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Tiêu đề Autolytic activity of human calpain 7 is enhanced by ESCRT-III-related protein IST1 through MIT–MIM interaction
Tác giả Yohei Osako, Yuki Maemoto, Ryohei Tanaka, Hironori Suzuki, Hideki Shibata, Masatoshi Maki
Trường học Nagoya University, Graduate School of Bioagricultural Sciences, Department of Applied Molecular Biosciences
Chuyên ngành Applied Molecular Biosciences
Thể loại Research article
Năm xuất bản 2010
Thành phố Nagoya
Định dạng
Số trang 15
Dung lượng 786,21 KB

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We found that glutathione-S-transferase GST-fused tandem MIT domains of calpain 7 calpain 7MIT pulled down FLAG-tagged IST1 expressed in HEK293T cells.. GST-fused calpain7MIT 1–165 amino

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ESCRT-III-related protein IST1 through MIT–MIM

interaction

Yohei Osako, Yuki Maemoto, Ryohei Tanaka, Hironori Suzuki, Hideki Shibata and Masatoshi Maki Department of Applied Molecular Biosciences, Graduate School of Bioagricultural Sciences, Nagoya University, Japan

Keywords

calpain 7; ESCRT-III; IST1;

microtubule-interacting and transport (MIT); proteolysis

Correspondence

M Maki, Department of Applied Molecular

Biosciences, Graduate School of

Bioagricultural Sciences, Nagoya University,

Furo-cho, Chikusa-ku, Nagoya 464-8601,

Japan

Fax: +81 52 789 5542

Tel: +81 52 789 4088

E-mail: mmaki@agr.nagoya-u.ac.jp

(Received 10 May 2010, revised 21 July

2010, accepted 20 August 2010)

doi:10.1111/j.1742-4658.2010.07822.x

Calpain 7, a mammalian ortholog of yeast Cpl1⁄ Rim13 and fungal PalB, is

an atypical calpain that lacks a penta-EF-hand domain Previously, we reported that a region containing a tandem repeat of microtubule-interact-ing and transport (MIT) domains in calpain 7 interacts with a subset of endosomal sorting complex required for transport (ESCRT)-III-related proteins, suggesting involvement of calpain 7 in the ESCRT system Although yeast and fungal calpains are thought to be involved in alkaline adaptation via limited proteolysis of specific transcription factors, proteo-lytic activity of calpain 7 has not been demonstrated yet In this study, we investigated the interaction between calpain 7 and a newly reported ESC-RT-III family member, increased sodium tolerance-1 (IST1), which pos-sesses two different types of MIT-interacting motifs (MIM1 and MIM2)

We found that glutathione-S-transferase (GST)-fused tandem MIT domains of calpain 7 (calpain 7MIT) pulled down FLAG-tagged IST1 expressed in HEK293T cells Coimmunoprecipitation assays with various deletion or point mutants of epitope-tagged calpain 7 and IST1 revealed that both repetitive MIT domains and MIMs are required for efficient interaction Direct MIT–MIM binding was confirmed by a pulldown exper-iment with GST-fused IST1 MIM and purified recombinant calpain 7MIT Furthermore, we found that the GST–MIM protein enhances the autolysis

of purified Strep-tagged monomeric green fluorescent protein (mGFP)-fused calpain 7 (mGFP–calpain 7–Strep) The autolysis was almost com-pletely abolished by 10 mm N-ethylmaleimide but only partially inhibited

by 1 mm leupeptin or E-64 The putative catalytic Cys290-substituted mutant (mGFP–calpain 7C290S–Strep) showed no autolytic activity These results demonstrate for the first time that human calpain 7 is proteolytically active, and imply that calpain 7 is activated in the ESCRT system

Structured digital abstract

l MINT-7990193 , MINT-7990213 , MINT-7990233 : calpain 7 (uniprotkb: Q9Y6W3 ) physically interacts ( MI:0915 ) with IST1 (uniprotkb: P53990 ) by anti tag coimmunoprecipitation ( MI:0007 )

l MINT-7990176 : calpain 7 (uniprotkb: Q9Y6W3 ) physically interacts ( MI:0915 ) with IST1 (uniprotkb: P53990 ) by pull down ( MI:0096 )

l MINT-7990252 : IST1 (uniprotkb: P53990 ) binds ( MI:0407 ) to calpain 7 (uniprotkb: Q9Y6W3 )

by pull down ( MI:0096 )

Abbreviations

ALLNal, N-acetyl- L -leucyl- L -leucyl- L -norleucinal; CBB, Coomassie Brilliant Blue R-250; CHMP, charged multivesicular body protein; CSD1, calpastatin domain 1; ESCRT, endosomal sorting complex required for transport; GFP, green fluorescent protein; GST, glutathione-S-transferase; IST1, increased sodium tolerance-1; mGFP, monomeric green fluorescent protein; MIM, microtubule-interacting and transport-interacting motif; MIT, microtubule-interacting and transport; pAb, polyclonal antibody; VPS, vacuolar protein sorting; WB, western blot.

