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Báo cáo khoa học: Stabilities and activities of the N- and C-domains of FKBP22 from a psychrotrophic bacterium overproduced in Escherichia coli pptx

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We have previously shown that the cellular content of FKBP22 SIB1 FKBP22 from a psychrotrophic Keywords domain structure; FKBP22; PPIase; psychrotrophic bacterium; thermal stability Corr

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of FKBP22 from a psychrotrophic bacterium overproduced

in Escherichia coli

Yutaka Suzuki1, Kazufumi Takano1,2and Shigenori Kanaya1

1 Department of Material and Life Science, Graduate School of Engineering, Osaka University, Suita, Osaka, Japan

2 PRESTO, JST, Suita, Osaka, Japan

When polypeptides are synthesized at ribosomes,

pep-tide bonds are connected in trans form In the case of

peptide bonds N-terminal of the proline residues,

how-ever, some of them form cis peptide bonds in correctly

folded proteins [1] Consequently, trans-to-cis

conver-sions of these peptide bonds (prolyl isomerizations)

should occur during protein folding reactions As

dem-onstrated in some refolding experiments [2,3], prolyl

isomerizations are relatively slow and can be the rate

limiting step in protein folding reactions The cis-trans isomerizations of peptide bonds N-terminal of the pro-line residues are catalyzed by peptidylprolyl cis-trans isomerases (PPIases; EC 5.2.1.8) [4] Three structurally unrelated families of PPIases are known They are cyclophilins, parvulins, and FK506-binding proteins (FKBPs) [5]

We have previously shown that the cellular content

of FKBP22 (SIB1 FKBP22) from a psychrotrophic

Keywords

domain structure; FKBP22; PPIase;

psychrotrophic bacterium; thermal stability

Correspondence

S Kanaya, Department of Material and Life

Science, Graduate School of Engineering,

Osaka University, 2-1, Yamadaoka, Suita,

Osaka 565-0871, Japan

Tel ⁄ Fax: +81 6 6879 7938

E-mail: kanaya@mls.eng.osaka-u.ac.jp

(Received 27 September 2004, revised 23

October 2004, accepted 29 October 2004)

doi:10.1111/j.1742-4658.2004.04468.x

FKBP22 from a psychrotrophic bacterium Shewanella sp SIB1, is a

dimer-ic protein with peptidyl prolyl cis-trans isomerase (PPIase) activity Accord-ing to homology modelAccord-ing, it consists of an N-terminal domain, which is involved in dimerization of the protein, and a C-terminal catalytic domain

A long a3 helix spans these domains An N-domain with the entire a3 helix (N-domain+) and a C-domain with the entire a3 helix (C-domain+) were overproduced in Escherichia coli in a His-tagged form, purified, and their biochemical properties were compared with those of the intact protein C-domain+was shown to be a monomer and enzymatically active Its opti-mum temperature for activity (10C) was identical to that of the intact protein Determination of the PPIase activity using peptide and protein substrates suggests that dimerization is required to make the protein fully active for the protein substrate or that the N-domain is involved in sub-strate-binding The differential scanning calorimetry studies revealed two distinct heat absorption peaks at 32.5C and 46.6 C for the intact protein, and single heat absorption peaks at 44.7C for N-domain+ and 35.6C for C-domain+ These results indicate that the thermal unfolding transi-tions of the intact protein at lower and higher temperatures represent those

of C- and N-domains, respectively Because the unfolding temperature of C-domain+ is much higher than its optimum temperature for activity, SIB1 FKBP22 may adapt to low temperatures by increasing a local flexibil-ity around the active site This study revealed the relationship between the stability and the activity of a psychrotrophic FKBP22

Abbreviations

ALPF, N-succinyl-Ala-Leu-Pro-Phe-p-nitroanilide; CD, circular dichroism; DSC, differential scanning calorimetry; FKBP, FK506-binding protein; MIP, macrophage infectivity potentiator; PPIase, peptidyl prolyl cis-trans isomerase.

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bacterium Shewanella sp SIB1 increases at 4C, as

