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The calpain 1–a-actinin interactionResting complex between the calcium-dependant protease and its target in cytoskeleton Fabrice Raynaud1, Chantal Bonnal1, Eric Fernandez2, Laure Bremaud

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The calpain 1–a-actinin interaction

Resting complex between the calcium-dependant protease and its target

in cytoskeleton

Fabrice Raynaud1, Chantal Bonnal1, Eric Fernandez2, Laure Bremaud3, Martine Cerutti4,

Marie-Christine Lebart1, Claude Roustan1, Ahmed Ouali2and Yves Benyamin1

1 UMR 5539 – CNRS, laboratoire de Motilite´ Cellulaire – EPHE, cc107, USTL, Montpellier, France; 2 Stationde Recherches sur la Viande, INRA-Theix, St-Gene`s-Champanelle, France; 3 Institut ‘Sciences de la Vie et de la Sante´’, Genetique Moleculaire Animale,

UR 1061, INRA-Universite´ de Limoges, Faculte´ des Sciences, Limoges, France; 4 Laboratoire de Pathologie Compare´e,

INRA-CNRS URA5087, Saint Christol Le`s Ale`s, France

Calpain 1 behaviour toward cytoskeletal targets was

inves-tigated using two a-actinin isoforms from smooth and

skel-etal muscles These two isoforms which are, respectively,

sensitive and resistant to calpain cleavage, interact with the

protease when using invitro binding assays The stability

of the complexes in EGTA [Kd(–Ca2+)¼ 0.5 ± 0.1 lM]

was improved in the presence of 1 mM calcium ions

[Kd(+Ca2+)¼ 0.05 ± 0.01 lM] Location of the binding

structures shows that the C-terminal domain of a-actinin

and each calpain subunit, 28 and 80 kDa, participates in

the interaction In particular, the autolysed calpain form

(76/18) affords a similar binding compared to the 80/28

intact enzyme, with an identified binding site in the

cata-lytic subunit, located in the C-terminal region of the chain

(domain III–IV) The invivo colocalization of calpain 1

and a-actinin was shown to be likely in the presence of calcium, when permeabilized muscle fibres were supple-mented by exogenous calpain 1 and the presence of cal-pain 1 in Z-line cores was shown by gold-labelled antibodies The demonstration of such a colocalization was brought by coimmunoprecipitation experiments of calpain 1 and a-actinin from C2.7 myogenic cells We propose that calpain 1 interacts in a resting state with cytoskeletal targets, and that this binding is strengthened

in pathological conditions, such as ischaemia and dystro-phies, associated with high calcium concentrations Keywords: calpain; cytoskeleton; alpha-actinin; muscle; calcium

Calpain 1 (Calp1) and calpain 2 (Calp2) are intracellular

Ca2+-dependent thiol endoproteases [1], expressed

through-out the animal kingdom, and recently reported in the plant

kingdom [2] These two proteases are particularly implicated

[1] in the selective proteolysis of factors involved in the cell

cycle, in myocyte fusion, during apoptosis in association

with caspases or in the cleavage of membrane-cytoskeleton

complexes during cell motility phases [3] Many of the

substrates are transcription and signalling factors with

intracellular presence of less than 2 h [4] or cytoskeletal

proteins with long half-lives, generally specialized in the

cross-link or the membrane anchorage of fibrillar

components [5] The hypothesis according to which calpains would be released from complexes with calpastatin (its natural inhibitor) to join membrane phospholipids where protease activation is achieved was proposed [6], but the origin of recognition of specific substrates by calpains [7,8] remains unclear

A statistical analysis of the presence of PEST sequences

in the target, critical for calpain recognition [9,10], gives valuable scores with short half-life proteins, but is not appropriate in the case of several cytoskeletal actin-binding proteins [1] For example, filamin, dystrophin and talin are known to be cleaved invivo by calpains It should be noted that the accessibility of the calmodulin (CaM)-binding domain in PEST sequences is an important factor to consider [11], as demonstrated for IjBa, a CaM and calpain-binding protein [12] Moreover, we have shown recently in muscle fibres [13] the presence of a stable

Ca2+-regulated complexbetween E64-treated Calp1 and the N-terminal region of the titin located between the Z-band and the N2-line in the I-band of myofibrils This titin region, rich in PEST sequences, was reported to show a marked calcium binding ability related to acidic sequences [14] In the absence of Ca2+ions, a weak interaction between the

Ca2+-binding titin fragments and Calp1 was observed

On the other hand, several other calpain substrates deprived of PEST sequences but containing calmodulin-binding domains [15] or EF-hand sequences [16] were

Correspondence to Y Benyamin, UMR 5539, laboratoire de Motilite´

Cellulaire – EPHE, Bt 24, cc107, USTL, place E Bataillon F-34095

Montpellier cedex5, France.

