGP64222 selectively inhibits HIV-1 long terminal repeat-driven gene expression and HIV-1(LAV) replication in lymphocytes. Here, we show that CGP64222 inhibits the replication of a wide range of laboratory strains of HIV-1 and HIV-2 in MT-4 cells. However, CGP64222 proved inactive in MT-4 cells against HIV-1 strains that are resistant to the bicyclams. The bicyclams are known to specifically interact with CXC-chemokine receptor 4, the main coreceptor used by T-tropic HIV strains to enter the cells. Mechanism of action studies revealed that CGP64222 can inhibit the HIV replicative cycle, also through a selective interaction with the CXC-chemokine receptor 4 coreceptor.
URI: 
ISSN: 0026-895X
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
Laboratory of Clinical and Epidemiological Virology (Rega Institute)
Molecular Virology and Gene Therapy
Laboratory of Experimental Oncology
× corresponding author
# (joint) last author

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