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Calpains are a family of intracellular Ca2+-dependent

cysteine proteases [1–3] Well-studied typical

mamma-lian calpains (l-calpain and m-calpain) are composed

of a catalytic large subunit and a regulatory small

sub-unit Both subunits have C-terminal penta-EF-hand

domains [4], which contribute to activation of the

pro-tease by Ca2+ binding, to heterodimerization of each

subunit, and to binding of the endogenous calpain

inhibitor calpastatin [5,6] Although the detailed

molecular mechanisms are still unknown, ubiquitously

expressed calpains, represented by l-calpain and

m-cal-pain, have been suggested to be involved in

fundamen-tal biological phenomena such as regulation of the cell

cycle and signal transduction [1,3,7–9] On the other

hand, tissue-specific calpains, such as p94⁄ calpain 3

and nCL-2⁄ calpain 8, have been suggested to have

spe-cific roles [10–12]

As the mRNA of calpain 7 is expressed ubiquitously

in human tissues, calpain 7 is expected to have

fundamental and essential roles in mammalian cells [13] Studies on calpain 7 have been preceded by those on yeast and fungal orthologs (Cpl1⁄ Rim13 and PalB, respectively), and accumulating data indicate that Cpl1 and PalB play critical roles in alkaline adaptation via processing of transcription factors Rim101⁄ PacC [14– 18] However, the functions of mammalian calpain 7 are still unknown It has not even yet been demonstrated whether calpain 7 has protease activity, and neither

in vivo nor in vitro substrates have been identified Although calpain 7 contains a C2-like domain, it lacks a penta-EF-hand domain and is classified as an atypical calpain As one of the significant structural features, mammalian calpain 7 possesses a tandem repeat of microtubule-interacting and transport (MIT) domains [19,20] at the N-terminus (Fig 1A) Several MIT domain-containing proteins have been shown to bind endosomal sorting complex required for transport (ESCRT)-III proteins and their related proteins [21–23]

Fig 1 Schematic representations of

calpain 7 and IST1 (A) Calpain 7 possesses

two MIT domains (MITa and MITb) at its

N-terminus, a calpain-like cysteine protease

domain (Cys290, a putative catalytic Cys) in

the middle, and a C2-like domain at its

C-ter-minus Catalytic triad residues are indicated

by closed triangles (B) IST1 has a

CHMP-like domain in its N-terminal half, a Pro-rich

linker in the middle, and two different types

of MIMs (from the N-terminal side, MIM2

and MIM1, respectively) at the C-terminus.

Amino acids that are important for binding

to the VPS4 MIT domain are indicated by

open triangles Wild-type (WT) as well as

deletion and amino acid substituted mutants

of calpain 7 and IST1 used in this study are

schematically represented The numbers

below the bars indicate positions in amino

acid residues.

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The ESCRT system was originally identified as

machinery contributing to multivesicular endosome

(multivesicular body) formation in the endocytic

path-way [24,25] ESCRT machinery has been proposed to

have additional roles in other membrane

deforma-tion⁄ fission events, such as retrovirus budding and

membrane fission of daughter cells in cytokinesis [26]

The core ESCRT system is composed of four

com-plexes, termed ESCRT-0, ESCRT-I, ESCRT-II and

ESCRT-III, and associated proteins, including

AAA-type ATPase vacuolar protein sorting (VPS)4 VPS4

interacts with components of ESCRT-III via its MIT

domain, and catalyzes the dissociation of ESCRTs

from membranes [27] We previously reported that

cal-pain 7 associates with a subset of ESCRT-III and its

related proteins: charged multivesicular body protein

CHMP4c and CHMP7 [28] We also showed that

cal-pain 7 interacts with CHMP1B via its tandem MIT

domains, and that it partially colocalizes with

endocy-tosed epidermal growth factor, suggesting involvement

of calpain 7 in the ESCRT system [28]

On the basis of the resolved 3D structure, the MIT

domain of VPS4 forms three-helix bundles ESCRT-III

proteins commonly contain conserved amino acid

sequences for MIT binding, termed MIT-interacting

motif (MIMs), in their C-termini Two types of MIM

have been identified: MIM1 and MIM2 The former

forms an amphipathic helix that binds to the groove

between VPS4 MIT domain helices 2 and 3 [29,30],

and the latter forms a Pro-rich strand that binds

between helices 1 and 3 [31]

Human increased sodium tolerance-1 (IST1), an

or-tholog of yeast Ist1, possesses both MIM1 and MIM2

at its C-terminus [32,33] IST1 and Ist1 can bind to

several ESCRT-related proteins, including VPS4⁄ Vps4

and CHMP1B⁄ Did2 [32–35] Interestingly, the 3D

structure of the IST1 N-terminal domain is very

similar to that of the core domain of CHMP3, an

ESCRT-III component [35,36] Although small

interfering RNA-mediated knockdown effects on the

endocytic pathway are not evident, IST1 is required

for efficient cytokinesis in HeLa cells [32,33] IST1 and

Ist1 associate with CHMP1⁄ Did2 to regulate the

local-ization and ATPase activity of VPS4⁄ Vps4 [32,33,37]