Fax: + 33 4 67144927, Tel.: + 33 4 67143813,

E-mail: benyamin@univ-montp2.fr

Abbreviations: ask, skeletal muscle a-actinin; asm, smooth muscle

a-actinin; Calp1, calpain 1 (l-calpain); Calp2, calpain 2 (m-calpain);

CaM, calmodulin; ELISA, enzyme-linked immunosorbant assay;

FITC, fluorescein 5-isothiocyanate; Seph-ask, Sepharose-insolubilized

skeletal muscle a-actinin.

Note: web pages are available at http://www.dbs.univ-montp2.fr/

umr5539/, http://www.ephe.univ-montp2.fr/

(Received 29 July 2003, accepted 30 September 2003)

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reported It was thus suggested that the calpain domains IV

and VI, which have a CaM-like structure and are members

of the penta-EF-hand family of proteins [1], could be the

binding structures of interfaces with cytoskeleton

compo-nents [17] and contribute to link the two subunits in calpains

[18] Indeed, the two subunits of 80 kDa (domains I–IV)

and 30 kDa (domains V–VI), contain altogether 10–11

putative EF-hands motifs in domains IV, VI and II

[1,19,20], from which five to sixare estimated to be

functional A negatively charged loop of domain III also

offers Ca2+ binding capacity [21,22], which maximizes

binding to eight equivalents of Ca2+in agreement with a

previous invitro evaluation [23] Domain III, which includes

binding sites for calpastatin and phospholipids [1,18],

appears as the regulation centre between the CaM-like

domains IV and VI and the catalytic domain II, which is in

interaction with domain III through Ca2+-regulated salt

bridges [20] Thus, according to a previous hypothesis, the

interaction between a PEST sequence, a CaM-binding

domain, or a Ca2+-binding motif and a CaM-like domain,

would place the catalytic site of calpain in close proximity to

the substrate

To test this hypothesis, we have investigated Calp1

interaction with two a-actinin isoforms, either resistant or

sensitive to calpain 1 proteolysis, purified from chicken

skeletal and smooth muscles, respectively The a-actinin

family displays two EF-hand motifs in the C-terminal

domain [24], presents low PEST scores after analysis, and

several isoforms are calpain substrates [16,25–27] Our study

of calpain 1–a-actinin interaction suggests the importance

of calmodulin-like domains and EF-hand motifs Finally, it

allows dissociation of two aspects in the protease behaviour

toward its target, binding and cleavage, in relation to the

presence of Ca2+ions

Materials and methods

Proteins

Bovine Calp1 (80/30) was isolated [28] from the bovine

skeletal Rectus abdominus muscle, excised within 1 h

post-stunning (INRA slaughterhouse, Clermont-Fd, France)

Smooth (asm) and skeletal (ask) muscle a-actinins were

purified from chicken gizzard and breast muscles,

respect-ively, obtained immediately after killing (Avigar

slaughter-house, Gard, France) Purification procedures were

described previously [29,30]

Human (887 b) cDNA (calpain 28 kDa regulatory

subunit) was expressed as C-terminal His-tagged protein

in the pET16b vector (Roche Diagnostics) The construct

was transformed into competent BL21(DE3) Escherichia

coli Expression was induced by adding 1 mM isopropyl

thio-b-D-galactoside for 3 h at 37C Slurry Ni/NTA were

added to supernatant after bacteria lysis and gently mixed

for 30 min Solid phase was packed in a column before

washing twice with the lysis buffer, adjusted to 20 mM

imidazole, pH 8, and the elution performed with the same

buffer adjusted to 250 mMimidazole Eluted fractions were

analysed by SDS/PAGE and Coomassie blue staining

Human 80 kDa catalytic subunit (microcalpain) was

expressed [31] in Spodoptra frugiperda (SF9) cells using a

recombinant 80 kDa subunit baculovirus Sf9 cell pellets

were lysed in 100 mM NaCl, 2 mM EGTA, 0.1% (v/v) Triton X-100, 20 mMTris/HCl, pH 7.5 buffer, supplemen-ted with antiproteases cocktail (Roche) and cleared at