compared to that at 20C [6] This protein is a member

of the macrophage infectivity potentiator (MIP)-like

FKBP subfamily proteins and shows amino acid

sequence identities of 56% to Escherichia coli FKBP22

[7], 43% to E coli FkpA [8], and 41% to Legionella

pneumophila MIP [9] SIB1 FKBP22 exists as a

homo-dimer and exhibits the PPIase activity like other

MIP-like FKBP subfamily proteins However, the optimum

temperature of this protein for activity (10C) is much

lower than that of E coli FKBP22 (> 25C) We

pose that this activity facilitates efficient folding of

pro-teins containing cis prolines in psychrotrophic bacteria

at low temperatures

According to the crystal structures of L pneumophila

MIP [10] and E coli FkpA [11], these proteins are

com-posed of N- and C-domains, which are spanned by a 40

amino acid long a3 helix The N-domain consists of a1

and a2 helices and an N-terminal region of a3 helix

The C-domain consists of six b-strands (b1–b6), a4

helix, and a C-terminal region of a3 helix The

N-domain is unique to the MIP-like FKBP subfamily

proteins This domain is involved in dimerization of the

protein and the interface between two monomers is

sta-bilized by the hydrophobic interactions of a1 and a2

helices In contrast, the C-domain (except a3 helix) is

conserved in all FKBP family proteins and contains the

entire PPIase active-site, suggesting that all FKBP

fam-ily proteins share a common catalytic mechanism The

a3 helix seems to be required to control the positions of

the two C-domains of the homodimer, such that these

domains are located with an appropriate distance and

orientation Because of the high similarity in the amino

acid sequence of SIB1 FKBP22 with that of L

pneumo-philaMIP and E coli FkpA, SIB1 FKBP22 might have

a similar three-dimentional structure

The stability–activity relationships of MIP-like FKBP

subfamily proteins remain to be analyzed Because the

prolyl isomerization is a spontaneous reaction and the

rate for this reaction increases as the reaction

tempera-ture increases, the PPIase activity cannot be accurately

determined at > 30C Therefore, it seems difficult to

analyze the stability–activity relationships of PPIases

from mesophilic and thermophilic organisms SIB1

FKBP22 seems to be an excellent model to analyze these

relationships because its optimum temperature for

activ-ity is 10C In addition, because this protein is expected

to consist of N- and C-domains, it would be informative

to construct the SIB1 FKBP22 variants containing

either one of these domains and compare their activities

and stabilities with those of the intact protein

In this report, the N- and C-domains of SIB1

FKBP22 were overproduced in E coli and purified in

an amount sufficient for physicochemical studies By comparing their activities and stabilities with those of the intact protein, we showed that the unfolding tem-perature of SIB1 FKBP22 is much higher than the optimum temperature for activity Based on these results, we discuss a role of each domain of SIB1 FKBP22 and a cold-adaptation mechanism of this protein

Results

Design

A model for the three-dimensional structure of the His-tagged form of SIB1 FKBP22 (SIB1 FKBP22*) was constructed based on the crystal structure of

L pneumophila MIP [10] (Fig 1) According to this model, SIB1 FKBP22 consists of N- and C-domains The N-domain of one molecule interacts with that of another molecule to form a homodimer The C-domain represents a catalytic domain Based on this model, three types of the SIB1 FKBP22 variants con-taining either one of these two domains were designed They are N-domain+, C-domain+, and C-domain– The primary structures of these variants are schemati-cally shown in comparison with that of the intact pro-tein in Fig 2 Because a long a3 helix spans both the N- and C-domains, and because the region containing only a1 and a2 helices seems to be too short to fold correctly, N-domain+ was designed such that

it contains the entire a3 helix Likewise, C-domain+ and C-domain– were designed such that the former

Fig 1 A tertiary model of SIB1 FKBP22 homodimer The a3 helix (Val52–Arg93), which spans both the N- and C-domains, is most deeply shaded The N-domain without a3 helix (Met1–Ala51), which

is involved in dimerization, is moderately shaded, and the C-domain without a3 helix (Asp94–Ile205), which is involved in catalytic func-tion, is most lightly shaded.

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contains the entire a3 helix and the latter does not

contain it

Overproduction and purification

Upon induction for overproduction at 10C,

N-domain+ and C-domain+ accumulated in the cells

in a soluble form, whereas C-domain– accumulated in

the cells in inclusion bodies (Fig 3) C-domain– was

solubilized in the presence of 6 m urea and refolded by

removing urea with a yield of nearly 100% All

pro-teins were purified to give a single band on

SDS⁄ PAGE (data not shown)

The molecular masses of N-domain+, C-domain+,

and C-domain– were estimated to be 15 kDa, 26 kDa,

and 17 kDa, respectively, by SDS⁄ PAGE (Fig 3)

These values are slightly larger than the calculated

ones from their amino acid sequences including a

His-tag (12 042 for N-domain+, 19 149 for C-domain+,

and 14 085 for C-domain–) The molecular mass of SIB1 FKBP22* estimated by SDS⁄ PAGE (29 kDa) has been reported to be larger than that determined by EMI-MS, which is identical to the calculated one (23 947) [6] Slow migration in the gel may be a char-acteristic common to SIB1 FKBP22* and its variants The molecular masses of N-domain+ and C-domain+ were also estimated to be 39 kDa and 23 kDa, respect-ively, by gel filtration column chromatography The former and latter values are larger than the calculated ones by 3.2 and 1.2 times, respectively, suggesting that N-domain+ exists as a trimer and C-domain+ exists

as a monomer However, the molecular mass of a dimeric form of SIB1 FKBP22* estimated by gel filtra-tion column chromatography has been reported to be larger than that determined by sedimentation equilib-rium analytical ultracentrifuge by 1.5 times [6] This discrepancy is probably caused by the unusual mole-cular shape of the protein, which is cylindrical rather