Because of the structural and functional resemblance

to CHMP proteins, IST1 is now regarded as a new

ESCRT-III family member

The findings described above led us to investigate

whether calpain 7 interacts with IST1 through MIT–

MIM interactions In this study, we examined

cal-pain 7–IST1 interactions by in vitro and in vivo binding

experiments, using purified recombinant proteins and

cultured mammalian cells expressing epitope-tagged proteins We also investigated the effect of this interac-tion on the autolysis of calpain 7

Results

Glutathione-S-transferase (GST) pulldown assay

of FLAG–IST1

To investigate whether MIT domains of calpain 7 (cal-pain 7MIT) interact with IST1, we first performed a GST pulldown assay (Fig 2) GST-fused calpain7MIT (1–165 amino acids) followed by the protease cleavage site and His6-tag (GST–MIT–pHis) was purified with His-tag affinity resin, immobilized on glutathione– Sepharose beads, and incubated with cleared lysates of HEK293T cells expressing FLAG-tagged CHMP1B, CHMP4b, CHMP6 or IST1 After incubation, the beads were pelleted by low-speed centrifugation and washed Cleared lysates and proteins bound to the

Fig 2 GST–MIT–pHis pulldown assay of FLAG–IST1 HEK293T cells were transfected with pFLAG–CHMP1B pFLAG–CHMP4b, pFLAG–CHMP6 or pFLAG–IST1 At 24 h after transfection, cells were lysed, and the cleared lysates were incubated with recombi-nant GST-fused tandem MIT domains of calpain 7 (GST–MIT–pHis)

or GST–pHis (negative control) immobilized on glutathione–Sepha-rose beads The beads were then pelleted by low-speed centrifuga-tion and washed with the lysis buffer The cleared lysates (Input) and proteins in the pellets (pulldown product, Pulldown) were sub-jected to SDS ⁄ PAGE (10% gel) and WB, with mAb against FLAG Immunoreactive bands were detected by the chemiluminescence method Membranes were also stained with CBB Bands of GST– MIT–pHis and GST–pHis in the pulldown products are indicated by arrows.

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beads (pulldown products) were separated by

SDS⁄ PAGE and subjected to western blot (WB)

analy-sis with mAb against FLAG or visualized by staining

with Coomassie Brilliant Blue R-250 (CBB) The

inten-sities of the immunoreactive bands for FLAG–IST1 in

the pulldown products of GST–MIT–pHis were much

stronger than those of FLAG–CHMP1B and FLAG–

CHMP4b For FLAG–CHMP6 (negative control), no

specific immunoreactive band was detected under the

conditions used No signals were detected in the

con-trol pulldown products of GST–pHis

Coimmunoprecipitation of FLAG–IST1 with

monomeric green fluorescent protein (mGFP)–

calpain 7 mutants

Next, we investigated the interaction between calpain 7

and IST1 in mammalian cells by the

coimmunoprecipi-tation method Cleared lysates (Fig 3, Input) of

HEK293T cells coexpressing mGFP fused with

cal-pain 7 and various mutants (Fig 1A) and FLAG–IST1

were incubated with anti-green fluorescent protein

(GFP) serum for immunoprecipitation Clear

immunoreactive bands of FLAG–IST1 were detected

for mGFP–calpain 7, mGFP–calpain 7C290S (a mutant

with replacement of the putative catalytic Cys, Cys290,

by Ser), and mGFP–calpain 7MIT by WB analysis with

mAb against FLAG (Fig 3, IP, lower panel) The

signal was weak but significant for

mGFP–cal-pain 7MITb Signals were reduced to the background

or control level for mGFP–calpain 7MITa and mGFP– calpain 7DMIT The results indicated that tandem MIT domains are required for efficient calpain 7–IST1 inter-action Intriguingly, the degradation bands seen in mGFP–calpain 7 (Fig 3, closed and open triangles) were not detected in the case of mGFP–calpain 7C290S, suggesting that the degradation was caused by proteo-lytic activity of mGFP–calpain 7 itself We refer to this issue later

Effects of mutations of IST1 MIMs on binding to mGFP–calpain 7MIT

To investigate whether the MIM1 and⁄ or MIM2 regions present in IST1 are responsible for interaction with calpain 7 MIT domains, we performed a similar coimmunoprecipitation assay with mGFP–cal-pain 7MIT and various FLAG–IST1MIM deletion and point mutants (L326D, MIM2 Leu326 replaced by Asp; L353A, MIM1 Leu353 replaced by Ala; Fig 1B), which were previously shown to lose the ability to bind

to the VPS4 MIT domain [32] As shown in Fig 4 (bottom panel), the immunoreactive band for wild-type FLAG-IST1 (WT) was clearly detected, but for FLAG–IST1DMIM1, FLAG–IST1DMIM2, and all MIM

Fig 3 Coimmunoprecipitation of FLAG–IST1 with mGFP–calpain 7

mutants HEK293T cells were cotransfected with pFLAG–IST1 and

plasmids expressing calpain 7 mutants fused with mGFP At 24 h

after transfection, cleared lysates (Input, 10%, upper panel; 1%,

lower panel) were subjected to immunoprecipitation (IP) with

anti-GFP serum followed by WB analysis with mAb against anti-GFP (upper

panel) and mAb against FLAG (lower panel), respectively

Proteoly-sed fragments of mGFP–calpain 7 in wild-type (WT) and DMIT

con-structs are indicated by closed ( 45 kDa) and open ( 30 kDa)

triangles.

