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Tài liệu Báo cáo khoa học: Interferon-a induces sensitization of cells to inhibition of protein synthesis by tumour necrosis factor-related apoptosis-inducing ligand ppt

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Tiêu đề Interferon-a induces sensitization of cells to inhibition of protein synthesis by tumour necrosis factor-related apoptosis-inducing ligand
Tác giả Ian W. Jeffrey, Androulla Elia, Stéphanie Bornes, Vivienne J. Tilleray, Karthiga Gengatharan, Michael J. Clemens
Trường học St George’s, University of London
Chuyên ngành Molecular and Metabolic Signalling
Thể loại báo cáo khoa học
Năm xuất bản 2006
Thành phố London
Định dạng
Số trang 11
Dung lượng 735,35 KB

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We have demonstrated previously that TRAIL has an inhibitory effect on protein synthesis [Jeffrey IW, Bushell M, Tilleray VJ, Morley S & Clemens MJ 2002 Cancer Res 62, 2272–2280] and we

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protein synthesis by tumour necrosis factor-related

apoptosis-inducing ligand

Ian W Jeffrey, Androulla Elia, Ste´phanie Bornes*, Vivienne J Tilleray, Karthiga Gengatharan and Michael J Clemens

Translational Control Group, Centre for Molecular and Metabolic Signalling, Division of Basic Medical Sciences, St George’s, University of London, UK

Members of the tumour necrosis factor-a (TNFa)

fam-ily are well known as inhibitors of cell growth and

inducers of apoptosis in a wide variety of systems [1]

We have previously shown that both TNFa and

tumour necrosis factor-related apoptosis-inducing

ligand (TRAIL) cause rapid downregulation of global

protein synthesis in MCF-7 breast cancer cells [2] In

addition, studies with embryonic fibroblasts deficient

in the interferon (IFN)-inducible, double-stranded

RNA-dependent protein kinase (PKR) demonstrated

that expression of this protein is essential for the

TNFa-induced inhibition of translation [2] Consistent

with these observations, the a subunit of polypeptide chain eukaryotic initiation factor eIF2, which is a sub-strate for PKR, becomes more highly phosphorylated

in cells exposed to TRAIL or TNFa It is well estab-lished that the phosphorylation of eIF2a by PKR results in inhibition of polypeptide chain initiation [3] There are, however, additional events that impinge

on the translational machinery in TNFa-treated or TRAIL-treated cells In particular, we have observed increased association of the inhibitory protein eukary-otic initiation factor 4E-binding protein (4E-BP1) with the mRNA cap-binding factor eIF4E in cells

Keywords

caspases; interferon-a; polypeptide chain

initiation; protein synthesis; TRAIL

Correspondence

M J Clemens, Division of Basic Medical

Sciences, St George’s, University of

London, Cranmer Terrace, London SW17

0RE, UK

Fax: +44 20 8725 2992

Tel: +44 20 8725 5762

E-mail: M.Clemens@sgul.ac.uk

*Present address

De´partement d’Oncoge´ne´tique, Centre

Biome´dicale de Recherche et Valorisation,

Clermont-Ferrand, France.

(Received 15 March 2006, revised 19 May

2006, accepted 12 June 2006)

doi:10.1111/j.1742-4658.2006.05374.x

Tumour cells are often sensitized by interferons to the effects of tumour necrosis factor-a-related apoptosis-inducing ligand (TRAIL) We have demonstrated previously that TRAIL has an inhibitory effect on protein synthesis [Jeffrey IW, Bushell M, Tilleray VJ, Morley S & Clemens MJ (2002) Cancer Res 62, 2272–2280] and we have therefore examined the consequences of prior interferon-a treatment for the sensitivity of transla-tion to inhibitransla-tion by TRAIL Interferon treatment alone has only a minor effect on protein synthesis but it sensitizes both MCF-7 cells and HeLa cells to the downregulation of translation by TRAIL The inhibi-tion of translainhibi-tion is characterized by increased phosphorylainhibi-tion of the a subunit of eukaryotic initiation factor eIF2 and dephosphorylation of the eIF4E-binding protein 4E-BP1 Both of these effects, as well as the decrease in overall protein synthesis, require caspase-8 activity, although they precede overt apoptosis by several hours Interferon-a enhances the level and⁄ or the extent of activation of caspase-8 by TRAIL, thus provi-ding a likely explanation for the sensitization of cells to the inhibition of translation

Abbreviations

4E-BP, eukaryotic initiation factor 4E binding protein; BID, Bcl-2-interacting death protein; eIF, eukaryotic initiation factor; FADD, Fas-associated death domain; IFN, interferon; PARP, poly(ADP-ribose) polymerase; PKR, RNA-dependent protein kinase; TNFa, tumour necrosis factor-a; TRAIL, tumour necrosis factor-a-related apoptosis-inducing ligand; zIETD.FMK, zIle-Glu-Thr-Asp-fluoromethyl ketone.

