In vitro evaluation of nonnucleoside reverse transcriptase inhibitors UC-781 and TMC120-R147681 as human immunodeficiency virus microbicides

被引：124

作者：

Van Herrewege, Y

Michiels, J

Van Roey, J

Fransen, K

Kestens, L

Balzarini, J

Lewi, P

Vanham, G

Janssen, P

机构：

[1] Inst Trop Med, Dept Microbiol, Immunol Lab, B-2000 Antwerp, Belgium

[2] Inst Trop Med, Dept Microbiol, AIDS Reference Lab, B-2000 Antwerp, Belgium

[3] Tibotec Virco NV, Mechelen, Belgium

[4] Katholieke Univ Leuven, Rega Inst Med Res, Lab Virol & Chemotherapy, B-3000 Louvain, Belgium

[5] Janssen Pharmaceut, Ctr Mol Design, Vosselaar, Belgium

来源：

ANTIMICROBIAL AGENTS AND CHEMOTHERAPY | 2004年 / 48卷 / 01期

关键词：

D O I：

10.1128/AAC.48.1.337-339.2004

中图分类号：

Q93 [微生物学];

学科分类号：

071005 ; 100705 ;

摘要：

The nonnucleoside reverse transcriptase inhibitors UC-781 and TMC120-R147681 (Dapivirine) effectively prevented human immunodeficiency virus (HIV) infection in cocultures of monocyte-derived dendritic cells and T cells, representing primary targets in sexual transmission. Both drugs had a favorable therapeutic index. A 24-h treatment with 1,000 nM UC-781 or 100 nM TMC120-R147681 prevented cell-free HIV infection, whereas 10-fold-higher concentrations blocked cell-associated HIV.

引用

收藏

页码：337 / 339

页数：3

相关论文

共 22 条

[11] Correlation of human immunodeficiency virus type 1 RNA levels in blood and the female genital tract [J].

Hart, CE ;

Lennox, JL ;

Pratt-Palmore, M ;

Wright, TC ;

Schinazi, RF ;

Evans-Strickfaden, T ;

Bush, TJ ;

Schnell, C ;

Conley, LJ ;

Clancy, KA ;

Ellerbrock, TV .

JOURNAL OF INFECTIOUS DISEASES, 1999, 179 (04) :871-882

[12] The urgent need for new HIV/STD prevention options for women [J].

Irwin, K ;

Scarlett, M ;

Moseley, R .

JOURNAL OF WOMENS HEALTH, 1998, 7 (09) :1081-1086

[13] Evolution of anti-HIV drug candidates.: Part 3:: Diarylpyrimidine (DAPY) analogues [J].

Ludovici, DW ;

De Corte, BL ;

Kukla, MJ ;

Ye, H ;

Ho, CY ;

Lichtenstein, MA ;

Kavash, RW ;

Andries, K ;

de Béthune, MP ;

Azijn, H ;

Pauwels, R ;

Lewi, PJ ;

Heeres, J ;

Koymans, LMH ;

de Jonge, MR ;

Van Aken, KJA ;

Daeyaert, FFD ;

Das, K ;

Arnold, E ;

Janssen, PAJ .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2001, 11 (17) :2235-2239

[14] MECHANISMS OF HIV/SIV MUCOSAL TRANSMISSION [J].

MILMAN, G ;

SHARMA, O .

AIDS RESEARCH AND HUMAN RETROVIRUSES, 1994, 10 (10) :1305-1312

[15] CONTRACEPTIVES OF THE FUTURE IN THE LIGHT OF HIV-INFECTION [J].

SHORT, RV .

AUSTRALIAN & NEW ZEALAND JOURNAL OF OBSTETRICS & GYNAECOLOGY, 1994, 34 (03) :330-332

[16] Cellular targets of infection and route of viral dissemination after an intravaginal inoculation of simian immunodeficiency virus into rhesus macaques [J].

Spira, AI ;

Marx, PA ;

Patterson, BK ;

Mahoney, J ;

Koup, RA ;

Wolinsky, SM ;

Ho, DD .

JOURNAL OF EXPERIMENTAL MEDICINE, 1996, 183 (01) :215-225

[17] Safety study of nonoxynol-9 as a vaginal microbicide: Evidence of adverse effects [J].

Stafford, MK ;

Ward, H ;

Flanagan, A ;

Rosenstein, IJ ;

Taylor-Robinson, D ;

Smith, JR ;

Weber, J ;

Kitchen, VS .

JOURNAL OF ACQUIRED IMMUNE DEFICIENCY SYNDROMES AND HUMAN RETROVIROLOGY, 1998, 17 (04) :327-331

[18] HIV PREVENTION - THE NEED FOR METHODS WOMEN CAN USE [J].

STEIN, ZA .

AMERICAN JOURNAL OF PUBLIC HEALTH, 1990, 80 (04) :460-462

[19] Considerations and development of topical microbicides to inhibit the sexual transmission of HIV [J].

Turpin, JA .

EXPERT OPINION ON INVESTIGATIONAL DRUGS, 2002, 11 (08) :1077-1097

[20] Activity of reverse transcriptase inhibitors in monocyte-derived dendritic cells:: A possible in vitro model for postexposure prophylaxis of sexual HIV transmission [J].

Van Herrewege, Y ;

Penne, L ;

Vereecken, C ;

Fransen, K ;

Van der Groen, G ;

Kestens, L ;

Balzarini, J ;

Vanham, G .

AIDS RESEARCH AND HUMAN RETROVIRUSES, 2002, 18 (15) :1091-1102