Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, a-790742.

Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, a-790742. Research Abstract Details 

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Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, a-790742. Abstract Text:

Tatyana Dekhtyar,Teresa I Ng,Liangjun Lu,Sherie Masse,David A Degoey,William J Flosi,David J Grampovnik,Larry L Klein,Dale J Kempf,Akhteruzzaman Molla,

A-790742 is a potent human immunodeficiency virus type 1 (HIV-1) protease inhibitor, with 50% effective concentrations ranging from 2 to 7 nM against wild-type HIV-1. The activity of this compound is lowered by approximately sevenfold in the presence of 50% human serum. A-790742 maintained potent antiviral activity against lopinavir-resistant variants generated in vitro as well as against a panel of molecular clones containing proteases derived from HIV-1 patient isolates with multiple protease mutations. During in vitro selection, A-790742 selected two primary mutations (V82L and I84V) along with L23I, L33F, K45I, A71V/A, and V77I in the pNL4-3 background and two other mutations (A71V and V82G) accompanied by M46I and L63P in the HIV-1 RF background. HIV-1 pNL4-3 clones with a single V82L or I84V mutation were phenotypically resistant to A-790742 and ritonavir. Taking these results together, A-790742 displays a favorable anti-HIV-1 profile against both the wild type and a large number of mutants resistant to other protease inhibitors. The selection of the uncommon V82L and V82G mutations in protease by A-790742 suggests the potential for an advantageous resistance profile with this protease inhibitor.

Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, a-790742. Publishing Authors By Initials

T Dekhtyar,TI Ng,L Lu,S Masse,DA Degoey,WJ Flosi,DJ Grampovnik,LL Klein,DJ Kempf,A Molla,

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Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, a-790742. Journal Published:

PUBLICATION TYPE: Journal Article

Journal: Antimicrobial agents and chemotherapy

VOLUME: 52

Page Numbers: 1337-44

Journal Abbreviation: Antimicrob. Agents Chemother.

ISSN: 0066-4804

DAY: 22

MONTH: 01

YEAR: 2008

Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, a-790742. Information

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LANGUAGE: eng

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AFFILIATION: 200 Abbott Park Rd., R43H, AP52-N, Abbott Park, IL 60064. tanya.chernyavskiy@abbott.com.

Country: United States

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MEDLINETA: Antimicrob Agents Chemother

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