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TMC310911, a Novel Human Immunodeficiency Virus Type 1 Protease Inhibitor, Shows In Vitro an Improved Resistance Profile and Higher Genetic Barrier to Resistance Compared with Current Protease Inhibitors

dc.contributor.authorDierynck, Inge
dc.contributor.authorVan Marck, Herwig
dc.contributor.authorVan Ginderen, Marcia
dc.contributor.authorJonckers, Tim H. M.
dc.contributor.authorNalam, Madhavi N. L.
dc.contributor.authorSchiffer, Celia A.
dc.contributor.authorRaoof, Araz
dc.contributor.authorKraus, Guenter
dc.contributor.authorPicchio, Gaston
dc.date2022-08-11T08:08:00.000
dc.date.accessioned2022-08-23T15:38:45Z
dc.date.available2022-08-23T15:38:45Z
dc.date.issued2011-12-08
dc.date.submitted2011-11-22
dc.identifier.citationAntimicrob Agents Chemother. 2011 Dec;55(12):5723-31. Epub 2011 Sep 6. <a href="http://dx.doi.org/10.1128/AAC.00748-11">Link to article on publisher's site</a>
dc.identifier.issn0066-4804 (Linking)
dc.identifier.doi10.1128/AAC.00748-11
dc.identifier.pmid21896904
dc.identifier.urihttp://hdl.handle.net/20.500.14038/26001
dc.description.abstractTMC310911 is a novel human immunodeficiency virus type 1 (HIV-1) protease inhibitor (PI) structurally closely related to darunavir (DRV) but with improved virological characteristics. TMC310911 has potent activity against wild-type (WT) HIV-1 (median 50% effective concentration [EC(50)], 14 nM) and a wide spectrum of recombinant HIV-1 clinical isolates, including multiple-PI-resistant strains with decreased susceptibility to currently approved PIs (fold change [FC] in EC(50), >10). For a panel of 2,011 recombinant clinical isolates with decreased susceptibility to at least one of the currently approved PIs, the FC in TMC310911 EC(50) was
dc.language.isoen_US
dc.relation<a href="http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?db=pubmed&cmd=Retrieve&list_uids=21896904&dopt=Abstract">Link to Article in PubMed</a>
dc.relation.urlhttp://dx.doi.org/10.1128/AAC.00748-11
dc.subjectDrug Resistance, Viral
dc.subjectHIV Antigens
dc.subjectHIV Protease Inhibitors
dc.subjectHIV-1
dc.subjectHumans
dc.subjectVirus Replication
dc.subjectgag Gene Products, Human Immunodeficiency Virus
dc.subjectBiochemistry, Biophysics, and Structural Biology
dc.subjectMicrobiology
dc.titleTMC310911, a Novel Human Immunodeficiency Virus Type 1 Protease Inhibitor, Shows In Vitro an Improved Resistance Profile and Higher Genetic Barrier to Resistance Compared with Current Protease Inhibitors
dc.typeJournal Article
dc.source.journaltitleAntimicrobial agents and chemotherapy
dc.source.volume55
dc.source.issue12
dc.identifier.legacycoverpagehttps://escholarship.umassmed.edu/bmp_pp/131
dc.identifier.contextkey2367980
html.description.abstract<p>TMC310911 is a novel human immunodeficiency virus type 1 (HIV-1) protease inhibitor (PI) structurally closely related to darunavir (DRV) but with improved virological characteristics. TMC310911 has potent activity against wild-type (WT) HIV-1 (median 50% effective concentration [EC(50)], 14 nM) and a wide spectrum of recombinant HIV-1 clinical isolates, including multiple-PI-resistant strains with decreased susceptibility to currently approved PIs (fold change [FC] in EC(50), >10). For a panel of 2,011 recombinant clinical isolates with decreased susceptibility to at least one of the currently approved PIs, the FC in TMC310911 EC(50) was</p>
dc.identifier.submissionpathbmp_pp/131
dc.contributor.departmentDepartment of Biochemistry and Molecular Pharmacology
dc.source.pages5723-31


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