23 000 g for 15 min Supernatant was incubated (4C,

60 min) with 800 lg of anti-Calp1 Ig (a purified low affinity antibody subfraction [32]), then supplemented with Seph-arose-protein A (Pharmacia, Uppsala, Sweden) and gently mixed for 60 min Solid phase was washed four times with the lysis buffer, before a batch elution with 0.6MKI, 2 mM dithiothreitol, 20 mMTris/HCl, pH 7.5 and dialysis against the interaction buffer

Proteolysis and protein modifications Calp1 autolysis was conducted [1,20,33] during 10 min at

20C in 1 mMCaCl2, 20 mMTris/HCl buffer, pH 7.5, to obtain the autolysed form (76/18) or during 120 min in the same buffer at 20C to conduct a more complete degra-dation Autolysis kinetics were followed by SDS/PAGE and stopped (2 mMEGTA) after an optimal incubation time Skeletal a-actinin cleavage was performed [30] with thermolysin (1 : 25 enzyme/substrate, w/w) The 30, 55 and 10 kDa domains issued from the cleavage were purified

on a PorosHQ/H (Boehringer, Manheim) FPLC column using the procedure previously described with fish ask ask and asm (1 mgÆmL)1) were treated in 1 mMCaCl2, 1 mM dithiothreitol, 50 mMKCl, 20 mMTris/HCl buffer, pH 7.5

by Calp1 during 2 h at 20C using a protease/substrate ratio of 1 : 10 (w/w) [1,25,30] Proteolysis was stopped by

2 mM EGTA, and the residual Calp1 discarded by the FPLC procedure Sepharose-insolubilized skeletal muscle a-actinin (Seph-ask) was obtained (1 mg proteinÆmL)1gel) with BrCN-activated Sepharose 4B (Pharmacia)

Protein labelling was performed with biotin succinimide ester [34] or fluorescein isothiocyanate (FITC) [35] Biotin-amidocaproate N-hydroxysuccinimide ester, E64 calpain inhibitor and fluorescein isothiocyanate were purchased from Sigma Chemical Co Thermolysin was from Serva (Heidelberg, Germany)

Antibody specificities The anti-Calp1 and anti-Calp1,2 Igs are directed against a specific sequence (539–553 in domain IV) and a conserved sequence (330–344 in the subdomain IIb) of the unprocessed

80 kDa subunit (SwissProt, ID number P07384), respect-ively Sequences were chosen according to their accessibility and helicoidal content criteria before synthesis and coupling

to hemocyanin using glutaraldehyde [36] Rabbit anti-(a-actinin) Igs cross-reacting with ask and asm [30] were fractionated with the 30 kDa, 55 kDa and 10 kDa Seph-arose 4B-insolubilized fragments, issued from ask thermo-lysin cleavage Anti-rabbit IgG conjugated with alkaline phosphatase was obtained from Biosys (Compiegne, France) Monoclonal (His)6antibody was from Qiagen Binding analysis

ELISA was performed [29] in microtitration plates (Poly-sorp, Nalgen Nunc International, Denmark) Incubation steps were carried out at 20C in 150 mM NaCl, 0.5% gelatine, 3% gelatine hydrolysate, 0.05% Tween 20, 20 m

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Tris/HCl buffer, pH 7.4 Each assay monitored at 405 nm

was conducted in triplicate and the mean value was plotted

after subtraction of nonspecific absorption

In spectrofluorescence experiments, interactions of the

fluorescein labelled Calp1 were performed at 20C in

50 mM KCl, 20 mM Tris/HCl buffer, pH 7.4, using a

Perkin-Elmer luminescence spectrometer LS 50 The

exci-tation was set at 494 nm and the emission spectrum

recorded between 510 and 550 nm Fluorescence changes

were deduced from the area of emission spectra [35]