Fig 3 Estimation of the amount of the proteins in soluble and insoluble forms by SDS ⁄ PAGE N-domain + (A), C-domain – (B), and C-domain +

(C) were overproduced in E coli as described for SIB1 FKBP22* [6] The soluble (lane S) and insoluble (lane P) fractions after sonication lysis were analyzed by 15% (for C-domain + ) and 17% (for N-domain + and C-domain – ) SDS ⁄ PAGE The gel was stained with Coomassie Brilliant Blue Arrows indicate the recombinant proteins overproduced in the cells The positions of the standard proteins contained in a low mole-cular mass marker kit (Pharmacia Biotech, Piscataway, NJ, USA) are shown alongside the gels, together with their molemole-cular masses.

Fig 2 Schematic representations of the pri-mary structures of SIB1 FKBP22* and its variants A His-tag attached to the N-termini

of the proteins is represented by shaded box The a-helices and b-strands are repre-sented by cylinders and arrows, respect-ively These secondary structures are arranged based on a tertiary model of SIB1 FKBP22 Numbers indicate the positions of the residues relative to the initiator methio-nine residue The ranges of the N- and C-domains are also shown.

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than globular Because N-domain+ is expected to

assume a similar cylindrical structure, sedimentation

equilibrium analytical ultracentrifugation was

per-formed to determine its molecular mass in solution

The data fitted well to a single-species model with no

evidence of aggregation, and the molecular mass was

determined to be 23 431 Da This value is 1.9 times

larger than that calculated from the amino acid

sequence, indicating that N-domain+exists as a dimer

CD spectra

The far-UV CD spectra of N-domain+, C-domain+,

C-domain–, and SIB1 FKBP22* were measured at

10C (Fig 4A) The spectrum of N-domain+, which

gave a broad trough with a double minimum at 208

and 222 nm, was similar to that of SIB1 FKBP22*,

although the depth of the trough in this spectrum is

larger than that in the SIB1 FKBP22* spectrum

The helical content was calculated to be 51% for

N-domain+ and 38% for SIB1 FKBP22* from these

spectra using the method of Wu et al [12] These

val-ues were comparable to those calculated from a

ter-tiary model of SIB1 FKBP22* (60% for N-domain+

and 34% for SIB1 FKBP22*), suggesting that

N-domain+ assumes a similar helical structure to that

of the N-domain in the intact molecule On the other

hand, the CD spectra of C-domain+ and C-domain–

gave a broad trough with a single minimum at 207 nm

and one without any clear minimum, respectively The

depths of these troughs were considerably smaller than

that in the SIB1 FKBP22* spectrum

The near-UV CD spectra of these proteins were also

measured at 10C (Fig 4B) These spectra reveal the

three-dimensional environments of aromatic residues

such as Trp and Tyr SIB1 FKBP22* contains one

tryptophan residue (Trp157), which is conserved in the

FKBP family proteins and required for PPIase activity,

and seven tyrosine residues Because most of these

residues (one tryptophan and six tyrosine residues) are located in its C-domain, the near-UV CD spectrum of SIB1 FKBP22* may reflect the conformation of the C-domain The spectrum of C-domain+was similar to that of SIB1 FKBP22*, suggesting that C-domain+ assumes a similar structure to that of the C-domain

in the intact molecule In contrast, the spectrum of C-domain– was quite different from those of C-domain+ and SIB1 FKBP22*, suggesting that the structure of C-domain– is considerably different from that of the C-domain in the intact molecule

PPIase activity When the PPIase activity was determined at 10C

by the protease coupling assay using N-succinyl-Ala-Leu-Pro-Phe-p-nitroanilide (ALPF) as a substrate, C-domain+ exhibited PPIase activity, whereas C-domain– did not The catalytic efficiency (kcat⁄ Km)

of C-domain+ was estimated to be 1.43 lm)1Æs)1, which was 1.6 times higher than that of SIB1 FKBP22* The temperature dependence of the PPIase activity of C-domain+ was nearly identical to that of SIB1 FKBP22* (Fig 5A) In contrast, when the PPI-ase activity was determined by the RNPPI-ase T1refolding assay, C-domain+exhibited much less activity as com-pared to that of SIB1 FKBP22* The acceleration effect of C-domain+ on the RNase T1 refolding reac-tion was not detected at 21 nm, but detected at 210 nm (Fig 5B) The acceleration effect similar to that detec-ted in the presence of 210 nm C-domain+was detected

in the presence of 19 nm SIB1 FKBP22* The kcat⁄ Km values were estimated to be 0.5 lm)1Æs)1 for SIB1 FKBP22* and 0.015 lm)1Æs)1for C-domain+

Thermal stability Heat induced unfolding of N-domain+, C-domain+, and SIB1 FKBP22* were analyzed by differential

Fig 4 CD spectra of SIB1 FKBP22* and its

variants The far-UV (A) and near-UV (B) CD

spectra of SIB1 FKBP22* (dashed line),

N-domain + (heavy thick line), C-domain – (thin

line), and C-domain + (moderately thick line)

are shown All spectra were measured at

10 C as described under Experimental

procedures.