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treated with TNFa [2] Competition between 4E-BP1

and eIF4G for binding to eIF4E regulates the extent

of formation of the eIF4F initiation complex and

hence the rate of 5¢-cap-dependent protein synthesis

[4–6]

Exposure to IFNs often alters the sensitivity of cells

to agents such as TRAIL, although this varies with cell

type (reviewed in [7]) In some cases, IFNs can be

proapoptotic in their own right [8–12], but more

usu-ally these cytokines are cytostatic rather than cytotoxic

when applied as single agents [13,14] However,

numer-ous reports indicate that prior treatment with IFNs

(either type I or type II) can sensitize cells to the

effects of members of the TNFa family [15–21]

(reviewed in [7,22]) In this study, we have investigated

whether IFNa also has effects on the sensitivity of cells

to TRAIL-induced downregulation of protein

synthe-sis Our data indicate that IFNa treatment sensitizes

both MCF-7 and HeLa cells to the translational

inhib-itory effect of TRAIL This inhibition of translation

precedes by several hours the appearance of overtly

apoptotic or nonviable cells

Binding of TRAIL to its active receptors,

TRAIL-R1 (DR4) and TRAIL-R2 (DR5), results in the

recruitment of procaspase-8 to the death-inducing

sig-nalling complex at the cell membrane, a process

mediated by the Fas-associated death domain

(FADD) protein [23] Procaspase-8 then undergoes

proteolytic processing that converts it from p53 and

p55 forms to p41 and p43 intermediates [24], and the

latter give rise to the large and small subunits of

act-ive caspase-8 [25,26] Caspase-8 in turn is responsible

for initiating a cascade of activation of effector

casp-ases that ultimately leads to the multiple changes in

cells characteristic of TRAIL-induced apoptosis [27]

The process of activation of caspase-8, and the

down-stream consequences that arise from it, are blocked

by the caspase-8-specific peptide inhibitor

zIle-Glu-Thr-Asp-fluoromethyl ketone (zIETD.FMK) [17] We

show here that the effects of TRAIL on overall

pro-tein synthesis and the phosphorylation of eIF2a

require the activity of caspase-8 Moreover, TRAIL

also causes extensive dephosphorylation of 4E-BP1,

and this too is a caspase-8-dependent phenomenon

Consistent with its effects on the regulation of protein

synthesis, IFNa enhances the extent of activation of

caspase-8 by TRAIL in MCF-7 and HeLa cells Our

data therefore suggest that the degree to which this

apical caspase is activated determines not only the

extent of apoptosis but also the ability of TRAIL to

regulate the initiation of translation at the level of

eIF2a phosphorylation and 4E-BP1

dephosphoryla-tion

Results

Effects of IFNa treatment on the sensitivity of cells to inhibition of protein synthesis by TRAIL

We have previously shown that protein synthesis is rapidly downregulated following exposure of cells to TRAIL and other inducers of apoptosis [2,28,29] In most cases, such inhibition precedes the loss of cell viability and is not simply a consequence of cell death However, the influence of IFNs on the regulation of translation by TRAIL has not previously been investi-gated We therefore examined the effect of increasing concentrations of TRAIL on the incorporation of [35S]methionine into total protein in cells that had or had not been pretreated with IFNa The data shown

in Fig 1A indicate that the combination of the two cytokines had a marked effect on overall protein syn-thesis in MCF-7 cells This was manifested as a sensiti-zation by IFNa pretreatment to the effect of TRAIL