ELISA and fluorescence binding assays were conducted

in the presence of 1 mM EGTA or 1 mM CaCl2

supple-mented with 10 lME64 to saturate all Ca2+binding sites,

including the non EF-hand ones [21,22,37] and avoid

proteolytic processes The parameters Kd(apparent

disso-ciation constant) and Amax(maximum effect) were obtained

(CURVEFIT software developed by K Raner Software,

Mount Waverley, Victoria, Australia) by nonlinear least

squares fitting of the experimental data points to the

following equation

A¼ Amax ½L=ðKdþ ½LÞ

where A is the measured effect and [L] is the ligand

concentration

Cell culture

C2.7 myoblasts derived from the C2 mouse myogenic cell

line [38] were cultured in DMEM (Gibco-BRL/Life

Tech-nology) supplemented with 2 mMglutamax(Gibco-BRL),

100 lgÆmL)1penicillin, 100 lgÆmL)1streptomycin

(Gibco-BRL), and 20% fetal bovine serum (Gibco-BRL) Cells in

proliferation (confluence stage) were lysed in 0.1% Triton

X-100, 150 mMNaCl, 2 mMEGTA, antiprotease cocktail

(Roche), 20 mMTris/HCl buffer (lysis buffer), then

centri-fuged

Protein cosedimentation and immunoprecipitation

Cosedimentations were performed at 20C using 2.5 lg of

Calp1 (80 kDa/28 kDa) mixed with 2.5 lg of the 10 min

autolysed form (76 kDa/18 kDa), 10 lg of the 120 min

autolysed form or 10 lg of the calpain 28 kDa subunit,

incubated with 50 lg of insolubilized Seph-ask in 200 lL of

50 mMTris/HCl pH 7.4 buffer supplemented with 150 mM

NaCl, 1 mM EGTA, 0.1% NP-40, and 0.25% gelatine

After 60-min incubation, the solid phase was washed four

times with 50 mM Tris/HCl, pH 7.4, 1 mMEGTA, 0.1%

NP-40 and resuspended in 60 lL of Laemmli loading

buffer Thirty microlitres of the suspension were analysed by

SDS/PAGE and Western blotting

The C2.7 line cell lysate supernatant obtained from 107

cells was incubated for 1 h at room temperature with 50 lg

of anti-Calp1 Ig, then with insolubilized Sepharose-protein

A (Sigma) in lysis buffer supplemented by 1% bovine serum

albumin After extensive washing in lysis buffer, the solid

phase was treated at 100C in Laemmli buffer A control

assay in the same conditions, but without anti-Calp1 Ig, was

performed

Electrophoresis (SDS/PAGE) was made [39] using 7.5%

resolving gels and stained with Coomassie blue or silver

Molecular mass standards were from Bio-Rad and

Phar-macia Western blotting [40] was performed using the appropriate antibody

Calp1 enrichment of permeabilized muscle fibres Glycerinated fibres were obtained as previously reported [25] Briefly, small fibre bundles (1· 5 mm) taken from freshly excised bovine longissiumus muscle, were stretched between two pins and immersed in 30 mM Tris/HCl,

pH 7.5, containing 50% glycerol, 5 mM EDTA and anti-proteases cocktail during 5 h, diced into small pieces (0.8· 0.2 mm), and maintained in the same solution for

18 h, before extensive washing in 200 mMKCl, antiprotease cocktail (Roche), 30 mM Tris/HCl pH 7.5, to flush out endogenous calpains and calpastatin complexes (Western blotting controls) Samples were then incubated under continuous mild stirring, with Calp1 (0.5 mgÆmL)1) in

30 mM Tris/HCl pH 7.5 containing 5 mM dithiothreitol,

2 mM EGTA or in 30 mM Tris/HCl, pH 7.5, containing

5 mMdithiothreitol, 1 mMCaCl2, and 10 lME64 for 1 h at room temperature Exogenous Calp1 added to permeabi-lized fibres was located using the postembedding procedure [41,42] performed with a gold (10 nm)-labelled secondary antibody (Sigma) diluted to 1 : 50

Results

Interaction of Calp1 with skeletal and smooth muscle a-actinins

Specificity of the antibodies directed against the specific sequence 539–553 in subdomain IV (anti-Calp1) and the conserved (Calp1 and Calp2) sequence 330–344 in subdo-main II (anti-Calp1,2) was assessed (Fig 1A) by Western blotting using bovine skeletal muscle crude extract and the purified Calp1 Calp1 in muscle fibre extract appears as a unique band at the 80 kDa level (Fig 1Ab,e) In particular,

no cross-reactivity of anti-Calp1 was detected toward the purified Calp2 (not shown) or Calp3 (p94) in extract (Fig 1A,b) As expected, anti-Calp1,2 was able to detect both Calp1 (Fig 1A,f) and Calp2 (not shown)