Fig 4 Effects of mutations of IST1 MIMs on binding to mGFP–cal-pain 7MIT mGFP–calmGFP–cal-pain 7MIT and various FLAG–IST1 mutants (see Fig 1B) were independently expressed in HEK293T cells Cleared lysate from cells expressing mGFP–calpain 7MIT was mixed with that expressing each FLAG–IST1 mutant, and each mix-ture was subjected to coimmunoprecipitation with anti-GFP serum The cleared lysates (Input) and immunoprecipitated proteins (IP) were subjected to WB analysis with mAb against GFP and mAb against FLAG, respectively.

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point mutants, signals were significantly weakened.

The signal for FLAG–IST1DMIM1,2decreased to almost

the background or negative control (FLAG–CHMP6)

level

Direct interaction between recombinant

calpain 7MIT and GST–IST1 proteins

The use of cleared lysates of HEK293T cells for all of

the experiments described above left the possibility

that unknown factors might mediate MIT–MIM

inter-actions To exclude this possibility, we performed in

vi-tro GST-pulldown assays with purified recombinant

calpain 7MIT, which was obtained by removal of GST

and His6-tag by digestion with PreScission protease

followed by ion exchange chromatography Purified

calpain 7MIT was incubated with GST–IST1 mutants

or GST immobilized on glutathione–Sepharose beads

Pulldown products were visualized by staining with

CBB Calpain 7MIT was pulled down by GST–IST1

and GST–MIM (Fig 5, Pulldown, open triangle) but

not by GST–MIML326D,L353Aor GST

Enhancement of autolytic activity of mGFP–

calpain 7 by calpain 7–IST1 interaction

As shown in Fig 3, expression of mGFP–calpain 7 in

HEK293T cells generated  45 and 30 kDa fragments

(designated as 45 K and 30 K, respectively, in this

arti-cle), and those bands were not detected in the case of

mGFP–calpain 7C290S A similar result was obtained

when we used HeLa cells (data not shown) mGFP–

calpain 7 was thought to be proteolysed by its own proteolytic activity, which led us to investigate this phenomenon further

Estimation of cleavage sites in mGFP–calpain 7 mGFP–calpain 7, mGFP–calpain 7C290S and mGFP– calpain 7C290A (a mutant with the putative catalytic Cys, Cys290, replaced by Ala) were transiently expressed in HEK293T cells, and total cell lysates were analyzed by WB analysis with mAb against GFP or polyclonal antibody (pAb) against calpain 7 (raised against recombinant MIT domains [28]) In the case of

WB analysis with mAb against GFP, 45 K and 30 K were reproducibly detected for mGFP–calpain 7 but not for mGFP–calpain 7C290S and mGFP–cal-pain 7C290A(Fig 6B, upper panel, closed and open tri-angles) With pAb against calpain 7, an  45 kDa fragment was also detected specifically for mGFP–cal-pain 7 (Fig 6B, lower panel, gray triangle) These data indicate that a putative catalytic Cys, Cys290, of cal-pain 7 has a critical role in the wild-type-specific prote-olysis To examine whether the 45 kDa fragment detected by WB analysis with pAb against calpain 7 is identical to 45 K, cleared lysates from cells expressing mGFP–calpain 7 or mGFP–calpain 7C290S were sub-jected to immunoprecipitation with anti-GFP serum or pAb against calpain 7, followed by WB analysis with mAb against GFP and mAb against calpain 7 (raised against calpain 7 MITb [28]), respectively As shown in Fig 6C, 45 kDa fragments were wild-type-specifically detected in both immunoprecipitation products (upper

Fig 5 Direct interaction between recombinant calpain 7MIT and GST–IST1 Purified recombinant calpain 7 MIT domain (1–165 amino acids), calpain 7MIT, was incubated with GST (negative control), GST–IST1, GST–IST1MIM or GST–IST1MIM L326D,L353A that had been immobilized

on glutathione–Sepharose beads and subjected to GST-pulldown assay Purified proteins, initial protein mixtures (Input) and pulldown prod-ucts (Pulldown) were resolved on a 15% gel by SDS ⁄ PAGE, and subjected to CBB staining Open triangles and closed triangles indicate bands of recombinant calpain 7MIT and GST, GST–IST1, GST–IST1MIM, and GST–IST1MIM L326D,L353A , respectively.

