ArticleAntimicrobial agents and chemotherapy2007
Identification and characterization of UK-201844, a novel inhibitor that interferes with human immunodeficiency virus type 1 gp160 processing.
Article in Antimicrobial agents and chemotherapy, 2007. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
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Who cites it
9 citing papers in PubMed, 14 citations in OpenAlex.
- Brief introduction of current technologies in isolation of broadly neutralizing HIV-1 antibodies.Virus research · 2018Review
- Targeting RNA-protein interactions within the human immunodeficiency virus type 1 lifecycle.Biochemistry · 2013Article
- Discovery of novel small-molecule HIV-1 replication inhibitors that stabilize capsid complexes.Antimicrobial agents and chemotherapy · 2013Article
- TargetHunter: an in silico target identification tool for predicting therapeutic potential of small organic molecules based on chemogenomic database.The AAPS journal · 2013Article
- Envelope glycoprotein of arenaviruses.Viruses · 2012Review
- Fangchinoline inhibits human immunodeficiency virus type 1 replication by interfering with gp160 proteolytic processing.PloS one · 2012Article
- HIV envelope: challenges and opportunities for development of entry inhibitors.Trends in microbiology · 2011Review
- HIV capsid is a tractable target for small molecule therapeutic intervention.PLoS pathogens · 2010Article
- New small-molecule inhibitor class targeting human immunodeficiency virus type 1 virion maturation.Antimicrobial agents and chemotherapy · 2009Article
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Authors and funding
13 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
More than 10(6) compounds were evaluated in a human immunodeficiency virus type 1 (HIV-1) high-throughput antiviral screen, resulting in the identification of a novel HIV-1 inhibitor (UK-201844). UK-201844 exhibited antiviral activity against HIV-1 NL4-3 in MT-2 and PM1 cells, with 50% effective concentrations of 1.3 and 2.7 microM, respectively, but did not exhibit measurable antiviral activity against the closely related HIV-1 IIIB laboratory strain. UK-201844 specifically inhibited the production of infectious virions packaged with an HIV-1 envelope (Env), but not HIV virions packaged with a heterologous Env (i.e., the vesicular stomatitis virus glycoprotein), suggesting that the compound targets HIV-1 Env late in infection. Subsequent antiviral assays using HIV-1 NL4-3/IIIB chimeric viruses showed that HIV-1 Env sequences were critical determinants of UK-201844 susceptibility. Consistent with this, in vitro resistant-virus studies revealed that amino acid substitutions in HIV-1 Env are sufficient to confer resistance to UK-201844. Western analysis of HIV Env proteins expressed in transfected cells or in isolated virions showed that UK-201844 inhibited HIV-1 gp160 processing, resulting in the production of virions with nonfunctional Env glycoproteins. Our results demonstrate that UK-201844 represents the prototype for a unique HIV-1 inhibitor class that directly or indirectly interferes with HIV-1 gp160 processing.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.