In MCF-7 cells not previously exposed to IFNa,

25 ngÆmL)1 TRAIL was required to inhibit protein synthesis by 50% within 5 h, whereas when the cells had been pretreated with IFNa, only 10 ngÆmL)1 TRAIL was required to produce the same extent of inhibition at this time-point (inset to Fig 1A) This sensitization was largely due to a permissive effect of IFNa, since the latter had only a relatively small effect

on protein synthesis in the absence of TRAIL We observed a similar sensitizing effect of IFN in HeLa cells (Fig 1B), although in this case the cells were

two-to three-fold more sensitive than MCF-7 cells two-to TRAIL As shown previously [2], the downregulation

of translation by TRAIL was not a secondary conse-quence of the loss of cell viability, since, during the times examined, viability remained close to 100% as judged by trypan blue exclusion (I W Jeffrey, unpub-lished results) Moreover, very few cells became overtly apoptotic at these early times after initiation of TRAIL treatment (see below)

Role of caspase-8 in the regulation of protein synthesis by TRAIL

We have examined whether caspase-8, which is activa-ted following the binding of TRAIL to its receptors and the formation of the death-inducing signalling complex [30], is required for the inhibition of transla-tion The data in Fig 2A show that in MCF-7 cells the caspase-8-specific inhibitor zIETD.FMK largely prevented the inhibitory effect of TRAIL on protein synthesis This was the case whether or not the cells had been pretreated with IFNa (I W Jeffrey, unpublished

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0 10 25 50 75 100 200 500

0

1

2

3

4

5

TRAIL (ng/ml)

3- )

A

0 25 50 75 100

TRAIL (ng/ml) (log scale)

0

1

2

3

4

TRAIL (ng/ml )

0.1 1 10 100 0

25 50 75 100

TRAIL (ng/ml) (log scale)

3-B

Fig 1 Effects of IFNa on the sensitivity of MCF-7 and HeLa cells

to inhibition of protein synthesis by TRAIL MCF-7 cells (A) and

HeLa cells (B) were cultured for 72 and 24 h, respectively, in the

absence (light-shaded bars) or presence (dark-shaded bars) of

human IFNa 2b (1000 UÆmL)1) and then further treated with the

indi-cated concentrations of TRAIL for the last 5 h (A) or 3 h (B) Protein

synthesis was measured by the incorporation of [ 35 S]methionine

into acid-insoluble material for the last 40 min The data are the

means ± SEM of three determinations Insets: percentage

inhibi-tion of protein synthesis as a funcinhibi-tion of TRAIL concentrainhibi-tion in

cells without IFN (squares) or with prior IFN treatment (triangles).

The arrows indicate the concentrations of TRAIL producing 50%

inhibition of protein synthesis.

0 25 50 75 100

A

TRAIL Control TRAIL + z-IETD.FMK

p18

full length (p53/55) p41/43

B

TRAIL Control z-IETD.FMK

full length t-BID

TRAIL + z-IETD.FMK

C

BID

(Pro)caspase-8

αα-tubulin

Fig 2 Effects of zIETD.FMK on TRAIL-induced inhibition of protein synthesis and caspase-8 activity in MCF-7 cells (A) MCF-7 cells were incubated with or without TRAIL (167 ngÆmL)1) for 5 h as indicated Where shown, zIETD.FMK was present at 10 l M Protein synthesis was then measured as described in Fig 1 The data are expressed as percentage of the value obtained with untreated con-trol cells and are the means ± SEM of three determinations (B) Total cytoplasmic extracts were prepared and subjected to SDS gel electrophoresis, and this was followed by immunoblotting for procaspase-8 and processed forms of the enzyme The positions of the full-length (p53 ⁄ p55) forms of the protein and the p41 ⁄ p43 and p18 cleavage products are indicated The samples were also immu-noblotted for a-tubulin as a loading control (C) A similar experiment was performed as in (B) and extracts were immunoblotted for BID The positions of the full-length protein and the cleavage product t-BID are indicated.

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results) Although peptide inhibitors containing the

IETD sequence preferentially inhibit caspase-8 [31], it

was possible that zIETD.FMK might directly affect

other caspases as well However, a specific requirement

for caspase-8 for the effect on protein synthesis is

indi-cated by the fact that caspase-8-deficient Jurkat cells

[32] are also largely resistant to the inhibition of

methionine incorporation by TRAIL, in contrast to

wild-type Jurkat cells (Table 1) In MCF-7 cells,

zIETD.FMK impaired the TRAIL-induced cleavage of

the p53 and p55 forms of procaspase-8 to the p41 and

p43 intermediates and the p18 subunit by only about

50% (Fig 2B) However, the effect of zIETD.FMK

was sufficient to restore protein synthesis to about

80% of the control rate Moreover, the

caspase-8-mediated cleavage of the Bcl-2 family member BID

[33,34] was completely inhibited by zIETD.FMK

under the same conditions (Fig 2C)

