IndraLab

Statements

Bevirimat inhibits CASP1. 24 / 24
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"First, bevirimat does not inhibit CA-SP1 processing in the context of monomeric Gag in solution but instead requires immature virus assembly for its activity."
19534569
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"A recently developed HIV-1 inhibitor, PA-457 or bevirimat, targets the CA-SP1 cleavage site to prevent virion maturation."
18657842
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"Furthermore, bevirimat was shown to block CA-SP1 processing in vitro when Gag self assembled into VLPs but not in the absence of assembly [91]."
18468560
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"Although the mechanism by which PA-457 prevents cleavage of CA-SP1 has not been fully defined, recent data suggest that the compound binds directly the CA-SP1 region of an oligomeric form of Gag withi[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
17586320
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"Specifically, PA-457 blocks the conversion of the capsid precursor (CA-SP1, p25) to mature capsid protein (CA, p24), resulting in the release of immature, noninfectious viral particles."
16863445
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"This observation suggests that Bevirimat not only prevents CA-SP1 cleavage but also may stabilize the immature lattice 33."
21762804
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"Since bevirimat treatment of virus producing cells does not completely block CA-SP1 processing XREF_BIBR, the degree of cleavage in the resulting particle preparations was determined by immunoblot (XREF_FIG)."
24915417
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"BVM specifically inhibits CA-SP1 cleavage, which occurs late in the Gag proteolytic cleavage cascade [XREF_BIBR, XREF_BIBR]."
22888428
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"The precise mechanism by which BVM inhibits CA-SP1 cleavage has not been established."
19782103
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"BVM does not inhibit CA-SP1 processing in the context of monomeric Gag in solution [XREF_BIBR], but instead requires Gag assembly for its activity [XREF_BIBR, XREF_BIBR, XREF_BIBR]."
22888428
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"We found that the BVM analogs could effectively block CA-SP1 processing of HIV-1 clade C in contrast to the parental BVM, which was completely inactive against the clade C clones."
27264714
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"Previous studies demonstrated that BVM does not completely block CA-SP1 processing but acts as a kinetic inhibitor to delay PR mediated cleavage at this site."
20172577
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"To determine whether BVM disrupts CA-SP1 processing in the context of the L363I and M367I mutations, we evaluated the effect of this compound on levels of CA, CA *, and CA-SP1 in virions by quantitative radioimmunoprecipitation analysis."
20172577
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"Further, BVM binds to a pocket formed during Gag oligomerization, as BVM does not inhibit CA-SP1 processing in the context of monomeric Gag in solution, but rather requires Gag assembly for its activity."
19782103
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"XREF_BIBR - XREF_BIBR Bevirimat (XREF_FIG) inhibits HIV-1 maturation by preventing the cleavage of CA-SP1 (p25) Gag into Capsid (p24) and SP1 (p2)."
21084190
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"Although bevirimat specifically disrupts CA-SP1 cleavage, it has been shown that the compound does not affect the viral PR function XREF_BIBR, XREF_BIBR."
26713265
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"It is noteworthy that BVM disrupts but does not completely block CA-SP1 processing; some mature CA is generated even at high concentrations of the compound."
23144615
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"The precise mechanism by which bevirimat prevents cleavage of CA-SP1 has not been fully elucidated; however, a large body of experimental data appears to suggest that the CA-SP1 junction of an oligomeric form of Gag within the immature particles is molecular target of bevirimat XREF_BIBR, XREF_BIBR, XREF_BIBR, XREF_BIBR, XREF_BIBR, XREF_BIBR, XREF_BIBR, XREF_BIBR, XREF_BIBR."
26713265
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"Two working models have been proposed to explain how bevirimat blocks processing of CA-SP1 cleavage site."
26713265
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"Specifically, PA-457 blocks the conversion of the capsid precursor (CA-SP1, p25) to mature capsid protein (CA, p24) resulting in the release of immature, non infectious viral particles."
15562372
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"Bevirimat causes a dose dependent inhibition of CA-SP1 cleavage and severely impairs HIV infectivity in human thymocytes."
21602280
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"Furthermore, in our in vitro maturation system, the maturation inhibitor BVM not only blocked cleavage of CA-SP1 but also partially protected the MA-CA cleavage site."
27958264
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"A recently developed HIV-1 inhibitor, PA-457 or bevirimat, targets the CA-SP1 cleavage site to prevent virion maturation."
18657842
reach
"The observation that bevirimat delays but does not completely block CA-SP1 processing suggests that the presence of uncleaved CA-SP1 may disrupt the maturation process in trans."
20172577