Chicken a-actinins extracted from skeletal muscle (ask) and gizzard (asm) were assayed as substrates of Calp1 As shown in Fig 1B, upon Calp1 treatment in the presence of

1 mMCaCl2, asm is deprived of a segment of about 5 kDa

in contrast to the ask isoform which resists to proteolysis The asm 95 kDa truncated protein did not react with the antibody directed against the C-terminal 10 kDa fragment

of a-actinin [25,30], indicating that the deleted segment is located at the C-terminal extremity (not shown) Similar calpain proteolysis was previously reported for fish a-actinin [25,30,43] and for nonmuscle isoforms [16] in contrast to porcine, bovine or rabbit skeletal muscles isoforms [44,45] which resist

Using two independent methods, interaction of a-actinins with Calp1 was investigated In solid phase assay (ELISA),

we observed that ask binds to coated Calp1 in the absence

of Ca2+ions with a significant affinity (Fig 2A) Apparent dissociation constant [Kd(–Ca2+)], calculated from five experiments performed in the presence of 1 mM EGTA, corresponds to 0.5 ± 0.1 lM A similar affinity (0.3 ± 0.1 l ) was observed when ask was immobilized instead of

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Calp1 (Fig 2A, inset) An equivalent result was obtained

with asm [Kd(– Ca2+)]¼ 1.0 ± 0.4 lM), except that the

95 kDa fragment generated after Calp1 cleavage did not

bind calpain (Fig 2B) These experiments were confirmed

using fluorescent assays in which increasing amounts of ask

were added to FITC-labelled Calp1 (Fig 2C) When the

interaction was conducted in the presence of 1 mMcalcium

(and E64 as calpain inhibitor), a tenfold increase in affinity

[K ¼ 0.05 ± 0.01 lM] was observed (Fig 2C,

Fig 1 Protein patterns (A) Specificity of the anticalpain 1 antibodies.

Bovine skeletal muscle extract (a,b), purified bovine Calp1 (c,e), and

10-min autolysed Calp1 (d) were stained by Coomassie blue (a), by

silver (c,d) or tested by Western blotting (b,e,f) using anti-Calp1 (b,e)

and anti-Calp1,2 (f) Igs (B) Proteolysis of smooth muscle a-actinin (a)

cleaved by Calp1 and revealed by anti-(a-actinin) after 30 min (b) and

120 min (c) The arrowhead points to the 95 kDa proteolysis product,

and the arrow indicates the position of the rabbit muscle

phosphory-lase B (97 kDa) (C), Western blotting of skeletal a-actinin (a) cleaved

by thermolysin (b) and the FPLC purified C-terminal 10 kDa

frag-ment (c) using anti-(a-actinin).

Fig 2 a-Actinin–Calp1 interactions (A) Solid phase immunoassay (ELISA) between coated Calp1 (j) or coated 10 min-autolysed Calp1 (h) and increasing ask concentrations or between coated ask and increasing Calp1 concentrations (inset) Binding was monitored at

405 nm using biotin-labelled proteins (ask or Calp1) and streptavidin– alkaline phosphatase-labelled (1 : 2000 diluted) (B) Solid phase immunoassay (ELISA) between coated Calp1 and increasing amounts

of intact asm (s) or the 95 kDa cleaved asm (d) The experimental conditions were those described in (A) (C) Decrease in the fluores-cence (DF) of FITC–Calp1 (1 lgÆmL)1) in interaction with increasing concentrations of ask in the presence of 1 m M EGTA or 1 m M CaCl 2

(inset).

