Structure-Activity Relationships of the Human Immunodeficiency Virus Type 1 Maturation Inhibitor PF-46396

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Structure-Activity Relationships of the Human Immunodeficiency Virus Type 1 Maturation Inhibitor PF-46396 is …
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scholarly articleQ13442814

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P356DOI10.1128/JVI.01075-16
P3181OpenCitations bibliographic resource ID4629845
P932PMC publication ID5008107
P698PubMed publication ID27384665

P50authorCatherine S AdamsonQ55364196
Nicholas J WestwoodQ58183835
P2093author name stringTerry K Smith
Lisa Pirrie
Fanny Tran
Christopher Murgatroyd
P2860cites workThe prototype HIV-1 maturation inhibitor, bevirimat, binds to the CA-SP1 cleavage site in immature Gag particlesQ21245046
A single polymorphism in HIV-1 subtype C SP1 is sufficient to confer natural resistance to the maturation inhibitor bevirimatQ24606079
Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infectionQ24672964
Alkyl Amine Bevirimat Derivatives Are Potent and Broadly Active HIV-1 Maturation InhibitorsQ27324263
Structures of the HIV-1 capsid protein dimerization domain at 2.6 A resolutionQ27617655
Cryo-electron microscopy of tubular arrays of HIV-1 Gag resolves structures essential for immature virus assemblyQ27683857
Structure of the immature HIV-1 capsid in intact virus particles at 8.8 Å resolutionQ27696126
Structure of the carboxyl-terminal dimerization domain of the HIV-1 capsid proteinQ27746461
Anti-human immunodeficiency virus activity of YK-FH312 (a betulinic acid derivative), a novel compound blocking viral maturationQ28360742
Structural and functional insights into the HIV-1 maturation inhibitor binding pocketQ28485054
Production of acquired immunodeficiency syndrome-associated retrovirus in human and nonhuman cells transfected with an infectious molecular cloneQ29547734
Assembly and architecture of HIV.Q30455050
Retroviral proteases and their roles in virion maturationQ38393674
HIV-1 assembly, release and maturation.Q38539565
HIV-1 protease inhibitor mutations affect the development of HIV-1 resistance to the maturation inhibitor bevirimat.Q38549717
Sequential steps in human immunodeficiency virus particle maturation revealed by alterations of individual Gag polyprotein cleavage sites.Q39579012
Characterization of a putative alpha-helix across the capsid-SP1 boundary that is critical for the multimerization of human immunodeficiency virus type 1 gag.Q39685850
A structurally disordered region at the C terminus of capsid plays essential roles in multimerization and membrane binding of the gag protein of human immunodeficiency virus type 1.Q39699793
Functional Surfaces of the Human Immunodeficiency Virus Type 1 Capsid ProteinQ39748566
The spacer peptide between human immunodeficiency virus capsid and nucleocapsid proteins is essential for ordered assembly and viral infectivityQ39870242
Methods for the study of HIV-1 assembly.Q39914278
The p2 domain of human immunodeficiency virus type 1 Gag regulates sequential proteolytic processing and is required to produce fully infectious virions.Q40042979
Mutagenesis of protease cleavage sites in the human immunodeficiency virus type 1 gag polyproteinQ40059062
Processing of in vitro-synthesized gag precursor proteins of human immunodeficiency virus (HIV) type 1 by HIV proteinase generated in Escherichia coli.Q40131039
Inhibition of HIV-1 maturation via drug association with the viral Gag protein in immature HIV-1 particlesQ40357793
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimatQ40750425
Mutation of the SP1 sequence impairs both multimerization and membrane-binding activities of human immunodeficiency virus type 1 Gag.Q40894533
Protease-Mediated Maturation of HIV: Inhibitors of Protease and the Maturation ProcessQ41844750
Susceptibility of human immunodeficiency virus type 1 to the maturation inhibitor bevirimat is modulated by baseline polymorphisms in Gag spacer peptide 1Q42202820
3-O-(3',3'-dimethysuccinyl) betulinic acid inhibits maturation of the human immunodeficiency virus type 1 Gag precursor assembled in vitroQ42424208
A strongly transdominant mutation in the human immunodeficiency virus type 1 gag gene defines an Achilles heel in the virus life cycleQ42546287
Flexibility in the P2 domain of the HIV-1 Gag polyproteinQ43094794
Treatment with indinavir, zidovudine, and lamivudine in adults with human immunodeficiency virus infection and prior antiretroviral therapyQ45760702
Cleavage of HIV-1 gag polyprotein synthesized in vitro: sequential cleavage by the viral proteaseQ69564852
