PT  - JOURNAL ARTICLE
AU  - Dirk Daelemans
AU  - Dominique Schols
AU  - Myriam Witvrouw
AU  - Christophe Pannecouque
AU  - Sigrid Hatse
AU  - Sonia van Dooren
AU  - François Hamy
AU  - Thomas Klimkait
AU  - Erik de Clercq
AU  - Anne-Mieke VanDamme
TI  - 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
DP  - 2000 Jan 01
TA  - Molecular Pharmacology
PG  - 116--124
VI  - 57
IP  - 1
4099  - http://molpharm.aspetjournals.org/content/57/1/116.short
4100  - http://molpharm.aspetjournals.org/content/57/1/116.full
SO  - Mol Pharmacol2000 Jan 01; 57
AB  - 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-1LAV 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. The American Society for Pharmacology and Experimental Therapeutics