TRAIL treatment strongly enhanced the

phosphory-lation of the a subunit of polypeptide chain initiation

factor eIF2 in MCF-7 cells, in the presence or absence

of prior IFN treatment (Fig 3A,B) Neither TRAIL

nor IFNa had any effect on the level of total eIF2a

TRAIL treatment also decreased the extent of

phos-phorylation of 4E-BP1, as revealed by a shift in the

migration of the latter protein on SDS gels from the

b and c forms to the hypophosphorylated a form

(Fig 3C,D) and by the loss of immunoreactivity with

a phosphospecific antibody directed at residue Ser65

(Fig 3D, right panel) In view of the effect of

zIE-TD.FMK on the inhibition of protein synthesis by

TRAIL (Fig 2A), the requirement for caspase-8 for

these events was determined Both the increase in

phosphorylation of eIF2a and the decrease in

phos-phorylation of 4E-BP1 caused by TRAIL were

com-pletely blocked by treatment of MCF-7 cells with

zIETD.FMK (Fig 3B,C) Similar results were

obtained with HeLa cells The caspase-8 inhibitor had

no effect on the total levels of these factors (A Elia, unpublished results) Moreover, treatment of caspase-8-deficient Jurkat cells with TRAIL failed to cause any dephosphorylation of 4E-BP1 (Fig 3D) or any change

in the phosphorylation of eIF2a (A Elia, unpublished results), in contrast to the effects of TRAIL on wild-type Jurkat cells

Since caspase-8 activity is required for the regulation

of translation by TRAIL, it was also of interest to determine whether IFN affected the level or extent of activation of caspase-8 in MCF-7 and HeLa cells

Table 1 Requirement for caspase-8 for inhibition of protein

synthe-sis by TRAIL Wild-type and caspase-8-deficient Jurkat cells

were incubated for 3 h in the absence or presence of TRAIL

(400 ngÆmL)1) Protein synthesis was measured by the

incorpor-ation of [35S]methionine into acid-insoluble material for the last

60 min The data are the means ± SEM of four to six

determina-tions.

Cell line

[ 35 S]methionine incorporation (counts per min per 10 5 cells) (· 10)3)

Inhibition by TRAIL (%)

Wild type 4.44 ± 0.08 1.11 ± 0.05 75.0

Caspase-8 deficient 3.89 ± 0.11 3.43 ± 0.11 11.8

eIF2 αα((P)

A TRAIL - + - +

eIF2 αα(P)

TRAIL - + - + Z.IETD.FMK - - + +

B

α

βγ

C

Total 4E-BP1

TRAIL - + + Z.IETD.FMK - - +

TRAIL - + - + TRAIL - + - + D

Total 4E-BP1

4E-BP1

Wild-type C8-deficient Wild-type C8-deficient

Fig 3 Caspase-8 requirement for TRAIL-induced changes in the state of phosphorylation of eIF2a and 4E-BP1 (A) MCF-7 cells were grown for 72 h in the absence or presence of human IFNa 2b (1000 UÆmL)1) and further treated with or without TRAIL (167 ngÆmL)1) for the last 5 h as indicated Total cytoplasmic extracts were prepared and analysed by SDS gel electrophoresis followed by immunoblotting for phosphorylated eIF2a (Ser51) and total eIF2a as indicated (B,C) MCF-7 cells were incubated for 5 h

in the absence or presence of TRAIL (167 ngÆmL)1) and zIETD.FMK (10 l M ) as indicated Extracts were prepared as in (A) and analysed

by immunoblotting for (B) phosphorylated eIF2a (Ser51) and (C) 4E-BP1 The hypophosphorylated (a) and the b and c forms of 4E-BP1 are indicated in (C) (D) Wild-type and caspase-8-deficient Jurkat cells were incubated for 3 h in the absence (-)or presence (+) of TRAIL (150 ngÆmL)1) Extracts were prepared and analysed by immunoblotting for total 4E-BP1 (left panel) and phosphorylated 4E-BP1 (Ser65) (right panel).