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panel, closed triangle; lower panel, gray triangle),

sug-gesting that 45 K contains both mGFP and MIT

domains of calpain 7 On the other hand, the

anti-GFP-reacting 30 kDa band was not detected in the

immunoprecipitates of antibody against calpain 7,

indicating a lack of MIT domains in 30 K Thus,

mGFP–calpain 7 contains at least two cleavage sites: one lies at the N-terminal boundary of the protease domain, generating 45 K, and the other lies between mGFP and MITa, generating 30 K (Fig 6A) To roughly estimate the latter cleavage site in mGFP–cal-pain 7, we used three types of unfused mGFP

Fig 6 Estimation of cleavage sites in

mGFP–calpain 7 (A) Schematic

representa-tions of mGFP–calpain 7 (fragmentary view)

and unfused mGFP constructs with stop

codons at different positions at their

C-ter-mini Two estimated cleavage sites

generat-ing 45 and 30 kDa fragments (designated 45

and 30 K, respectively) are indicated by solid

arrows (B) The putative catalytic residue

Cys290 was replaced by either Ser or Ala,

mGFP–calpain 7 (WT), mGFP–calpain 7 C290S

(C290S) and mGFP–calpain 7C290A(C290A)

were transiently expressed in HEK293T

cells, and total cell lysates were then

ana-lyzed by WB with mAb against GFP and

pAb against calpain 7, respectively Arrows

and closed and open triangles indicate

full-length mGFP–calpain 7 and 45 K and 30 K,

respectively, and the gray triangle indicates

the 45 kDa fragment (45 K) detected by WB

analysis with pAb against calpain 7 [also

shown in (C) and (D)] (C) Cleared lysates

from cells expressing mGFP–calpain 7 or

mGFP–calpain 7 C290S were subjected to

immunoprecipitation (IP) with anti-GFP

serum or pAb against calpain 7, followed by

WB analysis with mAb against GFP and

mAb against calpain 7, respectively (D)

mGFP–calpain 7, mGFP–calpain 7C290Sand

three types of unfused mGFP constructs

(mGFP 265 , mGFP 259 or mGFP 239 ) were

tran-siently expressed in HEK293T cells, and

total cell lysates from those cells and

un-transfected cells were analyzed by WB with

mAb against GFP to compare the

electro-phoretic mobility of 30 K with that of each

mGFP Asterisks indicate 33 kDa bands that

were detected in both the wild type (WT)

and Cys290-substituted mutants (C290S and

C290A).

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constructs that have stop codons at different positions

at their C-termini: mGFP265, mGFP259 and mGFP239

(see Fig 6A and Experimental procedures) These

mGFP proteins were transiently expressed in HEK293T

cells, and total cell lysates were analyzed by WB with

mAb against GFP to compare the electrophoretic

mobility of 30 K with that of each mGFP construct As

shown in Fig 6D, the electrophoretic mobility of 30 K

was closer to that of mGFP239 This result suggested

that mGFP–calpain 7 was cleaved at the point

immedi-ately after or in the vicinity of residue 239 of mGFP

In order to determine an autolytic cleavage site in

mGFP–calpain 7–Strep, we also attempted to purify a

C-terminal fragment by using Strep-Tactin Sepharose

beads Although extraneous bands other than intact

expression products were detected, they were common

to both the wild type and the C290S mutant (Fig 7A)

Moreover, no wild-type-specific bands were detected

by probing with antibody against Strep or

Strep-Tac-tin-conjugated horseradish peroxidase (data not

shown) Thus, it is likely that autolytic cleavage also

occurs near the C-terminus of calpain 7 before or

immediately after N-terminal cleavage The faint,

 33 kDa, bands detected with mAb against GFP

[indicated by asterisks in Fig 6: (B), top, lanes 3–5;

(C), top, lanes 1, 2, 4 and 5; (D), last two lanes] were

found not only for the wild type but also for the Cys

mutants (C290S and C290A) Thus, they were

proba-bly derived by limited digestion with other cellular

pro-teases, and not by autolysis of mGFP–calpain 7

Enhancement of autolysis of mGFP–

calpain 7–Strep by GST–MIM in vitro

As we observed direct MIT–MIM interaction in vitro

(Fig 5), we speculated that IST1 serves as an activator

for mGFP–calpain 7 via MIT–MIM interaction To

investigate this possibility, we performed an in vitro

‘autolysis assay’ mGFP–calpain 7–Strep was expressed

in HEK293T cells, and purified by affinity purification

with Strep-Tactin Sepharose beads (Fig 7A) Purified

mGFP–calpain 7–Strep ( 0.7 lg) was incubated with

1 lg of recombinant GST–IST1, GST–MIM or GST

(negative control) at 30C for 20 h After incubation,

samples were analyzed by WB with mAb against GFP

to detect proteolysed fragments of

mGFP–cal-pain 7–Strep As expected, addition of GST–IST1 and

GST–MIM enhanced the generation of 30 K, but

addi-tion of GST did not (Fig S1) As the purified

recombi-nant GST–IST1 contained multiple degraded

fragments, we used GST–MIM for further analyses

Next, we performed a similar assay with GST–

MIM, GST–MIML326D,L353A or GST-fused CHMP6

N-terminal half (GST–CHMP6NT) as a negative con-trol As shown in Fig 7B, addition of GST–MIM enhanced the generation of 30 K, but only a marginal enhancing effect was observed with the addition of GST–MIML326D,L353A or GST–CHMP6NT In the case of mGFP–calpain 7C290S–Strep, with or without any recombinant proteins, no degraded bands were

