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PDBsum entry 2l6t
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Antiviral protein
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PDB id
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2l6t
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References listed in PDB file
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Key reference
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Title
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Short-Term monotherapy in HIV-Infected patients with a virus entry inhibitor against the gp41 fusion peptide.
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Authors
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W.G.Forssmann,
Y.H.The,
M.Stoll,
K.Adermann,
U.Albrecht,
H.C.Tillmann,
K.Barlos,
A.Busmann,
A.Canales-Mayordomo,
G.Giménez-Gallego,
J.Hirsch,
J.Jiménez-Barbero,
D.Meyer-Olson,
J.Münch,
J.Pérez-Castells,
L.Ständker,
F.Kirchhoff,
R.E.Schmidt.
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Ref.
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Sci Transl Med, 2010,
2,
63re3-63re3.
[DOI no: ]
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PubMed id
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Abstract
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No abstract given.
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Secondary reference #1
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Title
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Discovery and optimization of a natural HIV-1 entry inhibitor targeting the gp41 fusion peptide.
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Authors
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J.Münch,
L.Ständker,
K.Adermann,
A.Schulz,
M.Schindler,
R.Chinnadurai,
S.Pöhlmann,
C.Chaipan,
T.Biet,
T.Peters,
B.Meyer,
D.Wilhelm,
H.Lu,
W.Jing,
S.Jiang,
W.G.Forssmann,
F.Kirchhoff.
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Ref.
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Cell, 2007,
129,
263-275.
[DOI no: ]
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PubMed id
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Figure 4.
Figure 4. Improved Antiviral Potency of VIRIP Derivatives
(A) P4-CCR5 indicator cells were infected with NL4-3 stocks
containing 1.0 ng p24 antigen in the presence of VIRIP, a
variety of VIRIP derivatives (amino acid sequence shown in left
panel; p, D-proline; cysteine residues are linked via a
disulfide bridge), or T20. Average values obtained from
quintuple infections are shown (right panel). The results were
confirmed in two to five independent experiments.
(B and C)
Dose-dependent inhibition of (B) primary HIV-1 isolates of
different subtype and coreceptor usage (indicated in
parentheses) or (C) RT-, protease-, and T20-resistant HIV-1
variants by VIR-576. NL4-3wt inhibition by VIRIP and T20 is
shown for comparison. All curves give average values obtained
from triplicate infections. Similar results were obtained in two
independent experiments.
(D and E) Inhibition of R5-tropic
HIV-1 replication in ex vivo infected human tonsillary
lymphocyte aggregate cultures by (D) VIR-353 and VIR-576 and (E)
T20. Shown are average luciferase activities in culture
supernatants derived from triplicate infections. Similar results
were obtained with another R5-tropic HIV-1 clone and X4-tropic
NL4-3wt. RLU/s, relative light units per second. Figure 4.
Improved Antiviral Potency of VIRIP Derivatives(A) P4-CCR5
indicator cells were infected with NL4-3 stocks containing 1.0
ng p24 antigen in the presence of VIRIP, a variety of VIRIP
derivatives (amino acid sequence shown in left panel; p,
D-proline; cysteine residues are linked via a disulfide bridge),
or T20. Average values obtained from quintuple infections are
shown (right panel). The results were confirmed in two to five
independent experiments.(B and C) Dose-dependent inhibition of
(B) primary HIV-1 isolates of different subtype and coreceptor
usage (indicated in parentheses) or (C) RT-, protease-, and
T20-resistant HIV-1 variants by VIR-576. NL4-3wt inhibition by
VIRIP and T20 is shown for comparison. All curves give average
values obtained from triplicate infections. Similar results were
obtained in two independent experiments.(D and E) Inhibition of
R5-tropic HIV-1 replication in ex vivo infected human tonsillary
lymphocyte aggregate cultures by (D) VIR-353 and VIR-576 and (E)
T20. Shown are average luciferase activities in culture
supernatants derived from triplicate infections. Similar results
were obtained with another R5-tropic HIV-1 clone and X4-tropic
NL4-3wt. RLU/s, relative light units per second.
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Figure 5.
Figure 5. Inhibitory Mechanism of VIRIP
(A) Inhibition of
HIV-1 Env-mediated cell fusion by the indicated peptides.
Identical symbols are also used in (B)–(D). Average values of
triplicate measurements are shown in (A)–(C).
(B)
Inhibitory effect of VIRIP derivatives and fusion inhibitors on
gp41 6-HB formation.
(C) Inhibitory effect of VIRIP
derivatives and T20 on hemolysis induced by HIV-1, SIV/HIV-2,
and MLV FPs.
(D) Inhibition of NL4-3wt, an NL4-3 chimera
containing the SIV/HIV-2 FP and SIVmac239, by various VIRIP
derivatives and T20. The upper panel shows an alignment of the
gp41 FP sequences of HIV-1 and SIV/HIV-2. Dashes and the dot
indicate amino acid identity and a gap, respectively. Average
values obtained from sextuple infections of P4-CCR5 indicator
cells are shown. Figure 5. Inhibitory Mechanism of VIRIP(A)
Inhibition of HIV-1 Env-mediated cell fusion by the indicated
peptides. Identical symbols are also used in (B)–(D). Average
values of triplicate measurements are shown in (A)–(C).(B)
Inhibitory effect of VIRIP derivatives and fusion inhibitors on
gp41 6-HB formation.(C) Inhibitory effect of VIRIP derivatives
and T20 on hemolysis induced by HIV-1, SIV/HIV-2, and MLV
FPs.(D) Inhibition of NL4-3wt, an NL4-3 chimera containing the
SIV/HIV-2 FP and SIVmac239, by various VIRIP derivatives and
T20. The upper panel shows an alignment of the gp41 FP sequences
of HIV-1 and SIV/HIV-2. Dashes and the dot indicate amino acid
identity and a gap, respectively. Average values obtained from
sextuple infections of P4-CCR5 indicator cells are shown.
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The above figures are
reproduced from the cited reference
with permission from Cell Press
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