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Examination of the levels of procaspase-8 in MCF-7

cells by immunoblotting and quantitative densitometry

(Fig 4A,C) showed that IFNa treatment resulted in a c

40% increase in the immunoreactive signals, but without

any activation of the enzyme (as indicated by the lack of

processing to the p41⁄ p43 or p18 products) TRAIL

treatment led to processing of the basal and elevated

amounts of procaspase-8 in both control and

IFN-trea-ted cells and there was an approximately two-fold

increase in the amount of the p18 large subunit of active

caspase-8 in cells treated with IFN and TRAIL,

com-pared to the amount in cells treated with TRAIL alone

(Fig 4A,C) Enhancement of the level of p18 was also

observed after IFN and TRAIL treatment of HeLa cells,

although densitometry of the immunoblots showed that

in this case there was no measurable increase in the level

of the proenzyme in cells treated with IFNa in the

absence of TRAIL (Fig 4B,C) In contrast to these

effects on caspase-8, there were no IFN-induced or

TRAIL-induced changes in the levels of other proteins

involved in TRAIL signalling (i.e FADD and the

TRAIL receptors DR4 and DR5), or in levels of the

caspase-8 antagonist cellular FLICE-like inhibitory

protein (I W Jeffrey, unpublished results)

To investigate whether IFNa could enhance the activity of caspase-8 in cells subsequently treated with TRAIL, we examined the extent of cleavage of the caspase-8 substrate Bcl-2-interacting death protein (BID) to form truncated BID (t-BID) [33,34] We also monitored the cleavage of the 116 kDa caspase sub-strate poly(ADP-ribose) polymerase (PARP) to pro-duce its characteristic 89-kDa cleavage product The results in Fig 5 show that TRAIL alone induced partial cleavage of BID and PARP within 5 h IFNa alone had no effect on BID or PARP cleavage, but enhanced the effect of TRAIL such that very little of the full-length form of either protein remained in the IFN-treated cells after 5 h of exposure to TRAIL Thus, the activity of caspase-8, and most likely that of downstream effector caspases also, is enhanced in cells treated with the combination of IFNa and TRAIL, relative to TRAIL alone

In view of the cleavage of caspase substrates such as BID and PARP, the effect of IFNa and TRAIL on the DNA content of MCF-7 cells was also assessed, using fluorescence-activated cell sorting Figure 6 shows that, in spite of the activation of caspase-8 and the cleavage of BID and PARP, TRAIL alone had

full length (p53/55) p41/43

p18

A Control TRAIL IFNααα IFNαα

+ TRAIL

Caspase-8

B

full length (p53/55) p41/43

p18

Control TRAIL IFNα IFNα

+TRAIL

αα-tubulin

0 25 50 75

100

p53/p55 0

25 50 75

100

MCF-7 cells

HeLa cells

Control + TRAIL + IFNαα

(141%)

(88%) (103%)

(90%)

(143%) C

Fig 4 Effects of IFNa and TRAIL on levels and activation of caspase-8 in MCF-7 and HeLa cells MCF-7 cells (A) and HeLa cells (B) were incubated for 72 h and 24 h, respectively, in the absence or presence of IFNa (1000 unitsÆmL)1), and then treated with or without TRAIL as indicated (MCF-7 cells, 5 h at 167 ngÆmL)1; HeLa cells, 3 h at 10 ngÆmL)1) Total cytoplasmic extracts were prepared and analysed by SDS gel electrophoresis followed by immunoblotting for caspase-8 and a-tubulin In (A) the samples were analysed in duplicate The positions of the full-length (p53 ⁄ p55) forms of caspase-8 and the p41 ⁄ p43 and p18 cleavage products are indicated (C) The intensities of the caspase-8 bands were determined by quantitative densitometry The values in brackets above the histograms show the relative intensities of the appropriate bands in the IFN-treated cells, as a percentage of the values seen in the absence of IFNa treatment.

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very little effect on the appearance of cells with a

sub-G1 DNA content Approximately 1 and 6% of the

total cell population showed a decreased DNA content

after 4 and 16 h, respectively In cells pretreated with

IFNa, the corresponding figures were approximately 2

and 16% at 4 and 16 h after exposure to TRAIL,

respectively A recent report has analysed the basis for

the relative insensitivity of MCF-7 cells to these and

other apoptotic effects of TRAIL, and it has been

sug-gested that this is due to the absence of caspase-3 [35]

