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HIV-1 Entry, Inhibitors, and Resistance
Department of Molecular Biology and Microbiology and Division of Infectious Diseases, Department of Medicine, Case Western Reserve University, 10900 Euclid Ave., Cleveland, OH 44106, USA
* Author to whom correspondence should be addressed.
Received: 23 February 2010; in revised form: 16 April 2010 / Accepted: 18 April 2010 / Published: 29 April 2010
Abstract: Entry inhibitors represent a new class of antiretroviral agents for the treatment of infection with HIV-1. While resistance to other HIV drug classes has been well described, resistance to this new class is still ill defined despite considerable clinical use. Several potential mechanisms have been proposed: tropism switching (utilization of CXCR4 instead of CCR5 for entry), increased affinity for the coreceptor, increased rate of virus entry into host cells, and utilization of inhibitor-bound receptor for entry. In this review we will address the development of attachment, fusion, and coreceptor entry inhibitors and explore recent studies describing potential mechanisms of resistance.
Keywords: HIV-1; envelope; gp120; V3 loop; gp41; CCR5; maraviroc; vicriviroc
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Lobritz, M.A.; Ratcliff, A.N.; Arts, E.J. HIV-1 Entry, Inhibitors, and Resistance. Viruses 2010, 2, 1069-1105.
Lobritz MA, Ratcliff AN, Arts EJ. HIV-1 Entry, Inhibitors, and Resistance. Viruses. 2010; 2(5):1069-1105.
Lobritz, Michael A.; Ratcliff, Annette N.; Arts, Eric J. 2010. "HIV-1 Entry, Inhibitors, and Resistance." Viruses 2, no. 5: 1069-1105.