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inset) in comparison to the binding [Kd(–Ca2+)¼

0.5 ± 0.1 lM] obtained in the absence of calcium A similar

calcium effect [Kd(+Ca2+)¼ 0.2 ± 0.04 lM; Kd(–Ca2+)¼

1 ± 0.2 lM] was observed with asm (not shown)

In conclusion, ask and ask isoforms are able to bind

Calp1 in the absence and in the presence of calcium, with an

important increase in the affinity in the presence of calcium

Furthermore, the cleavage of asm by calpain 1 generates a

fragment of 95 kDa which is unable to interact with Calp1

This indicates the presence of a calpain binding site in the

C-terminal domain of smooth muscle a-actinin

Involvement of the C-terminal domain of ask

in Calp1 binding

In order to locate the region responsible for the binding of

Calp1 on ask isoform, which is not sensitive to calpain

cleavage, we tested the three fragments issued from the

proteolysis of ask by thermolysin (Fig 1Ca,b): the 30

(N-terminal actin binding domain), the 60 (spectrin-like

repeats, central domain), and the 10 kDa (C-terminal

EF-hand domain) In solid phase assay, we observed

(Fig 3A) that the purified 10 kDa fragment (Fig 1Cc)

was the only one to bind Calp1 with a detectable affinity

We confirmed this result using fluorescent assays (Fig 3B)

and found a higher affinity in the presence of calcium

[Kd(+Ca2+)¼ 1.0 ±0.1 lM] in comparison with its absence

[Kd(–Ca2+)¼ 2.5 ±0.3 lM] Thus, a Calp1 binding site is

included in the C-terminal domain of the ask molecule,

and this binding is independent of the susceptibility of the

a-actinin isoform to calpain proteolysis

Identification of the calpain 1 subunit implicated

in a-actinin interaction

The regulatory (28 kDa) and the catalytic (80 kDa)

sub-units, expressed as recombinant proteins, were assayed for

binding activity toward skeletal muscle a-actinin We

observed (Fig 4) that in the presence of 1 mM Ca2+the

two subunits interact with ask, the catalytic 80 kDa subunit

having a better affinity [Kd(+Ca2+)¼ 0.5 ± 0.1 lM] than

the regulatory 28 kDa chain [Kd(+Ca2+)¼ 1.4 ± 0.2 lM]

In the absence of calcium (1 mM EGTA), the 28 kDa

subunit interaction is very weak [Kd(–Ca2+)> 10 lM] in

contrast to that of the 80 kDa chain Binding between the

28 kDa subunit and ask in the presence of calcium, was

confirmed [Kd(+Ca2+)¼ 2.5 ± 0.5 lM) using fluorescence

assays (not shown) and cosedimentation experiments using

Seph-ask (Fig 5A)

Similarly, we have shown that the intact (80 kDa/

28 kDa) calpain 1 (Fig 1A) and the 10-min autolysed

(76 kDa/18 kDa) form (Fig 1Ad) have the same binding

ability toward ask in the absence of calcium (Figs 2A and

5B, 10 min) as in its presence (not shown) Furthermore, the

76, 50 and 30 kDa fragments issued from the 120 min

autolysis of Calp1, and recognized by anti-Calp1 (Fig 5Ba,

120 min), cosedimented with ask (Fig 5Bb, 120 min) It

can be observed (Fig 5Bb,c, 120 min) that only the 76 kDa

fragment is recognized by Calp1 (domain IV) and

anti-Calp1,2 (domain II), which locates the 50 kDa and the

30 kDa fragments in the C-terminal region (domains

III–IV) of the catalytic subunit

Thus, the 28 kDa subunit (probably its C-terminal

18 kDa region) in a calcium-dependent fashion, and the C-terminal part (domains III–IV) of the 80 kDa subunit, are implicated in the interface linking calpain 1 to skeletal muscle a-actinin

Colocalization of microcalpain and a-actinin

in myogenic cells Calpains and a-actinin were previously located in Z-disks [44], and adhesion structures [5], without evidence of strong molecular proximity To confirm that the a-actinin–Calp1 interaction was physiologically relevant, we first performed coimmunoprecipitation studies As shown in Fig 5C, a-actinin was coprecipitated with calpain 1 from a cell

Fig 3 Interactions of ask domains with Calp1 (A) Solid phase immunoassay (ELISA) between coated 30 (u), 60 (j) and 10 kDa (s) ask fragments and increasing amounts of biotin-labelled Calp1 Binding was determined at 405 nm using streptavidin–alkaline phosphatase labelling (1 : 2000) (B) Fluorescence decrease (DF) of FITC-labelled Calp1 (1 lgÆmL)1) in interaction with increasing concentrations of the 10 kDa fragment in the presence of 1 m M CaCl 2

(s) or 1 m M EGTA (d) Glutathione S-transferase (Sigma) was used

as a negative control (j) of the interaction.

