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Tài liệu Báo cáo khoa học: Insights into the structure of plant a-type phospholipase D Susanne Stumpe, Stephan Konig and Renate Ulbrich-Hofmann ¨ ppt

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Tiêu đề Insights into the structure of plant a-type phospholipase D
Tác giả Susanne Stumpe, Stephan König, Renate Ulbrich-Hofmann
Trường học Martin-Luther University Halle-Wittenberg
Chuyên ngành Biochemistry and Biotechnology
Thể loại báo cáo khoa học
Năm xuất bản 2007
Thành phố Halle
Định dạng
Số trang 11
Dung lượng 629,48 KB

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The activity Keywords calcium binding; phospholipase D; small-angle X-ray scattering; stability; structure Correspondence R.. In this study, the isoenzyme form of phospholipase D from w

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Susanne Stumpe, Stephan Ko¨nig and Renate Ulbrich-Hofmann

Martin-Luther University Halle-Wittenberg, Institute of Biochemistry and Biotechnology, Halle (Saale), Germany

Phospholipase D (PLD; EC 3.1.4.4), which hydrolyzes

phospholipids to phosphatidic acid and the head group

alcohol, occurs in plants, microorganisms and animals

In plants, PLD isoenzymes play multiple regulatory

roles in diverse processes, including abscisic acid

signa-ling, programmed cell death, root hair patterning, root

growth, freezing tolerance, and other stress responses

[1] There is growing evidence for phosphatidic acid

being an intracellular lipid messenger in plants as well

as in mammals [2,3] Most PLDs also catalyze the

transphosphatidylation reaction in which the

phos-phatidyl moiety is transferred to a suitable alcohol In

biotechnology, this phospholipid-transforming reaction

has been exploited on a laboratory and industrial scale

[4]

In plants, multiple PLD genes encoding isoforms with distinct regulatory and catalytic properties have been identified [5,6] The most prevalent isoenzyme, which is responsible for the common PLD activity observed in leaves or seeds of plants, is the a-type PLD (PLDa) The conventional PLDa does not require phosphoinositides for activity when assayed

at millimolar levels of calcium ions It exhibits opti-mum activity at pH values between 5 and 6, and nonphysiologic high calcium concentrations between

30 and 100 mm [3,7,8] In contrast, the PLD isoen-zymes of the b, c, d and e types from Arabidopsis show highest activity at micromolar calcium concen-trations, and require the presence of phosphatidy-linositol 4,5-bisphosphate (PtdInsP2) [5] The activity

Keywords

calcium binding; phospholipase D;

small-angle X-ray scattering; stability; structure

Correspondence

R Ulbrich-Hofmann, Martin-Luther

University Halle-Wittenberg, Institute

of Biochemistry and Biotechnology,

Kurt-Mothes-Str 3, 06120 Halle (Saale),

Germany

Fax: +49 345 5527303

Tel: +49 345 5524864

E-mail: Renate.Ulbrich-Hofmann@

biochemtech.uni-halle.de

(Received 29 December 2006, revised 23

February 2007, accepted 20 March 2007)

doi:10.1111/j.1742-4658.2007.05798.x

Phospholipases D play an important role in the regulation of cellular pro-cesses in plants and mammals Moreover, they are an essential tool in the synthesis of phospholipids and phospholipid analogs Knowledge of phos-pholipase D structures, however, is widely restricted to sequence data The only known tertiary structure of a microbial phospholipase D cannot be generalized to eukaryotic phospholipases D In this study, the isoenzyme form of phospholipase D from white cabbage (PLDa2), which is the most widely used plant phospholipase D in biocatalytic applications, has been characterized by small-angle X-ray scattering, UV-absorption, CD and fluorescence spectroscopy to yield the first insights into its secondary and tertiary structure The structural model derived from small-angle X-ray scattering measurements reveals a barrel-shaped monomer with loosely structured tops The far-UV CD-spectroscopic data indicate the presence

of a-helical as well as b-structural elements, with the latter being dominant The fluorescence and near-UV CD spectra point to tight packing of the aromatic residues in the core of the protein From the near-UV CD signals and activity data as a function of the calcium ion concentration, two bind-ing events characterized by dissociation constants in the ranges of 0.1 mm and 10–20 mm can be confirmed The stability of PLDa2 proved to be sub-stantially reduced in the presence of calcium ions, with salt-induced aggre-gation being the main reason for irreversible inactivation

Abbreviations

PLD, phospholipase D; PLDa, a-type phospholipase D; PLDa2, isoenzyme form of phospholipase D from white cabbage; PpNp,

phosphatidyl-p-nitrophenol; PtdIns(4,5)P2, phosphatidylinositol 4,5-bisphosphate; SAXS, small-angle X-ray scattering.