However, in MCF-7 cells, the cleavage of DNA during

apoptosis may also be effected through the activity of

caspase-6 and⁄ or caspase-7 [36,37] Our data therefore

indicate that, although the substantial inhibition of

protein synthesis caused by TRAIL within 4–5 h

requires caspase-8 activity, it precedes the loss of

cellu-lar DNA and is not a consequence of overt apoptosis

However, the sensitizing effect of IFNa for

caspase-mediated substrate cleavages in cells exposed to

TRAIL is reflected in the increased number of cells

with a sub-G1 content of DNA appearing at later

times, confirming the reports that IFNa can sensitize

cells to TRAIL-induced apoptosis [15–21]

Discussion

Effects of TRAIL on protein synthesis

Previous studies have shown that a rapid decrease in

the rate of overall protein synthesis occurs in cells

exposed to various proapoptotic stimuli, including

treatment with members of the TNFa family [2,28]

Using MCF-7 and HeLa cells, we have now shown

that the TRAIL-induced inhibition of translation is a

caspase-8-dependent event that is modified by IFNa

treatment The effect of IFN is to sensitize MCF-7

and HeLa cells to the effects of TRAIL, and the enhanced downregulation of translation seen in the presence of IFN correlates with increased caspase activity Although the inhibition of protein synthesis requires caspase activity, it precedes the appearance of

an overtly apoptotic phenotype and the loss of cell viability (Fig 6) In contrast to the effects of TRAIL, IFN treatment alone has relatively little effect on translation; it also does not significantly activate caspase-8 (Fig 4) or result in any cleavage of BID or PARP (Fig 5)

In TRAIL-treated cells, both the increased phos-phorylation of eIF2a and the modulation of 4E-BP1 activity are blocked by the broad-specificity caspase inhibitor zVal-Ala-Asp-fluoromethyl ketone [2] We have now extended those findings to demonstrate a specific requirement for caspase-8 activity for these changes The caspase-8 inhibitor zIETD.FMK was able to prevent completely both the phosphorylation

of eIF2a and the dephosphorylation of 4E-BP1 in cells exposed to TRAIL (Fig 3B,C) Moreover, in Jurkat cells, deficiency for caspase-8 [32] rendered the cells resistant to the effects of TRAIL on initiation factor phosphorylation (Fig 3D) and overall protein synthe-sis (Table 1) Caspase-8 is intimately involved in the function of the TRAIL-activated death-inducing sig-nalling complex [27,30], and so it is not surprising that its activity is required However, it is of interest that caspase-8 plays a specific role in the regulation of translation, particularly as the inhibition of polypep-tide chain initiation by TRAIL precedes apoptosis by several hours The requirement for caspase-8 activity

in MCF-7 cells, as revealed by the inhibitor studies, is confirmed by the inability of caspase-8-deficient cells

to show extensive inhibition of translation in response

to TRAIL treatment (Table 1)

The IFN-induced sensitization of MCF-7 and HeLa cells to TRAIL is consistent with the enhancement by IFN of the level of TRAIL-induced active caspase-8 (Fig 4) Our data suggest that, at least in MCF-7 cells, IFN pretreatment induces cells to express a higher level of procaspase-8 We have not determined the molecular basis for this, but others have shown that the promoter for procaspase-8 contains an IFN-stimu-lated response element and responds to both IFNa and IFNc with transcriptional upregulation [38–40] In Huh7 hepatoma cells, IFNa treatment results in enhancement of the expression of procaspase-8 at both the RNA and protein levels, and this sensitizes the cells to the proapoptotic effects of TRAIL Interest-ingly, our data suggest that only relatively small changes in caspase-8 activity appear to be sufficient to alter substantially the cellular sensitivity to TRAIL

Control TRAIL IFNα IFNα

+ TRAIL

α−

α−tubulin

BID

full length protein

cleavage product (t-BID) full length protein

Fig 5 TRAIL-induced caspase activity is enhanced by IFNa

pre-treatment MCF-7 cells were grown for 72 h in the absence or

presence of human IFNa 2b (1000 UÆmL)1) and further incubated

with or without TRAIL (167 ngÆmL)1) for the last 5 h as indicated.

Total cytoplasmic extracts were prepared and subjected to SDS gel

electrophoresis, followed by immunoblotting for BID, PARP and

a-tubulin The positions of the full-length proteins and their caspase

cleavage products are indicated.