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scanning calorimetry (DSC) (Fig 6, Table 1) All DSC

curves were reproduced by repeating thermal scans,

indicating that thermal unfoldings of these proteins are

highly reversible The denaturation curve of SIB1

FKBP22* clearly showed two well separated

transi-tions Deconvolution of the thermogram according to

a non-two-state denaturation model gives melting

tem-perature (Tm) values of 32.5C and 46.6 C for these

transitions These Tmvalues are nearly equal to those

of C-domain+ (35.6C) and N-domain+ (44.7C),

suggesting that the thermal unfolding transitions of

SIB1 FKBP22* at lower and higher temperatures

rep-resent those of its C-domain and N-domain,

respect-ively For unfolding of N-domain+, the van’t Hoff

enthalpy (DHvH) was roughly two times larger than the

calorimetric enthalpy (DHcal) Because N-domain+

exists as a dimer, this result possibly reflects a coupling

of the unfolding of N-domain+ to dissociation of the homodimer Similarly, the unfolding reaction of C-domain+ seems to contain complex processes, as indicated by theDHcal⁄ DHvHratio far from unity

Comparison of thermal stability of SIB1 FKBP22* and E coli FKBP22*

To examine whether SIB1 FKBP22* is less stable than its mesophilic counterpart, heat induced unfolding of

E coli FKBP22* was analyzed by DSC However, thermodynamic parameters including Tmcould not be obtained because of the poor reversibility of this pro-tein in thermal unfolding Therefore, thermal stabilities

of SIB1 FKBP22* and E coli FKBP22* were analyzed

by circular dichroism (CD) The far-UV CD spectra of SIB1 FKBP22* and E coli FKBP22* were measured

at various temperatures and the spectra of SIB1 FKBP22* at 10 and 50 C are shown in comparison with those of E coli FKBP22* at 20 and 80C in Fig 7 The spectrum of SIB1 FKBP22* at 10C is identical to that shown in Fig 4A The spectra of

Table 1 Thermodynamic parameters for heat induced unfolding of SIB1 FKBP22*, C-domain + and N-domain + recorded by microcalori-metry The melting temperature (Tm), calorimetric enthalpy (DH cal ), and van’t Hoff enthalpy (DH vH ) were obtained from the DSC curves shown in Fig 6, using ORIGIN software (MicroCal, Inc.).

Protein T m (C) DH cal (kJÆmol)1) DH vH (kJÆmol)1)

Fig 6 DSC curves of N-domain+, C-domain+, and SIB1 FKBP22*.

The DSC curves of N-domain + (thick line), C-domain + (thin line), and

SIB1 FKBP22* (dashed line), which were measured at a scan rate

of 1 CÆmin)1, are shown These proteins were dissolved in 20 m M

sodium phosphate (pH 8.0) at 0.6 mgÆmL)1.

Fig 5 PPIase activities of C-domain + (A) The temperature dependence of the PPIase activity of C-domain + (–d–), which was determined

by protease coupling assay using ALPF as a substrate, is shown in comparison with that of SIB1 FKBP22* (–s–) The catalytic efficiency,

kcat⁄ K m , was calculated according to Harrison & Stein [34] The experiment was carried out in duplicate Each plot represents the average value and errors from the average values are shown (B) The increase in tryptophan fluorescence at 323 nm during refolding of RNase T1 (0.2 l M ) is shown as a function of the refolding time Refolding reaction was carried out at 10 C in the absence (dotted line), or presence of

21 n M of C-domain + (thick solid line), 210 n M of C-domain + (thin solid line) or 19 n M of SIB1 FKBP22* (dashed line).