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of plant PLDf is independent of calcium ions, but

the enzyme requires PtdInsP2 to selectively hydrolyze

phosphatidylcholine With the exception of PLDf,

which contains a Phox (PX) and a Pleckstrin (PH)

homology domain in the N-terminal region, all the

other PLD isoenzymes possess a calcium- and

phos-pholipid-binding domain (C2 domain) at the

N-ter-minus [5]

From white cabbage, the most traditional source of

PLD for biocatalytic phospholipid transformations,

two PLDs of the a type (PLD1 and PLD2) were

expressed in Escherichia coli and purified [8] The

amino acid sequence of PLD2, called PLDa2 in the

following, is identical with that of PLD isolated from

cabbage leaves [9] Figure 1A shows a schematic

pic-ture of the primary strucpic-ture of PLDa2 with the C2

domain and four conserved regions (I–IV) specific for

the PLD superfamily, where regions II and IV are two

copies of the HxKx4Dx6GSxN (HKD) motif [10,11]

The H, K and D residues of theses motifs are

abso-lutely conserved [11] As derived from the only crystal

structure of a PLD, the prokaryotic PLD from

Strep-tomyces sp strain PMF, the two HKD motifs form

one catalytic site [12] For comparison, Fig 1B,C

shows schemes of the primary structures for a

mam-malian and a microbial PLD, demonstrating that the

PLD-specific regions I–IV are present in all members

of the PLD superfamily However, there is low

similar-ity in the remaining parts of the molecules Most

mam-malian PLDs contain a PX and a PH domain instead

of the C2 domain in plants, whereas microbial PLDs

lack such probably regulatory domains

Despite the increasing amount of primary structural

data for PLDs, there is almost no information on the

secondary and tertiary structures of plant PLDs

Although Abergel et al reported the crystallization of

the cowpea PLD [13], no crystal structure has been

published so far Even reports on purified plant PLDs

are extremely rare Obviously, the biochemical and structural characterization of plant PLD enzymes has been hindered by their instability during and after purification from plant tissues [14,15] or the low yields

in recombinant protein production [16], respectively These difficulties were recently overcome by using

Ca2+-mediated hydrophobic chromatography [17] combined with recombinant PLD production in E coli [8] This purification method was also successfully applied to PLDa enzymes from soybean [18], cowpea [19], and poppy [20,21]

In the present study, the first insights into the secon-dary and tertiary structure of PLDa2 from cabbage are given The surface structure of the enzyme was investigated by small-angle X-ray scattering (SAXS) Further structural information was obtained by the spectroscopic characterization of PLDa2 in the native state The high instability of purified plant PLDs, as reported above, was shown to result from salt effects that can be eliminated in low-buffered solutions at room temperature From spectroscopic and activity measurements, two classes of calcium-binding events, with dissociation constants varying by at least two orders of magnitude, were derived

Results

PLDa2 preparation PLDa2 was produced according to Scha¨ffner et al [8] with slight modifications as described in Experi-mental procedures, which improved the yield of active enzyme The amount of homogeneous PLDa2 obtained was 3.5–5.0 mg per liter of cell culture The specific activity towards the synthetic substrate phos-phatidyl-p-nitrophenol (PpNp) was 10.2–14.7 UÆmL)1, which is consistent with the activity of PLDa2 in pre-vious preparations [8]

A

C B

Fig 1 Scheme of the primary structure of

PLDs (A) PLDa2 from cabbage (P55939).

(B) PLD1 from human (Q13393) (C) PLD

from Streptomyces sp (1V0YA) The

N-terminal C2 domain (A), the PX and PH

domains (B) and the four PLD specific

con-served regions (I–IV) are marked Regions II

and IV represent the two HKD motifs

form-ing the active site In (A), the positions of

the 30 tyrosine and 15 tryptophan residues

are marked by stars.

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Structural information from SAXS

Scattering measurements with synchrotron radiation

were performed at pH 7.0 with 2 and 4.7 mgÆmL)1

PLDa2 A typical SAXS profile of PLDa2 is shown

for 4.7 mgÆmL)1in Fig 2A From scattering intensities

I(0), a molecular mass of 97 kDa was calculated (using

BSA as standard), which is in accordance with

a monomer of PLDa2 Correspondingly, no

aggre-gates were detected at a PLDa2 concentration of

0.05–0.2 mgÆmL)1 in size exclusion chromatography

The molecular mass deduced from the amino acid

sequence is 91.9 kDa, whereas the molecular mass

determined by size exclusion chromatography was

85.8 kDa (data not shown) The radius of gyration Rg

(2.87 ± 0.02 nm) extracted by gnom [22] from the

scattering data was in good agreement with the Rg

value estimated by primus [23] from the Guinier plots

(2.89 ± 0.01 nm) and is in the typical range for a

spherical particle The bell-shaped distance distribution

function illustrates the quality of the experimental data

(Fig 2B)