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zIETD.FMK caused only a partial reduction in

TRAIL-induced cleavage of procaspase-8 (Fig 2B),

and IFN treatment caused at best only a two-fold

increase in the level of the catalytically active form of

caspase-8 in cells subsequently exposed to TRAIL

(Fig 4) Nevertheless, zIETD.FMK was able to

decrease the inhibition of protein synthesis by TRAIL

by 80% (Fig 2A) and, conversely, IFNa enhanced the

sensitivity of protein synthesis to TRAIL in MCF-7

cells and HeLa cells by 2.5-fold and 10-fold,

respect-ively (Fig 1) These results are consistent with the

con-cept that the activity of caspase-8 is rate-limiting for

the biological effects of TRAIL [40] and that relatively

small changes in caspase-8 activity can be amplified by

downstream events, including the activation of effector caspases

Mechanisms of inhibition of protein synthesis

We have shown that TRAIL treatment causes both phosphorylation of eIF2a and dephosphorylation of 4E-BP1 The latter change results in increased associ-ation of 4E-BP1 with eIF4E (S Bornes, unpublished results) The question therefore arises as to which mechanism is responsible for the inhibition of overall protein synthesis Since Kim et al [41] have previously reported that MCF-7 cells are relatively insensitive to the effects of eIF2a phosphorylation, it is likely that

Control

DNA content

Sub-G1 0.3%

DNA content

Sub-G1 0.4%

DNA content

+TRAIL (4h)

Sub-G1 0.8%

DNA content

+TRAIL (4h)

Sub-G1 1.6%

DNA content

+TRAIL (16h)

Sub-G1 6.1%

DNA content

+TRAIL (16h)

Sub-G1 16.0%

Fig 6 Effects of IFNa and TRAIL on cellular DNA content MCF-7 cells were incubated for 24 h in the absence or presence of human IFNa2b (1000 UÆmL)1) and then further treated with or without TRAIL (100 ngÆmL)1) for the last 4 h or 16 h as indicated The cells were fixed, stained with propidium iodide and analysed for DNA content by fluorescence-activated cell sorting The percentage of cells with a sub-G1 DNA content is indicated in each panel.

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the regulation of 4E-BP1 activity is the more

import-ant change for the downregulation of translation

following TRAIL treatment Nevertheless, TRAIL

treatment enhances the level of the transcription factor

ATF4 (I W Jeffrey, unpublished results), the

expres-sion of which is known to be upregulated at the

trans-lational level in response to increased phosphorylation

of eIF2a [42] This suggests that increased eIF2a

phos-phorylation does have a role to play in the cellular

response to TRAIL TRAIL may be able to activate

the IFN-inducible protein kinase PKR, which targets

eIF2a as a substrate and is required for inhibition of

protein synthesis by TNFa [2] However, it is possible

that other eIF2a kinases are also stimulated by

TRAIL

Relationship of translational inhibition to

apoptosis

A striking synergistic effect on the induction of

apoptosis is often observed when cells are treated

with members of the IFN and TNF families together

(reviewed in [7,22]), and the enhanced inhibition of

protein synthesis by TRAIL observed in IFN-treated

MCF-7 and HeLa cells is clearly related to this

However, this inhibition is an early effect of TRAIL

treatment and, at least in MCF-7 cells, precedes

apoptosis by several hours Compared to HeLa cells,

MCF-7 cells are in fact relatively insensitive to the

apoptosis-inducing effect of TRAIL This may be

because they lack caspase-3 activity [35]

Interest-ingly, although caspase-3 is clearly not essential for

the inhibition of protein synthesis, MCF-7 cells are

also much less sensitive than HeLa cells to this effect

of TRAIL (Fig 1)

As indicated above, our data are consistent with a

role for caspase-8 regulation in mediating the effect of

IFNa on the sensitivity of protein synthesis to

inhibi-tion by TRAIL In other systems, increased apoptosis

seen in response to IFNa plus TRAIL is characterized

by elevated caspase-8 and caspase-9 activity, with

enhanced degradation of BID and translocation of

Bax to mitochondria [15], and we have also observed

similar phenomena As well as the induction of

ca-spase-8 by IFNs [40,43–45], there are several other

potential mechanisms that could also operate to bring

about such synergism, including IFN-induced

enhance-ment of the expression of TRAIL receptors [15] IFN

treatment might also inhibit the activity of

antiapop-totic mechanisms that counteract the death-inducing

effects of TNF family members [19] However, we have

not observed any consistent IFN-induced changes in

the levels of TRAIL receptor proteins or the large or

small forms of the caspase-8 antagonist protein c-FLIP (I W Jeffrey, unpublished results)