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SIB1 FKBP22* at 10C and E coli FKBP22* at

20C, which represent the spectra of these proteins in

a native form, were similar to each other, suggesting

that the tertiary structures of these proteins are similar

to each other With a temperature shift from 10 to

50C, the spectrum of SIB1 FKBP22*, which gave a

broad trough with double minimum [h] values of

)11 200 at 209 nm and )12 100 at 222 nm, was

greatly changed so that it exhibits a trough with a

minimum [h] value of )7800 at 207 nm, which is

accompanied by a shoulder with a [h] value of )5700

at 220 nm A similar spectral change was observed for

E coli FKBP22* when the temperature was shifted

from 20 to 80C The spectra of SIB1 FKBP22* at

50C and E coli FKBP22* at 80 C were not

seri-ously changed at higher temperatures, indicating that

these spectra represent the spectra of these proteins in

a denatured form In these conditions, SIB1 FKBP22*

was fully reversible in thermal denaturation, whereas

E coli FKBP22* was not The reversibility of E coli

FKBP22* was roughly 70%

The thermal denaturation curves of SIB1 FKBP22*

and E coli FKBP22* were measured by monitoring a

change in the CD values at 222 nm (Fig 8) SIB1

FKBP22* apparently unfolded through an

intermedi-ate stintermedi-ate The Tmvalues for the first and second

transi-tions were roughly estimated to be 32 and 44C,

respectively, which were comparable with those

determined by DSC As compared to SIB1 FKBP22*,

E coli FKBP22* unfolded at higher temperatures, indicating that it is more stable than SIB1 FKBP22* However, it is unclear whether this protein unfolds through an intermediate state as well, because this intermediate state was not clearly detected The ther-mal unfolding curve of this protein did not fit the the-oretical curve, which was drawn on the assumption that the protein unfolds in a single cooperative fashion (data not shown)

Discussion

Unfolding of SIB1 FKBP22*

In this study, SIB1 FKBP22* was shown to unfold in

a complex non-two-state mechanism with two peaks apparent in the DSC curve Construction of the N-domain+ and C-domain+, which lack the C- and N-domains, respectively, followed by DSC analyses, clearly showed that two peaks of heat capacity observed in thermal unfolding of SIB1 FKBP22* rep-resent unfoldings of its N- and C-domains In this thermal unfolding process, the C- and N-domains unfold at lower and higher temperatures, respectively

It has been reported that a phosphoglycerate kinase [13] and a chitobiase [14] from psychrophilic bacteria consist of a heat labile domain and a heat stable domain Bentahir et al [13] have proposed that a heat labile domain provides a sufficient flexibility around the active site, and a heat stable domain provides a sufficient rigidity to the substrate-binding site, so that

Fig 8 Thermal denaturation curves of SIB1 FKBP22* and E coli FKBP22* The [h] values of SIB1 FKBP22* (trace 1) and E coli FKBP22* (trace 2) at 222 nm are shown as a function of tempera-ture The proteins were dissolved in 20 m M sodium phosphate (pH 8.0) at 0.30 mgÆmL)1for SIB1 FKBP22* and 0.29 mgÆmL)1for

E coli FKBP22* A cell with an optical path length of 2 mm was used Temperature was linearly raised at 1 CÆmin)1.

Fig 7 Far-UV CD spectra of SIB1 FKBP22* and E coli FKBP22*.

The CD spectra of SIB1 FKBP22* measured at 10 C (thick line) and

50 C (thick dashed line), and those of E coli FKBP22* measured at

20 C (thin line) and 80 C (thin dashed line) are shown The spectra

were measured as described under Experimental procedures.

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the enzymatic reaction is efficiently achieved at low

temperatures Because the C-terminal catalytic domain

of SIB1 FKBP22 represents a heat labile domain, the

instability of this domain may be required to increase

the flexibility of the active-site at low temperatures

Stability and activity of SIB1 FKBP22*

SIB1 FKBP22* was shown to be much less stable than

E coli FKBP22* Its optimal temperature for activity

has been reported to be greatly shifted downward as

compared to that of E coli FKBP22* [6]

Cold-adap-tation has been specified by the increase in the

cata-lytic efficiency at low temperatures, the downward

shift in the optimum temperatures for activity, and the

reduction in the conformational stability [15]

There-fore, SIB1 FKBP22 can be defined as a cold-adapted

enzyme, although it is less active than E coli

FKBP22* even at low temperatures [6] Several

cold-adapted enzymes have also been reported to be less

active than their mesophilic counterparts [16–19]

Analyses of the thermal stability of SIB1 FKBP22*

by DSC (Fig 3) and CD (Fig 8) indicate that

unfold-ing of this protein is initiated at > 25C In fact, the

CD spectrum of SIB1 FKBP22* at 20C was nearly

identical to that at 10C (data not shown), suggesting

that the conformation of this protein is not seriously

changed upon temperature shift from 10 to 20C

Thermal unfolding of C-domain+ is also initiated

at > 25C Nevertheless, SIB1 FKBP22* and

C-domain+ both exhibit the maximal PPIase activity

at 10C and their activities are greatly reduced at

20C These results suggest that a subtle

conforma-tional change around the active-site causes a great

reduction of the enzymatic activity The large

differ-ence in the temperatures for enzymatic inactivation

and structural unfolding has been observed for

cold-adapted a-amylase and family 8 xylanase from an

Antarctic bacterium [20,21] The apparent optimal

temperatures of these proteins for enzymatic activities

are much lower than the temperatures at which any

significant conformational event occurs In contrast,

the optimal temperatures for the activities of their

mesophilic and thermophilic counterparts closely

cor-relate with the temperatures for their structural

transi-tions Thus, the large difference in the temperatures

for enzymatic inactivation and structural unfolding

seems to be a characteristic feature of cold-adapted

enzymes It has been proposed that this difference is

caused by a cold-adaptation strategy termed ‘localized

flexibility’ [20] Although an increase in flexibility

around the active site increases kcat by reducing the

energy cost of conformational change during the

cata-lytic reaction, it should increase Km concomitantly By restricting the increase of flexibility within small areas, cold-adapted enzymes prevent unfavorable increases in