Fig 7 Enhancement of autolysis of mGFP–calpain 7–Strep by GST–MIM in vitro (A) Purification of mGFP–calpain 7–Strep and mGFP–calpain 7 C290S –Strep from HEK293T cells Cleared lysate of untransfected HEK293T cells (mock) and those of cells expressing C-terminally Strep-tagged mGFP–calpain 7 (WT) or mGFP–cal-pain 7 C290S (C290S) were incubated with Strep-Tactin Sepharose beads After incubation, unbound proteins were removed (Unbound), and the beads were washed Proteins bound to the beads were eluted with a buffer containing 5 m M D -desthiobiotin (Purified proteins) Samples were separated by SDS ⁄ PAGE fol-lowed by CBB staining The arrow and asterisk indicate bands of mGFP–calpain 7–Strep and Strep-Tactin detached from beads, respectively (B) Purified mGFP–calpain 7–Strep (WT and C290S) proteins ( 0.7 lg) were incubated at 30 C for 20 h with either GST–MIM, GST–MIM L326D,L353A or GST–CHMP6NT (1 lg) or with-out additional proteins ( )) Samples without incubation (time 0) were also analyzed After incubation, samples were subjected to SDS ⁄ PAGE (15% gel) and analyzed by WB with mAb against GFP

to detect proteolysed fragments of mGFP–calpain 7–Strep Bands

of full-length WT and C290S are indicated by the arrow, and those

of 30 K are indicated by the open triangle.

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detected This result strongly suggests that 30 K is

generated by proteolytic activity of

mGFP–cal-pain 7–Strep itself, not by potentially contaminating

proteases in the preparations, and that MIT–MIM

interaction enhances the autolytic activity of mGFP–

calpain 7–Strep in vitro

Autolytic properties of mGFP–calpain 7–Strep

We further characterized the autolytic activity of

mGFP–calpain 7–Strep Purified

mGFP–cal-pain 7–Strep was incubated with GST–MIM in a

buf-fer containing 2 mm CaCl2 or EGTA As compared

with the control (a sample without addition of CaCl2

or EGTA), neither enhancing nor inhibitory effects on

the generation of 30 K were observed with the

addi-tion of 2 mm CaCl2 or EGTA (data not shown) On

the other hand, when purified mGFP–calpain 7–Strep

was incubated with GST–MIM in the presence of

vari-ous protease inhibitors or N-ethylmaleimide, a

sulfhy-dryl modification reagent, the generation of 30 K was

almost completely abolished by 10 mm

N-ethylmalei-mide (Fig 8A) and partially inhibited by 1 mm

leupep-tin (inhibitor of trypsin-type serine proteases and

cysteine proteases) or 1 mm E-64 (cysteine protease

inhibitor) (Fig 8B) Obvious effects of other protease

inhibitors were not observed with the use of 3 lm

recombinant human calpastatin domain 1 (CSD1,

cal-pain inhibitor protein), 0.5 lm ovocystatin (cysteine

protease inhibitor protein), 20 lm MG-132

(protea-some inhibitor), 20 lm antipain (cysteine protease

inhibitor), 20 lm

N-acetyl-l-leucyl-l-leucyl-l-norleuci-nal (ALLNal) (calpain inhibitor) or 2 mm pefabloc

(serine protease inhibitor)

Effects of ESCRT-related proteins on autolysis of

mGFP–calpain 7 in vivo

Next, we examined whether IST1 affects the generation

of 30 K in vivo mGFP–calpain 7 was coexpressed with

either FLAG–IST1 or FLAG–IST1DMIM1,2 in

HEK293T cells, and total cell lysates were analyzed by

WB with mAb against GFP As shown inFig 9A, the

effect of coexpression with FLAG–IST1 on the

genera-tion of 30 K was not so obvious regarding the ratio of

precursor (arrow) and 30 K (open triangle) On the

other hand, coexpression with FLAG–IST1DMIM1,2

reduced 30 K generation Overexpression of VPS4BE235Q

(a VPS4B mutant with replacement of Glu235 by Gln,

lacking ATPase activity) is known to cause

accumula-tion of ESCRTs on the endosomal membrane to form

aberrant multivesicular bodies MVB [27] As shown in

Fig 9B, coexpression with FLAG–VPS4BE235Q

signifi-cantly reduced the generation of 30 K as compared with the control vector

Discussion

IST1 is a newly reported ESCRT-III (or CHMP) fam-ily member, and interacts with the MIT domain of VPS4 [32,33] In this study, we showed for the first time that a tandem repeat unit of MIT domains of human calpain 7 directly interacts with the C-terminal region of IST1 (Fig 5) We previously reported an interaction between calpain 7 and CHMP1B [28], but this interaction seems to be much weaker than that between calpain 7 and IST1 under the conditions employed (Fig 2) As shown by mutational analyses (Fig 4), the observed stronger interaction may be attributable to the presence of two potential binding sites in the IST1 C-terminal region, which contains