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lysate issued from C2.7 myoblasts, by using rabbit

anti-Calp1 Ig and insolubilized protein A Furthermore,

after incubation of permeabilized muscle fibres with

exogenous Calp1 in the presence of 1 mMCa2+ions, we

observed that calpain 1 was strikingly concentrated in the

Z-disk core (Fig 6) in comparison with the A- or M-bands

When calcium was omitted, we were unable to detect a

preferential location of exogenous Calp1 in myofibrils

Thus, Ca2+ions seem to favour the targeting of Calp1 to

Z-line and the interaction of the protease with the

compo-nents of this anchorage structure However, in the case of

C2.7 cells, coimmunoprecipitation of a-actinin by the

anti-Calp1 Ig was also observed in the absence of Ca2+ions,

which is likely considering the invitro binding analysis

Discussion

We have investigated the hypothesis, according to which

calpain 1, as calpain 3 (p94) with titin and glial filaments

[46,47], could bind directly to targets in cytoskeleton

through specific and stable interactions This hypothesis

involves questions related to the origin of interactions

[9,10,12,27] with the targets, the stability of complexes in the

resting stage [3,48] and the activation state [7,33] of the

binding calpain The topology of the interface with respect

to the catalytic domain II [1] and the cleavage site in target

are also underlying

Two muscle a-actinin isoforms (ask and asm) with

different calpain cleavage susceptibilities were chosen as

targets and their binding with calpain 1 analysed by

independent invitro and invivo approaches According to

the presented results, Calp1–a-actinin interaction is

inde-pendent of the cleavage susceptibility of the target and

occurred in the absence of calcium, but is improved in its

presence In the absence of calcium, the apparent dissociation

constant of Calp1–ask (or asm) complexes is measured in the micromolar order and decreased to the submicromolar level

in the presence of 1 mMCa2+and E64 The autolysed Calp1 (76/18) form and the intact enzyme (80/28) afforded the same binding ability toward a-actinin

In the experiments performed in the presence of 1 mM calcium, Calp1 was used at 1 lgÆmL (coated or FITC-protein) supplemented with 10 lME64 to avoid its auto-proteolysis and its aggregation [37] In fact, the affinity increase in the presence of Ca2+ions, was observed from

50 lM CaCl2, and the effect increased with increasing calcium concentration Thus, the conformation changes

Fig 4 Calp1 subunits binding assays Solid phase immunoassay

(ELISA) between the 30 (s,d) and the 80 kDa (h,j)-coated Calp1

subunits and biotin-labelled ask in the presence of 1 m M CaCl 2 (open

symbols) or 1 m M EGTA (filled symbols) Binding was determined at

405 nm using streptavidin–alkaline phosphatase labelling (1 : 2000).

Fig 5 Cosedimentation of calpain–a-actinin complexes (A) Cosedi-mentation with Seph-ask of His-tagged 30 kDa subunit (a), in the presence of 1 m M CaCl 2 (b) or 1 m M EGTA (c) Suspensions were centrifuged at 2000 g and the pellet revealed after SDS/PAGE by Western blotting using anti-His 6 Ig (1 : 1000 diluted) (B), cosedi-mentation of the 10 min autolysed Calp1 supplemented by the intact Calp1 (left part, lane a) or the 120 min autolysed Calp1 (right part, lane a) incubated in 1 m M EGTA with Seph-ask (see Materials and methods) Pellets (lanes b) are revealed after SDS/PAGE with Coo-massie blue (left part) or by Western blotting using anticalpain anti-bodies (right part, lanes b and c) A negative control (c) using inert Sepharose was included (left part) Anti-Calp1 (lane a,b) and anti-Calp1,2 (lane c) were used (right part) (C) Coimmunoprecipitation of Calp1–ask complexes from C2.7 lysate by anti-Calp1 and Sepharose-protein A The presence of ask in the pellet was searched in the assay (a) and in the control performed without the anti-Calp1 (b), after SDS/ PAGE and Western blotting, using anti-(a-actinin).