Km [22] SIB1 FKBP22 probably adopts a similar strategy for cold-adaptation

Structural importance of a3 helix

Two types of the SIB1 FKBP22* variants, which con-tain the C-domain, were designed based on its tertiary model C-domain+ contains an entire a3 helix, whereas C-domain– does not contain it These two proteins differ greatly in their biochemical properties C-domain+ was overproduced in E coli in a soluble form and exhibited the PPIase activity Its near-UV

CD spectrum was similar to that of SIB1 FKBP22*

In contrast, C-domain– was overproduced in E coli in inclusion bodies and exhibited little PPIase activity Its near-UV CD spectrum was quite different from that of SIB1 FKBP22* These results strongly suggest that a3 helix is required to facilitate folding of the C-domain,

or to stabilize it, so that the C-domain assumes a native conformation It has previously been reported that limited proteolysis of L pneumophila MIP allows the separation of their N- and C-domains such that the C-domain contains the C-terminal half of the a3 helix [23,24] In addition, the C-domain of E coli FkpA shows a high tendency to form inclusion bodies when it is overproduced in E coli in a form without a3 helix [25] These results are consistent with our results According to the crystal structure of L pneu-mophila MIP, there are three distinct contacts between the C-terminal region of a3 helix and the C-domain [10] These contacts may also be conserved in the structure of SIB1 FKBP22

Role of N- and C-domains Most organisms contain multiple PPIases within a sin-gle cell They are usually composed of several domains; one is common to the members of each family and specifies the family to which that PPIase belongs, and the others are unique to the particular PPIase and thought to be related to the protein’s distinct function The C- and N-domains of MIP-like FKBP subfamily proteins represent the former and latter domains, respectively Therefore, biochemical charac-terizations of N-domain+ and C-domain+ will facili-tate understanding of the roles of these domains in the intact molecule

The observation that N-domain+ exists as a dimer, whereas C-domain+ exists as a monomer supports a tertiary model of SIB1 FKBP22, in which the a1 and a2

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helices form the dimerization core of the protein In

addition, we showed that the PPIase activity of

C-domain+determined by the RNase T1refolding assay

was greatly reduced as compared to that of the intact

protein These results suggest that a dimeric structure of

SIB1 FKBP22 is responsible for its high PPIase activity

for protein substrates Alternatively, N-domain contains

a binding site for protein substrates Similar results have

been reported for other MIP-like FKBP subfamily

pro-teins For example, The C-domain of L pneumophila

MIP produced upon limited proteolysis has been

repor-ted to exist as a monomer and exhibit weak PPIase

activity for protein substrate [23] Likewise, the

C-domain of E coli FkpA is devoid of chaperone-like

function, although it shows PPIase activity [11,25]

Fur-thermore, it has been reported that human FKBP12

which intrinsically consists of a single domain, exhibited

lower activity for RNase T1substrate and higher activity

for tetrapeptide substrates than E coli FkpA [25]

How-ever, the reason why C-domain alone exhibits a weak

activity for protein substrates remains to be clarified

Further structural and functional studies of these

pro-teins will be required to clarify this reason

Experimental procedures

Cells and plasmids

Psychrotrophic bacterium Shewanella sp SIB1 was isolated

from water deposits in a Japanese oil reservoir [26] E coli

JM109 [recA1, supE44, endA1, hsdR17, gyrA96, relA1, thi,

D(lac-proAB) ⁄ F¢, traD36, proAB+, lacIq lacZDM15] was

obtained from Toyobo Co., Ltd (Kyoto, Japan) E coli

BL21(DE3) [F–, ompT, hsdSB (rB–, mB–), gal, dcm (DE3)]