Fig 8 Autolytic properties of mGFP–calpain 7–Strep Effects of protease inhibitors and sulfhydryl modification reagent on autolysis

of mGFP–calpain 7–Strep were investigated Purified mGFP–cal-pain 7–Strep was incubated at 30 C for 20 h with GST–MIM in a buffer containing protease inhibitors as indicated (A) As a control, the same volume of a vehicle used for dissolving reagents was added to the reaction mixture in place of inhibitors Bands of full-length mGFP–calpain 7–Strep and those of 30 K are shown in the upper and lower panels, respectively Additionally, leupeptin, E-64 and pefabloc were tested at higher concentrations (B).

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two types of MIM motif (MIM1 and MIM2) for

bind-ing to VPS4 MIT [32,33] MIM1 and MIM2 were

orig-inally defined by differences in binding to different

grooves formed by a three-helix bundle of the MIT

domain of mammalian VPS4 or yeast Vps4 [29–31]

MIM1 of CHMP1A or Vps2 binds to the groove

between helices 2 and 3, and MIM2 of CHMP6 binds

to that between helices 1 and 3 Bajorek et al [32]

suggested that MIM1 and MIM2 of IST1 also bind to

the different grooves of VPS4 MIT, on the basis of NMR chemical shift mapping Their mutational analy-ses revealed that MIM1 and MIM2 have a synergistic effect on binding to MIT, suggesting that the two grooves in the three-helix bundle of VPS4 MIT accept MIM1 and MIM2 simultaneously [32] In analogy to those findings, either one of the MIT domains of cal-pain 7 seems to be sufficient for binding to MIMs of IST1 However, our data indicated that both MIT domains are required for efficient interaction (Fig 3) One conceivable explanation for this observation is that tandem MIT domains may act as a single inte-grated module The yeast ESCRT-related protein Vta1 also has tandem MIT domains, and the 3D structures showed that they are closely associated by extensive hydrophobic interactions, which make two MIT domains an apparent single module [38] As the linker region between the MIT domains of calpain 7 is much shorter than that of Vta1 (five residues versus 21 resi-dues), it is not certain whether the same theory applies to calpain 7, but the idea that tandem MIT domains of calpain 7 affect each other to maintain an interacting interface seems attractive However, at present, we have no clue as to whether MIM1 and MIM2 bind to only one MIT domain or bind to each

of the two MIT domains of calpain 7, and it is not known why interaction between calpain 7 and the MIM2-containing protein CHMP6 was not observed (Fig 2) [28] Structural studies, such as cocrystalliza-tion and X-ray analysis of tandem MIT domains of calpain 7 and IST1 MIM elements, should clarify these issues in the future

Although the physiological role of human calpain 7

is still unknown, the presence of tandem MIT domains might contribute to its role being different from that in unicellular organisms Whereas Cpl1 (yeast calpain 7) does not possess an apparent MIT domain, PalB (fun-gal calpain 7) has only a single MIT domain In accor-dance with this difference, reported binding partners are not identical among calpain 7, Cpl1 and PalB Cpl1 and PalB were shown to interact with the ESC-RT-III core proteins Snf7⁄ Vps32 (CHMP4) and Vps24 (CHMP3), respectively [39,40], but interaction between Cpl1⁄ PalB and CHMP1 orthologs (Did2 ⁄ DidB) has not been reported Thus, the N-terminal regions of calpain 7 might have evolved to acquire different strat-egies for involvement in the ESCRT system, and the tandem MIT domains may govern interacting features unique to human calpain 7, enabling it to execute its physiological roles differently from lower eukaryotic calpains

In yeast and fungi, the transcription factor Rim101⁄ PacC is thought to be a substrate of Cpl1⁄ PalB, and it

Fig 9 Effects of ESCRT-related proteins on autolysis of

mGFP–cal-pain 7 in vivo (A) mGFP–calmGFP–cal-pain 7 of either the wild type (WT) or

C290S mutant was coexpressed with either FLAG–IST1 or FLAG–

IST1 DMIM1,2 in HEK293T cells, and total cell lysates were analyzed

by WB with mAb against GFP and mAb against FLAG, respectively.

Bands of 45 kDa (45 K) and 30 kDa (30 K) are indicated by closed

and open triangles, respectively Cotransfection with a blank vector

instead of IST1 expression plasmids was performed for control

experiments (B) The effect of coexpression of FLAG–VPS4B E235Q

on mGFP–calpain 7 autolysis was investigated as shown in (A).

