Inhibition of Human Immunodeficiency Virus Type 1 Integration by Diketo Derivatives-Reference-Cited by-同舟云学术

Inhibition of Human Immunodeficiency Virus Type 1 Integration by Diketo Derivatives

Published:2002-10 Issue:10 Volume:46 Page:3292-3297
ISSN:0066-4804
Container-title:Antimicrobial Agents and Chemotherapy
language:en
Short-container-title:Antimicrob Agents Chemother

Author:

Pluymers Wim¹,Pais Godwin²,Van Maele Bénédicte¹,Pannecouque Christophe¹,Fikkert Valery¹,Burke Terrence R.²,De Clercq Erik¹,Witvrouw Myriam¹,Neamati Nouri³,Debyser Zeger¹

Affiliation:

1. Rega Institute for Medical Research, K.U. Leuven, Minderbroedersstraat 10, B-3000 Leuven, Belgium

2. Laboratory of Medicinal Chemistry, Center for Cancer Research, National Cancer Institute, Frederick, Maryland 21702

3. School of Pharmacy, University of Southern California, Los Angeles, California 90089

Abstract

ABSTRACT A series of diketo derivatives was found to inhibit human immunodeficiency virus type 1 (HIV-1) integrase activity. Only L-708,906 inhibited the replication of HIV-1(III B ) (50% effective concentration, 12 μM), HIV-1 clinical strains, HIV-1 strains resistant to reverse transcriptase or fusion inhibitors, HIV-2 (ROD strain) and simian immunodeficiency virus (MAC 251 ). The combinations of L-708,906 with zidovudine, nevirapine, or nelfinavir proved to be subsynergistic. In cell culture, addition of L-708,906 could be postponed for 7 h after infection, a moment coinciding with HIV integration. Inhibition of integration in cell culture was confirmed by quantitative Alu-PCR.

Publisher

American Society for Microbiology

Subject

Infectious Diseases,Pharmacology (medical),Pharmacology

Link

https://journals.asm.org/doi/pdf/10.1128/AAC.46.10.3292-3297.2002

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