Exactly how the levels of phosphorylation of eIF2a

or 4E-BP1 are regulated by caspase activity remains to

be determined In the case of eIF2a, there is a preced-ent for caspase-induced cleavage and activation of PKR [46] This enzyme is present in both MCF-7 and HeLa cells, and its level is enhanced by IFN treatment (I W Jeffrey, unpublished results) As a basis for the dephosphorylation of 4E-BP1, there may be caspase-mediated inhibition of one or more protein kinases and⁄ or activation of protein phosphatase(s) such as PP2A that act on 4E-BP1 [47] A substantial body of evidence suggests involvement of protein phosphatases

in mediating the effects of apoptotic stimuli [48–50], but further work will be needed to determine whether regulation of these enzymes by TRAIL (via caspase-8)

is responsible for the changes in 4E-BP1 phosphoryla-tion identified here

Experimental procedures Materials

Materials for tissue culture were obtained from Sigma (Poole, UK) Monoclonal antibody against PARP (C2-10) was obtained from Trevigen (Gaithersburg, MD, USA) Antibodies against 4E-BP1 and a-tubulin were obtained from Santa Cruz Biotechnology (Santa Cruz, CA, USA) and Sigma, respectively Monoclonal antibodies to eIF2a and phosphorylated eIF2a (Ser51) were as previously des-cribed [2,51] Antibodies to phosphorylated 4E-BP1 (Ser65), caspase-8 and BID were obtained from Cell Signalling Technology (Beverley, MA, USA) PVDF paper (Hybond P) was obtained from GE Healthcare (Chalfont St Giles, UK) TRAIL was obtained from PeproTech EC (London, UK) and IFNa2b (Intron A) was obtained from

inhibitor zIETD.FMK was obtained from Calbiochem (Nottingham, UK) All other chemicals were from Sigma

Cell culture and cytokine treatments

The human breast cancer cell line MCF-7 was kindly provi-ded by R Ja¨nicke (University of Dusseldorf, Germany) These cells, as well as HeLa cells, were cultured under the conditions previously described [2] Both cell lines were treated with IFNa2b (1000 International reference unitsÆmL)1) for the times shown in the legends to Figs 1,3,4,5 and 6 No significant differences in the effects of IFN were noted between 24 h and 72 h of treatment Wild-type and caspase-8-deficient Jurkat cells were grown as previously described [28] For all cell lines TRAIL was added at the concentrations stated for the last 4–5 h of the incubations

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Cell growth and viability measurements

The cells were harvested by trypsinization, resuspended and

counted in a haemocytometer Cell viability was determined

by trypan blue exclusion Cells were fixed with ethanol,

stained with propidium iodide, treated with ribonuclease A

and analysed for DNA content and the appearance of a

sub-G1 fraction by fluorescence-activated cell sorting, as

described previously [29]

Determination of protein synthesis rates

Overall rates of protein synthesis in intact cells were

meas-ured by the incorporation of [35S]methionine (10 lCiÆmL)1)

into trichloroacetic acid-insoluble material for 40 min

Radioactivity was determined as previously described [2]

Protein content was determined and rates of protein

synthe-sis are expressed as counts per min incorporated per lg

protein

Immunoblotting of cell extracts

Cells were harvested, washed in NaCl⁄ Piand lysed as

des-cribed previously [2] Samples containing equal amounts of

protein were subjected to electrophoresis on SDS

polyacryl-amide gels and the proteins transferred to PVDF

mem-branes using a semidry blotting apparatus (Bio-Rad, Hemel

Hempstead, UK) Blots were blocked, incubated with the

appropriate primary antibodies and developed using

horse-radish peroxidase-linked secondary antibodies Enhanced

chemiluminescence was performed using Lumiglo reagent

(Cell Signaling Technology) according to the

manufac-turer’s instructions Quantitative densitometry of

appropri-ate bands was performed using Scion image software

(Scion Corporation, Frederick, MD)

Acknowledgements

We are grateful to Bill Newman for assistance with the

fluorescence-activated cell sorter analysis This work

was supported by grants from the Association for

International Cancer Research, the Leukaemia

Research Fund and the Cancer Prevention Research

Trust SB was funded by a fellowship from the

Fonda-tion pour la Recherche Me´dicale

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