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has been proposed that Rim101⁄ PacC is also recruited

around the ESCRTs on the endosomal membranes by

binding to Snf7⁄ Vps32-interacting factor Rim20 ⁄ PalA

[16,18] On the other hand, a human homolog of

Rim101⁄ PacC has not been identified Futai et al

showed that His-tagged calpain 7 purified from COS

cells does not proteolyse typical calpain substrates

in vitro [13] In this study, we found that GST-fused

MIM of IST1 enhances the autolysis of purified

mGFP–calpain7–Strep in vitro (Fig 7B),

demonstrat-ing the protease activity of calpain 7 for the first time

This finding suggests that calpain 7 also functions as a

protease rather than as a structural protein in

mamma-lian cells, and that MIT domains are involved in

cal-pain 7 activation This notion leads us to suggest two

possible activation mechanisms of calpain 7 in vitro:

(a) by binding of MIM, MIT domains dissociate from

the protease domain to expose the catalytic core; and

(b) binding of MIM causes a conformational change

of calpain 7 to create an active catalytic core We

observed that an mGFP-fused calpain 7 mutant

lack-ing tandem MIT domains (mGFP–calpain 7DMIT) is

still proteolysed to generate 30 K in cultured cells

(Fig 3), apparently supporting the former possibility

However, it is also possible that IST1 acts on the

sub-strate rather than on the protease To investigate

fur-ther whefur-ther the autolysis is an intermolecular or

intramolecular reaction, we purified N-terminally

Strep-tagged calpain 7 as a protease source, and

incu-bated it with either mGFP–calpain 7C290S–Strep or

mGFP–calpain 7DMITC290S–Strep in the presence of

GST–MIM As a result, proteolysed

mGFP–cal-pain 7C290S–Strep fragment (30 K) was detected

(Fig S2), suggesting that autolysis of calpain 7 is

inter-molecular As the degree of degradation of

mGFP–cal-pain 7DMITC290S–Strep was slightly decreased, it is

likely that IST1 acts on MIT of the substrate and

influences the accessibility of the substrate to the

enzyme However, there remains a possibility that a

gross conformational change induced by deletion of

MIT from mGFP–calpain 7C290S–Strep itself made the

substrate more resistant to the protease Moreover, the

efficiency of generation of 30 K in the intermolecular

reaction experiment seems less than that observed in

the experiment in which mGFP–calpain 7 was

incu-bated, and we cannot exclude the possibility that both

an intramolecular reaction and an intermolecular

reac-tion occur in the autolysis Therefore, it is premature

to draw conclusions regarding the mechanism of the

enhancing effects of IST1 on mGFP–calpain 7–Strep

autolysis in vitro

Both mGFP–calpain 7 and IST1 have been reported

to accumulate on aberrant endosomes when an

ATPase-defective VPS4 mutant (VPS4BE235Q, used in this study) is expressed in HeLa cells [28,33] However, overexpression of FLAG–VPS4BE235Q reduced 30 K generation (Fig 9B), suggesting that proper recruit-ment of calpain 7 is important for its activation In the case of conventional calpains, a C2-like domain has been suggested to partially contribute to Ca2+ -depen-dent membrane binding [41] However, we previously reported that the subcellular distribution of calpain 7

is not significantly affected by Ca2+, and that mGFP– calpain 7DMIT coexpressed with monomeric red fluo-rescent protein–VPS4BE235Q does not accumulate on aberrant endosomes [28] These observations strongly suggest that MIT domains are responsible for regulat-ing the subcellular localization of calpain 7 As shown

in Fig 9A, overexpression of FLAG–IST1 did not enhance the autolysis of mGFP–calpain 7 in cultured cells On the other hand, overexpression of FLAG– IST1DMIM1,2suppressed the autolysis This observation might be explained by regarding IST1 as a regulator of the intracellular localization of calpain 7, because IST1 was previously reported to contribute to recruitment of VPS4 to an ESCRT-III-accumulated region in the cell [32,33] Given that endogenous IST1 is sufficient for the recruitment of calpain 7 around ESCRTs, overex-pression of FLAG–IST1 would have no additive effects On the other hand, overexpressed FLAG– IST1DMIM1,2 would occupy the ESCRT surface, and hamper binding of endogenous IST1, resulting in fail-ure of calpain 7 recruitment and exhibiting a domi-nant-negative effect To test this hypothesis, we performed fluorescence microscopic analyses, and investigated the subcellular localization of overexpres-sed FLAG–IST1⁄ IST1DMIM1,2 and mGFP–calpain 7 in HeLa cells These proteins displayed diffuse or par-tially colocalized punctate distribution around nucleus There were no significant differences in the punctate distribution of mGFP–calpain 7 between cells coex-pressing FLAG–IST1 and and those coexcoex-pressing FLAG-IST1DMIM1,2 (data not shown) Thus, it is not clear why FLAG–IST1 had no enhancing effects on autolysis and FLAG–IST1DMIM1,2inhibited the autoly-sis of mGFP–calpain 7 Other unknown cytosolic fac-tors that physically associate with IST1 but whose amounts are limited might be involved in enhancing the autolysis of mGFP–calpain 7

When fungal calpain 7 (PalB) cleaves PacC (a tran-scription factor acting on alkaline adaptation), PalA functions as a scaffold to recruit PacC to endosomal membranes by recognizing two YPXL motifs present

in the C-terminal half of PacC [16] A human ortholog

of PalA, ALIX (also known as AIP1), functions in the budding of enveloped RNA viruses from plasma

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