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induced by the saturation of low affinity Ca2+-binding sites,

changes mainly localized at level of the 28 kDa subunit [37],

and the exposure of hydrophobic patches on the surface of

the protease which aggregates calpain 1 molecules [37],

could lead to a sticky interaction with a-actinin

Neverthe-less, the fact that efficient calcium concentrations (from

50 lM) are higher than the physiological ones, may be

considered in view of several pathological situations such as

brain and muscle ischemia [49,50], or several muscle

dystrophies [1], but also during necrosis [51], apoptosis

[52], or myoblast fusion [53] where Ca2+ions concentration

increases in unknown proportions In these cases, the

accumulation of calpain 1 on cytoskeleton could explain

the rapid intervention of the protease and the quick

Ca2+-dependent degradation of several cytoskeletal

proteins [25,51]

Binding interface between Calp 1 and ask was further

located in this study Calpain binding structures were found

within the 10 kDa C-terminal domain of the a-actinin

molecule The inability of the 95 kDa chain (issued from the

cleavage of asm by Calp1) to interact with calpain 1, could restrict the location of the binding elements to the last

5 kDa, although we cannot rule out the possibility of conformational changes induced to the 95 kDa by the cleavage We can thus conclude that calpain 1 displays two distinct behaviours, one consisting of interaction with its target and the other being responsible for the proper cleavage action of the target

The attempt to locate the binding structures on Calp1 implied disposal of the two 28 and 80 kDa isolated subunits

in the correct conformation, which was effective by using

E coli [54] and SF9-Bacculo virus [55] as ex pression systems, respectively We have concluded that both subunits display binding abilities, although the regulatory subunit (28 kDa) is strongly controlled by calcium which binds to the CaM-like domain VI Concerning the catalytic subunit (80 kDa), the restriction was brought by cosedimentation assays to the 50 kDa C-terminal part, bearing domains III and IV Thus, the ability of the two isolated subunits or the autoproteolysed Calp1 products (18/76 and 55 kDa) to interact with ask indicates that the domains III–IV and

VI participate to the interface with the C-terminal region of a-actinin These domains concentrate 10 EF-hand motifs and an acidic Ca2+binding sequence [1,20,21]

It is noteworthy that the location of a Calp1 binding site in the C-terminal region of a-actinin [56] situates the protease in the vicinity of titin [57] and CapZ [34], two proteins described

as a-actinin partners in the Z-line and known as calpain substrates [1,25,34] In this context, according to our experimentation of enrichment of permeabilized fibres by exogenous Calp1 on Z-line, one could hypothesize that the two myofibrillar proteins could also bind Calp1, as a-actinin does Note that these three proteins strongly participate in the Z-disk organization, a compartment rapidly proteolysed during muscle ischemia [25,45] or after a calpain treatment of isolated myofibrils [25] Targeting of Z-disk by calpains was previously suggested [25,44,48] and a quick ask release from muscles treated by calpains in the presence of calcium was observed Furthermore, a-actinin is also located in cellular adhesion structures [5], in a colocation with integrin, talin and vinculin [56,58] Immunoprecipitation of a-actinin from C2.7 lysate by anti-Calp1 proves the association of the protease with a-actinin, either in direct contact or in a complexincluding the two proteins

In conclusion, our study proves the interaction between a-actinin and calpain 1 and locates binding motifs within regions where the EF-hand domains of the protease and the cytoskeletal protein are concentrated The behaviour of calpain 1 toward cytoskeletal targets appears dual In its first state, the protease would oscillate between cytoskeleton components, calpastatin and phospholipids in membrane according to the local calcium concentrations This would eventually lead to the cleavage of close substrates in cytoskeleton This equilibrium is currently under investiga-tion by using C2.7 cell line transfecinvestiga-tion assays with calpain 1 CaM-like subdomains

Acknowledgements

This work was supported by grants from the Association Franc¸aise contre les Myopathies (AFM) and PPF network (EPHE) Authors are grateful to Professor H Sorimachi for the calpain 1 constructs gift.

Fig 6 Muscle fibres treatment by inactivated Calp1 Permeabilized

muscle fibres were enriched with exogenous Calp1 in the presence of

either 1 m M Ca 2+ ions (A) or 2 m M EGTA (B) during 1 h, stained

with anti-Calp1, then with a gold-labelled secondary anti-rabbit IgG.

Z, Z-band; M, M-band; A, A-band.

Trang 8

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