and plasmid pET-28a were obtained from Novagen

(Madi-son, WI, USA) Plasmid pUC18 was obtained from Takara

Shuzo Co., Ltd (Kyoto, Japan) The E coli transformants

were grown in Luria–Bertani medium containing 50 mgÆL)1

ampicillin or 35 mgÆL)1kanamycin

Plasmid construction

Plasmid pSIB1-Nd, pSIB1-Cd, and pSIB1-a3+Cd for

over-production of a His-tagged form of the N-domain of SIB1

FKBP22 with entire a3 helix (N-domain+), C-domain

with-out a3 helix (C-domain–), and C-domain with entire a3 helix

(C-domain+), respectively, were constructed by ligating a

part of the SIB1 FKBP22 gene amplified by PCR into

pET-28a as follows Genomic DNA was prepared from a Sarkosyl

lysate of the Shewanella sp SIB1 cells [27] and used as a

tem-plate The gene encoding Met1–Asp94 of SIB1 FKBP22 was

amplified by PCR and ligated into the NdeI–SacI sites of

pET-28a to produce plasmid pSIB1-Nd Likewise, the genes

encoding Gly95–Ile205 and Gly47–Ile205 of SIB1 FKBP22 were amplified by PCR and ligated into pET-28a to produce plasmids pSIB1-Cd and pSIB1-a3+Cd, respectively The sequences of the 5¢ PCR primers were 5¢-AGAGAGAA TTCATATGTCAGATTTGTTCAG-3¢ for N-domain+,

AGAAAGC-3¢ for C-domain+

, where underlined bases show the position of the NdeI site The sequences of the 3¢ PCR primers were 5¢-GACTCTGAGCTCGTAATCTAGT CACGCTTA-3¢ for N-domain+, where underlined bases show the position of the SacI site, and 5¢- GGCCACT

and C-domain+, where underlined bases show the position

of the BamHI site PCR was performed with GeneAmp PCR system 2400 (PerkinElmer, Tokyo, Japan) using KOD polymerase (Toyobo Co., Ltd) according to the procedures recommended by the supplier

Overproduction and purification His-tagged forms of SIB1 FKBP22 (SIB1 FKBP22*) and

E coli FKBP22 (E coli FKBP22*) were overproduced and purified as described previously [6] N-domain+, C-domain–, and C-domain+ were overproduced in the

E coli BL21(DE3) cells transformed with plasmids

pSIB1-Nd, pSIB1-Cd, and pSIB1-a3+Cd, respectively, and puri-fied, as described for SIB1 FKBP22* [6], except for the purification of C-domain– For purification of C-domain–, which was overproduced in inclusion bodies, the cells were disrupted by sonication and centrifuged at 15 000 g for

30 min at 4C The pellet was dissolved in 20 mm sodium phosphate (pH 8.0) containing 6 m urea and 0.5% (w⁄ v) Triton X-100, and incubated overnight at 4C After cen-trifugation at 15 000 g for 30 min at 4C to remove insol-uble materials, the protein was refolded by dialysis against

20 mm sodium phosphate (pH 8.0), and purified as des-cribed for SIB1 FKBP22* using metal chelating affinity chromatography and gel filtration chromatography [6] Production of the recombinant proteins in the E coli cells, as well as their purities, were analyzed by SDS⁄ PAGE [28] on a 15 or 17% polyacrylamide gel, followed by stain-ing with Coomassie Brilliant Blue

Protein concentration Protein concentrations were determined from the UV absorption on the basis that the absorbance at 280 nm of

a 0.1% solution is 0.68 for SIB1 FKBP22*, 0.12 for N-domain+, 1.01 for C-domain–, 0.75 for C-domain+and 0.69 for E coli FKBP22* These values were calculated by

using ¼ 1576 m)1Æcm)1 for Tyr and 5225 m)1Æcm)1 for Trp at 280 nm [29] For N-domain+, which contains only one tyrosine residue and no tryptophan residues, a method

Trang 9

of Scopes [30] was used to confirm the accuracy of its

concentration In this method, the protein concentration

(mgÆmL)1) is calculated from A205nm⁄ (31 · b), where

A205nm represents absorbance at 205 nm and b represents

an optical path length (cm)

Molecular mass

The molecular masses of purified proteins were estimated by

gel filtration column chromatography using a Superdex 200

16⁄ 60 gel filtration column (Amersham Biosciences,

Piscat-away, NJ, USA) equilibrated with 50 mm Tris⁄ HCl (pH 8.0)

containing 50 mm NaCl Elution was performed at a flow

rate of 0.5 mLÆmin)1 Bovine serum albumin (67 kDa),

ovalbumin (44 kDa), chymotrypsinogen A (25 kDa), and

RNase A (14 kDa) were used as standard proteins

The molecular mass of N-domain+in solution was

deter-mined by sedimentation equilibrium analytical

ultracentri-fugation Sedimentation equilibrium experiments were

performed at 10C for 20 h with a Beckman Optima XL-A

Analytical Ultracentrifugate using an An-60 Ti rotor at a

speed of 28 000 r.p.m Before measurements, the protein

solutions were dialyzed overnight against 20 mm sodium

phosphate (pH 8.0) at 4C The initial loading

concentra-tion of the protein was 1.8 mgÆmL)1 The protein

concen-tration distribution within the cell was monitored by the

absorbance at 280 nm Analysis of the sedimentation

equili-bria was performed using the program xlavel (Beckman,

Tokyo, Japan, version 2)