Reconstruction of the overall shape of the PLDa2

from the X-ray scattering data was achieved by the

ab initiomodeling program dammin [24] The

superpo-sition of the 10 calculated models (Fig 3) shows a

longish molecule with loosely structured apical and

basal regions The lid-like region (Fig 3, left) can be

construed as a separate domain, but was not explicitly

visible in all individual models The Porod volume

(volume of the hydrated solute particle) of the

low-resolution models averages 126.7 ± 3.5 nm3

Structural information from spectroscopy

UV absorption spectra (Fig 4A) show a maximum at

280 nm, with a slight shoulder at 295 nm assigned

to the tryptophan residues The absence of absorption

in the UV region > 310 nm, characteristic for light scattering of high molecular mass species, provides no

Fig 2 SAXS profile (A) and distance distribution function (B) of PLDa2 (A) Experimental data are indicated by open circles The solid line shows the scattering curve fitted by the program GNOM

[22] The PLDa2 concentration was 4.7 mgÆmL)1.

Fig 3 Ab initio low-resolution structure model of PLDa2 calculated from the SAXS pattern The balls represent the dummy atoms used in the simulated annealing procedure of program DAMMIN [24] to restore the models The model resulting from superposition of 10 individual models is shown in three different views obtained by 90 rotation around the y-axis (middle) and the z-axis (right).

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evidence for aggregates, and reconfirms the size

exclu-sion chromatography results

The fluorescence spectra have an emission

wave-length maximum at 334 nm and refer to a hydrophobic

environment for most or all tryptophan side chains

(Fig 4B) The similar shape and fluorescence emission

maxima of the spectra at both excitation wavelengths

(278 and 295 nm) indicate a complete resonance energy

transfer from the tyrosine to the tryptophan residues

The secondary structure of PLDa2 was investigated

by far-UV CD spectroscopy (Fig 4C) The far-UV

CD spectrum of PLDa2 exhibits: (a) a sharp maximum

at 192 nm; and (b) a wide minimum between 208

and 220 nm The a-helix and b-strand contents of the

protein were calculated with the online programs

dichroweb [25] and k2d [26], respectively With the

program k2d, the b-sheet content (0.45) was higher

than the a-helix content (0.08), whereas the program

dichroweb computed secondary structure contents

with 0.20 a-helix, 0.28 b-sheet, and 0.21 turn

confor-mation Both methods agreed in indicating more

b-sheet than a-helix content

The near-UV CD spectrum of native PLDa2 (250–

300 nm, Fig 4D), describing the chiral environment of

the aromatic amino acid side chains, has a defined

structure that presents two sharp minima at 288 and

295 nm, and two maxima at 274–283 nm (wide) and

290 nm (sharp)

Storage stability and aggregation propensity

The instability of the purified enzyme described in the

literature [14,15] prompted us to analyze the

inactiva-tion of PLDa2 under selected condiinactiva-tions Storage at lower temperatures (0–10 C) resulted in faster inacti-vation of the enzyme than at room temperature (23C) Under physiologic conditions (pH 7.0 and an ionic strength of 150 mm, adjusted with sodium chlor-ide), as well as under conditions where the enzyme is most active (pH 5.5 and 40–100 mm calcium chloride), PLDa2 was more rapidly inactivated than in the absence of higher salt concentrations In Table 1, the rate constants of irreversible inactivation, which fol-lowed first-order kinetics, in the absence and presence

of NaCl and CaCl2at pH 5.5 and 23C are compared The results show that the instability of PLDa2 is

B

C

A

D

Fig 4 Spectra of native PLDa2 (A) UV

absorbance spectrum (B) Fluorescence

emission spectra with excitation at 278 nm

(black) and 295 nm (gray) (C) Far-UV CD

spectrum (D) Near-UV CD spectra in the

absence (black) and the presence of

100 m M CaCl2(gray) All spectra were

obtained in 50 m M sodium acetate buffer

(pH 5.5) at 20 C The PLDa2 concentrations

were 253 lgÆmL)1(A), 25 lgÆmL)1(B), and

1 mgÆmL)1(C, D), respectively.

Table 1 Influence of salts on the observed first-order rate con-stants (kobs) of PLDa2 inactivation and fluorescence decrease PLDa2 was incubated in 50 m M sodium acetate buffer (pH 5.5) at

23 C To follow the inactivation, PLDa2 (280 lgÆmL)1) was incuba-ted for 5 min to 36 days, and the residual activity was measured after dilution to 9.3 lgÆmL)1 as described in Experimental proce-dures The fluorescence intensity of PLDa2 (25 lgÆmL)1) was measured at an excitation wavelength of 278 nm and an emission wavelength of 335 nm NM, not measurable.

