Entry inhibitors, viruses

Petersen J, Dandri M, Mier W, Lfltgehetmann M, Volz T, von Weizsacker F, Haberkom U, Fischer L, Pollok JM, Erbes B, Seitz S, Urban S (2008) Prevention of hepatitis B virus infection in vivo by entry inhibitors derived from the large envelope protein, Nat Biotechnol 26 335-341 PorniUos O, Garrus JE, Sundquist WI (2002) Mechanisms of enveloped RNA virus budding. Trends CeU Biol 12 569-579... 

Abstract The entry of viruses into target cells involves a complex series of sequential steps, with opportunities for inhibition at every stage. Entry inhibitors exert their biological properties by inhibiting protein-protein interactions either within the viral envelope (Env) glycoproteins or between viral Env and host-cell receptors. The nature of resistance to entry inhibitors also differs from compounds inhibiting enzymatic targets due to their different modes of action and the relative variability in... 

Jacobson JM, Lowy 1, Fletcher CV, O NeUl TJ, Tran DN, Ketas TJ, Trkola A, Klotman ME, Maddon PJ, Olson WC, Israel RJ (2000) Single-dose safety, pharmacology, and antiviral activity of the human immunodeficiency virus (HIV) type 1 entry inhibitor PRO 542 in HIV-infected adults. J Infect Dis 182 326-329... 

Platt EJ, Dumin IP, Rabat D (2005) Kinetic factors control efficiencies of cell entry, efficacies of entry inhibitors, and mechanisms of adaptation of human immunodeficiency virus, J Virol 79 4347 356... 

Fig. 1 Antiviral genes inhibit virus replication at different stages of the viral life cycle. Early inhibitors prevent the establishment of the viral genome in the target cell (class I, e.g., entry inhibitors, RT inhibitors for HIV). Intermediate inhibitors prevent viral gene expression or amplification of the viral genome (class II, e.g., siRNAs, antisense RNAs). Late inhibitors prevent virion assembly or release, or inactivate the mature virions (class III, e.g., transdominant core proteins, capsid-targeted virion inactivation, CTVI). A list of antiviral genes in each class is found in Table 1...

Reeves JD, Miamidian JL, Biscone MJ, et al. Impact of mutations in the coreceptor binding site on human immunodeficiency virus type 1 fusion, infection, and entry inhibitor sensitivity. J Virol 2004 78(10) 5476-5485. 

Studying the molecular recognition of hgands by native viruses and VLPs offers structural insight into the viral attachment and entry processes. Details at atomic resolution are important for our understanding of these early events during the viral life cycle [6]. Drug development benefits from this effort in order to develop entry inhibitors. 

Zhang HJ, Rothwangl K, Mesecar AD, Sabahi A, Rong LJ, Fong HHS. Lamiridosins, Hepatitis C Virus Entry Inhibitors from Lamium album. Journal of Natural Products 2009 72 2158-2162. 

Finally, a group of agents known as HIV entry inhibitors is beginning to reach the market. These drugs impair the ability of the virus to attach to the host cell s surface, thereby inhibiting HIV entry into susceptible lymphocytes. If the virus cannot enter the cell, it cannot infect that cell or begin the process of viral replication. Enfuviritide (Fuzeon) is the first HIV entry inhibitor to be approved, and other drugs of this type will hopefully be available in the near future. 

Jiang S, Lu H, Liu S et al (2004) N-substituted pyrrole derivatives as novel human immunodeficiency virus type 1 entry inhibitors that interfere with the gp41 six-helix bundle formation and block virus fusion. Antimicrob Agents Chemother 48 4349-4359... 

Hartley, O., Dorgham, K., Perez-Bercoff, D., Cerini, F., Heimann, A., Gaertner, H., Offord, R. E., Pancino, G., Debre, P., and Gorochov, G. (2003). Human immunodeficiency virus type 1 entry inhibitors selected on living cells from a library of phage chemokines. / Virol. 77, 6637-6644. 

Human iinniunodeficiency virus. 369t. 372 Humon immunodeficiency virus infection chcmokinc receptor binders for. 387 gp4I fusion activity inhibitors for. 387-388 HIV entry inhibitors for. 387 HIV protease inhibitors for. 384-387 iniegrase inhibiion for. 388 newer agents for. 382-388 reverse transcriptase inhilulors for. 372. 379-381... 

Lobritz MA, Ratcliff AN, Arts EJ (2010) HIV-1 entry, inhibitors, and resistance. Viruses 2 1069-1105... 

Madani N, Perdigoto AL, Srinivasan K et al (2004) Localized changes in the gp 120 envelope glycoprotein confer resistance to human immunodeficiency virus entry inhibitors BMS-806 and 155. J Virol 78 3742-3752... 

Wang T. Inhibitors of Human Immunodeficiency Virus Type 1 (HIV-1) attachment. Part x. SAR of 4-Methoxy 6-Azaindole series of HIV gpl20 entry inhibitors and discovery of BMS-626529 and its phosphonoxymethyl prodrug BMS-663068 (Manuscript in preparation)... 

Lu RJ, Tucker JA, Zinevitch T et al (2007) Design and synthesis of human immunodeficiency virus entry inhibitors sulfonamide as an isostere for the a-ketoamide group. J Med Chem 50 6535-6544... 

Lu R-J, Tucker JA, Pickens J et al (2009) Heterobiaryl human immunodeficiency virus entry inhibitors. J Med Chem 52 4481 1487... 

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