Enzymatic activity

The PPIase activity was determined by protease-coupling

assay [31,32] and RNase T1 refolding assay [33] For the

protease-coupling assay, chymotrypsin was used as the

protease and N-succinyl-Ala-Leu-Pro-Phe-p-nitroanilide

(ALPF; Wako Chemicals, Osaka, Japan) was used as the

substrate The reaction mixture (2.1 mL) contained 35 mm

Hepes buffer (pH 7.8), 25 lm tetrapeptide substrate, and

the appropriate amount of the enzyme The reaction

mix-ture was incubated at reaction temperamix-ture (4, 10, 15 or

25C) for 3 min prior to the addition of chymotrypsin

The reaction was initiated by the addition of 30 lL of

0.76 mm chymotrypsin The isomerization reaction

cata-lyzed by PPIases was measured by monitoring the change

in the concentration of p-nitroaniline, because p-nitroaniline

is not released from the substrate when the peptide bond

N-terminal of the proline residue is in the cis conformation

The concentration of p-nitroaniline was determined from

the absorption at 390 nm with the molar absorption

coeffi-cient value of 8900 m)1Æcm)1 using a Hitachi U-2010

UV⁄ VIS spectrophotometer (Hitachi Instruments, Tokyo,

Japan) The catalytic efficiency (kcat⁄ Km) was calculated

from the relationship kcat⁄ Km¼ (kp– kn)⁄ E, where E

repre-sents the concentration of the enzyme, and kp and kn

represent the first-order rate constants for the release of p-nitroaniline from the substrate in the presence and absence of the enzyme, respectively [34]

For the RNase T1 refolding assay, RNase T1 was first unfolded by incubating the solution containing 50 mm Tris⁄ HCl (pH 8.0), 1 mm EDTA, 5.6 m guanidine hydro-chloride, and 16 lm RNase T1(Funakoshi, Tokyo, Japan) at

10C overnight Refolding was then initiated by diluting this solution 80-fold with 50 mm Tris⁄ HCl (pH 8.0) containing SIB1 FKBP22* or C-domian+ The final concentrations of RNase T1, SIB1 FKBP22*, and C-domian+ were 0.2 lm,

19 nm, and 21 or 210 nm, respectively The refolding reaction was monitored by measuring the increase in tryptophan fluorescence with an F-2000 spectrofluorometer (Hitachi Instruments) The excitation and emission wavelengths were

295 and 323 nm, respectively, and the band width was

10 nm The refolding curves were analyzed with double expo-nential fit [35] The kcat⁄ Kmvalues were calculated from the relationship described above, where kpand knrepresent the first-order rate constants for the faster refolding phase of RNase T1 in the presence and absence of the enzyme, respectively

Circular dichroism The CD spectra were recorded on a J-725 automatic spec-tropolarimeter from Japan Spectroscopic Co., Ltd (Tokyo, Japan) The proteins were dissolved in 20 mm sodium phos-phate (pH 8.0) and incubated for 30 min at the temperatures indicated prior to the CD measurement For measurement

of the far-UV CD spectra (200–260 nm), the protein concen-tration was approximately 0.2 mgÆmL)1 and a cell with an optical path length of 2 mm was used For measurement of the near-UV CD spectra (240–320 nm), the protein concen-tration was 0.4–1.0 mgÆmL)1and a cell with an optical path length of 10 mm was used The mean residue ellipticity, h, which has units of degÆcm2Ædmol)1, was calculated by using

an average amino acid molecular mass of 110

Differential scanning calorimetry DSC measurements were carried out on a high-sensitivity VP-DSC controlled by the vpviewerTM software package (Microcal, Inc., Northampton, MA, USA) at a scan rate of

1CÆmin)1 Prior to the measurements, samples were fil-tered through 0.22 lm pore size membranes and then de-gassed in a vacuum The protein concentrations during the measurements were  0.5 mgÆmL)1 The reversibility of thermal denaturation was verified by reheating the samples

Homology modeling

A model for dimeric structure of SIB1 FKBP22 was built

by SWISS-MODEL (Swiss Institute of Bioinfomatics)

Trang 10

[36,37] using the structure of L pneumophila MIP (PDB

ID: 1fd9) as a template

Acknowledgements

We thank K Ogasahara (Institute for Protein Research,

Osaka University) for use of Hitachi U-2010 UV⁄ VIS

spectrophotometer and microcal DSC, and Dr M

Morikawa for helpful discussions This work was

sup-ported in part by a Grant-in-Aid for National Project

on Protein Structure and Functional Analyses and by a

Grant-in-Aid for Scientific Research (No 16041229)

from the Ministry of Education, Culture, Sports,

Science and Technology of Japan, and by a research

grant from the Noda Institute for Scientific Research

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