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Supplementary Information accompanies the paper on www.nature.com/nature.
Acknowledgements We thank M. Fujioka and J. Jaynes for transgenic flies containing the eve
4 þ 6–lacZ construct; L. Andrioli for discussions and support; A. Oberstein for technical
assistance; and C. Desplan, J. Blau and T. Cook for encouragement and comments on the
manuscript. D.E.C. was supported by a grant from the NSF. This work was also supported by a
grant from the NIH.
Competing interests statement The authors declare that they have no competing financial
interests.
Correspondence and requests for materials should be addressed to S.S. (stephen.small@nyu.edu).
..............................................................
The gene product Murr1
restricts HIV-1 replication
in resting CD4
1
lymphocytes
Lakshmanan Ganesh
1
, Ezra Burstein
1,2
, Anuradha Guha-Niyogi
1
,
Mark K. Louder
1
, John R. Mascola
1
, Leo W. J. Klomp
3
, Cisca Wijmenga
3
,
Colin S. Duckett
2
& Gary J. Nabel
1
1
Vaccine Research Center, NIAID, National Institutes of Health, Building 40,
Room 4502, MSC-3005, 40 Convent Drive, Bethesda, Maryland 20892-3005,
USA
2
University of Michigan, Medical Science I, Room 5315, 1301 Catherine Street,
Ann Arbor, Michigan 48109-0602, USA
3
University Medical Center Utrecht, Lundlaan 6, 3584 EA Utrecht,
The Netherlands
.............................................................................................................................................................................
Although human immunodeficiency virus-1 (HIV-1) infects
quiescent and proliferating CD4
1
lymphocytes, the virus repli-
cates poorly in resting T cells
1–6
. Factors that block viral replica-
tion in these cells might help to prolong the asymptomatic phase
of HIV infection
7
; however, the molecular mechanisms that
control this process are not fully understood. Here we show
that Murr1, a gene product known previously for its involvement
in copper regulation
8,9
, inhibits HIV-1 growth in unstimulated
CD4
1
T cells. This inhibition was mediated in part through its
ability to inhibit basal and cytokine-stimulated nuclear factor
(NF)-kB activity. Knockdown of Murr1 increased NF-kB activity
and decreased IkB-a concentrations by facilitating phospho-IkB-
a degradation by the proteasome. Murr1 was detected in CD4
1
T cells, and RNA-mediated interference of Murr1 in primary
resting CD4
1
lymphocytes increased HIV-1 replication. Through
its effects on the proteasome, Murr1 acts as a genetic restriction
factor that inhibits HIV-1 replication in lymphocytes, which
could contribute to the regulation of asymptomatic HIV infec-
tion and the progression of AIDS.
Murr1 is a highly conserved 190-amino-acid protein that does
not have any identifiable motifs, and a homozygous deletion in the
gene encoding canine Murr1 leads to copper toxicosis in Bedlington
terriers
8
. In this study, Murr1 was initially identified in a two-hybrid
screen by binding the X-linked inhibitor of apoptosis, a known
activator of NF-kB (refs 10, 11, and E.B., unpublished observations).
To study its effect on NF-kB, HIV-1 reporter plasmids with wild-
type or mutant (DkB) sites
2
were co-transfected with control or
Murr1 expression plasmids in the different cell lines. Murr1 inhib-
ited both basal and tumour necrosis factor (TNF)-a-dependent
HIV-1 transcription from the wild-type but not the kB-mutant
reporter in Jurkat T-leukaemia and 293T renal epithelial cell lines
(Fig. 1a, left and middle panels). In contrast, Murr1 did not
substantially inhibit tumour growth factor-b-dependent transcrip-
tion in HepG2 cells, confirming its specificity (Fig. 1a, right panel).
The kB effect was dose-dependent and observed with other inducers
of NF-kB, including interleukin-1 (IL-1) and 12-O-tetradecanoyl-
phorbol-13-acetate (TPA) (Fig. 1b). Murr1 modulated the
expression of endogenous kB-regulated genes: transfection into
293T cells decreased the endogenous cell-surface expression of
major histocompatibility complex (MHC) class I, in contrast to
CD9, which is independent of NF-kB (Fig. 1c).
Its site of action in the NF-kB signalling pathway was further
defined by co-transfection of different regulators with an NF-kB
reporter in Jurkat T cells. Whereas Murr1 inhibited both IKK-1- and
IKK-2-induced NF-kB activity (Fig. 1d, middle and right panels), it
failed to block RelA-mediated transcription (Fig. 1d, left panel),
indicating that Murr1 might interact downstream of the IkB
kinase signalosome. As determined by immunoprecipitation, co-
transfected haemagglutinin (HA)-tagged Murr1 and Myc-tagged
IKK-2 did not associate in vivo (Fig. 2a, lane 2, left panel). Although
IKK-1 also did not associate with Murr1 (data not shown), an
interaction between transfected HA-tagged Murr1 and endogenous
IkB-a was readily detected (Fig. 2a, lane 6). The ankyrin domain of
IkB-a was required for association with Murr1, as were amino acids
1–160 of Murr1 (Supplementary Fig. 1a).
A polyclonal antibody against Murr1 demonstrated the associ-
ation between endogenous Murr1 and IkB-a in vivo. RelA antibody
immunoprecipitated IkB-a,IkB-b and Murr1 (Fig. 2b, lane 10).
IkB-a antibody also pulled down RelA and Murr1 (Fig. 2b, lane 12),
but the IkB-b antibody did not precipitate Murr1 (Fig. 2b, lane 14),
suggesting that Murr1 interacted preferentially with the NF-kB–
IkB-a complex. This association was confirmed in vivo by confocal
microscopy with fluorescent fusion proteins (Supplementary
Fig. 1b), similarly to the pattern of RelA association with IkB-a
12–14
.
The physiological consequences of these interactions were deter-
mined by knockdown of endogenous Murr1 in 293T cells using
control and Murr1-specific short interfering RNA (siRNA)
duplexes. The specificity of two such siRNAs, Murr1-1 and
Murr1-2, directed to different Murr1 sequences, was first confirmed
by transfecting 293T cells with wild-type or mutant siRNAs along
with wild-type or mutant Murr1 complementary DNAs modified at
the siRNA target site (Supplementary Fig. 2). Transient transfection
of Murr1-specific siRNA duplexes downregulated endogenous Murr1
and IkB-a, had little effect on IkB-b, p65 or IKK-2 (Fig. 3a, left panel),
and increased kB-dependent reporter activity (Fig. 3a, right panel).
To investigate the mechanism of Murr1 action, 293T cells were
transfected with a control or Murr1 siRNA. Four days after
transfection, cells were treated with the proteasome inhibitor
MG132 for 2 h or with vehicle alone and stimulated with TNF-a.
Cells depleted of Murr1 showed a decrease in basal IkB-a (Fig. 3a)
and an increase and persistence of phospho-IkB-a in response to
stimulation with TNF-a (Fig. 3b, left panel). This effect was
observed in the absence of a proteasome inhibitor, MG132, but
not in its presence (Fig. 3b, right panel), indicating that Murr1
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