Human immunodeficiency virus type 1 resistance to the small molecule maturation inhibitor 3-O-(3',3'-dimethylsuccinyl)-betulinic acid is conferred by a variety of single amino acid substitutions at the CA-SP1 cleavage site in GagQ30478394
Electron cryotomography of immature HIV-1 virions reveals the structure of the CA and SP1 Gag shellsQ30479297
Replacement of the P1 amino acid of human immunodeficiency virus type 1 Gag processing sites can inhibit or enhance the rate of cleavage by the viral proteaseQ30850215
Helical structure determined by NMR of the HIV-1 (345-392)Gag sequence, surrounding p2: implications for particle assembly and RNA packagingQ30980940
Novel approaches to inhibiting HIV-1 replication.Q33624690
The capsid-spacer peptide 1 Gag processing intermediate is a dominant-negative inhibitor of HIV-1 maturationQ33727091
A putative alpha-helical structure which overlaps the capsid-p2 boundary in the human immunodeficiency virus type 1 Gag precursor is crucial for viral particle assemblyQ33782377
Role of matrix in an early postentry step in the human immunodeficiency virus type 1 life cycleQ33782781
Relationship between human immunodeficiency virus type 1 Gag multimerization and membrane bindingQ33787084
Roles of matrix, p2, and N-terminal myristoylation in human immunodeficiency virus type 1 Gag assemblyQ33794223
Anti-AIDS agents 81. Design, synthesis, and structure-activity relationship study of betulinic acid and moronic acid derivatives as potent HIV maturation inhibitorsQ33814879
Polymorphisms in Gag spacer peptide 1 confer varying levels of resistance to the HIV- 1 maturation inhibitor bevirimatQ33864444
On the role of the SP1 domain in HIV-1 particle assembly: a molecular switch?Q34164929
HIV chemotherapyQ34223088
p6Gag is required for particle production from full-length human immunodeficiency virus type 1 molecular clones expressing proteaseQ34288376
A controlled trial of two nucleoside analogues plus indinavir in persons with human immunodeficiency virus infection and CD4 cell counts of 200 per cubic millimeter or less. AIDS Clinical Trials Group 320 Study TeamQ34438252
HIV-1 maturation inhibitor bevirimat stabilizes the immature Gag latticeQ34529834
The survival benefits of AIDS treatment in the United StatesQ34533291
In vitro resistance to the human immunodeficiency virus type 1 maturation inhibitor PA-457 (Bevirimat).Q35139703
Identification of an HIV-1 Mutation in Spacer Peptide 1 That Stabilizes the Immature CA-SP1 Lattice.Q35832693
Synthesis of betulinic acid derivatives as entry inhibitors against HIV-1 and bevirimat-resistant HIV-1 variantsQ36185528
Anti-AIDS agents 90. novel C-28 modified bevirimat analogues as potent HIV maturation inhibitors.Q36340098
Role of the major homology region of human immunodeficiency virus type 1 in virion morphogenesis.Q36624411
Evidence for a functional interaction between the V1/V2 and C4 domains of human immunodeficiency virus type 1 envelope glycoprotein gp120.Q36632356
Partial inhibition of the human immunodeficiency virus type 1 protease results in aberrant virus assembly and the formation of noninfectious particles.Q36650046
New betulinic acid derivatives for bevirimat-resistant human immunodeficiency virus type-1.Q36691642
Human immunodeficiency virus type 1 assembly, release, and maturation.Q36857103
The gag gene products of human immunodeficiency virus type 1: alignment within the gag open reading frame, identification of posttranslational modifications, and evidence for alternative gag precursorsQ36881276
Small-molecule inhibition of human immunodeficiency virus type 1 replication by specific targeting of the final step of virion maturationQ36944553
PA-457: A potent HIV inhibitor that disrupts core condensation by targeting a late step in Gag processingQ37089562
Impact of human immunodeficiency virus type 1 resistance to protease inhibitors on evolution of resistance to the maturation inhibitor bevirimat (PA-457)Q37192174
A two-pronged structural analysis of retroviral maturation indicates that core formation proceeds by a disassembly-reassembly pathway rather than a displacive transition.Q37336728
New small-molecule inhibitor class targeting human immunodeficiency virus type 1 virion maturationQ37450688
HIV-1 assembly, budding, and maturationQ38023864
P433issue18
P407language of work or nameEnglishQ1860
P304page(s)8181-8197
P577publication date2016-09-15
P1433published inJournal of VirologyQ1251128
P1476titleStructure-Activity Relationships of the Human Immunodeficiency Virus Type 1 Maturation Inhibitor PF-46396
P478volume90

Reverse relations

cites work (P2860)
Q37676344Insights into the activity of maturation inhibitor PF-46396 on HIV-1 clade C
Q90646261Resistance to Second-Generation HIV-1 Maturation Inhibitors

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