Additive

kobs(10)7Æs)1)

Inactivation

Fluorescence decrease

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caused by high ionic strength rather than by specific

ionic effects At comparable ionic strengths of sodium

and calcium chloride, the observed kinetic constants

were nearly identical Interestingly, however, the

inacti-vation could be further decreased by the addition of

EDTA; inactivation constants were no longer

measur-able At room temperature, the loss of activity in

slightly buffered solutions (10 mm Pipes, pH 7.0, or

50 mm sodium acetate, pH 5.5) with 10 mm EDTA

amounted to only 17% after 5 months

When we looked for spectroscopic alterations in

the course of inactivation, neither sodium chloride nor

calcium chloride was found to induce spectroscopic

changes in the absorption, fluorescence or far-UV CD

spectra (data not shown) Interestingly, near-UV CD

spectroscopy revealed changes in the presence of

cal-cium chloride (Fig 4D), but not in the presence of

sodium chloride Therefore, the spectroscopic

altera-tions could stem from specific calcium binding rather

than from nonspecific salt effects (see next paragraph)

Although no shift of the fluorescence emission

max-ima was measurable, the fluorescence intensity

decre-ased with increasing incubation time (data not shown)

Also, the decrease of the fluorescence signal followed

a first-order reaction, and allowed us to determine

rate constants (Table 1) These constants, determined

at about 10-fold lower protein concentration than

the measurements of inactivation, show the same

trends with respect to the effects of NaCl, CaCl2 and

EDTA as the inactivation constants As shown

by SDS⁄ PAGE (Fig 5), the decrease in fluorescence

intensity was caused by precipitation of PLDa2, which

is faster in the presence of salts

Calcium binding

Whereas calcium ions did not change the absorption,

fluorescence and far-UV CD spectra of native PLDa2,

the near-UV CD signal in the range 258–292 nm was

increased in the presence of calcium chloride, with a maximum at 280 nm (Fig 4D) The increase in

near-UV CD intensity was specific for calcium ions, as neither sodium nor magnesium ions showed any com-parable effect The increase in the near-UV CD signal

at 280 nm was dependent on the concentration of calcium ions in a hyperbolic fashion (Fig 6A) The data could be fitted well using a double hyperbolic function yielding two dissociation constants, KD1¼ 10.24 mm and KD2¼ 0.123 mm Two binding events are also evident in a Scatchard-like plot [27], where the relative change in the near-UV CD signal (DF) repre-sents the amount of the Ca2+–PLDa2 complexes (Fig 6B) Calcium ions are crucial for PLDa2 activity, and could not be replaced by other ions such as mag-nesium ions At concentrations of calcium ions

< 1 mm, no significant activity could be detected Up

to 100 mm, PLDa2 activity increased with increasing concentration of calcium ions, independent of the counterion, chloride or acetate (Fig 7A) At calcium ion concentrations above 100 mm, the PLDa2 activity dropped again, and the decrease was steeper with cal-cium acetate than with calcal-cium chloride Interestingly, the activity data in the range 0.01–100 mm CaCl2 could be fitted in similar way as the near-UV CD data, using a double hyperbolic function (Fig 7B) The resulting dissociation constants were KD1¼ 17.38 mm and KD2¼ 0.073 mm A modified Scatchard plot

of these data, with DA being the change in relative activity (Fig 7C), shows two linear parts, indicating that at least two separate calcium-binding events affect PLDa2 activity

A

B

Fig 5 Kinetics of PLDa2 precipitation followed by SDS ⁄ PAGE.

PLDa2 (280 lgÆmL)1) was incubated in 50 m M sodium acetate

buf-fer (pH 5.5) in the absence (A) and the presence of 300 m M NaCl

(B) at 23 C After 0 min, 5 min, 30 min, 1 h, 2 h, 4 h, 8 h, 1 day,

2 days, 3 days and 4 days (lanes 1–11), samples were analyzed by

SDS ⁄ PAGE Lane 12 shows the protein band in the precipitate

after 1 week of incubation.

B A

Fig 6 Calcium binding measured by near-UV CD spectroscopy (A) Direct plot The solid line shows the double hyperbolic fit (B) Modi-fied Scatchard plot The CD signals, measured at different concen-trations of CaCl 2 , were taken at 280 nm and averaged over 5 min The PLDa2 concentration was 1 mgÆmL)1 DF corresponds to the change in the CD signal [Q] MRW (degÆcm 2 Ædmol)1) at 280 nm.

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PLDa2 is a barrel-shaped monomer with loosely

structured tops

Despite the great number of plant PLDs identified at

the DNA or cDNA level, only a few of these enzymes

have been characterized in purified, isolated form

Cor-respondingly, there is almost no information on the

secondary and tertiary structures of plant PLDs

Simi-larly, structural information on other eukaryotic PLDs

is rare

The two members of the PLD superfamily whose

crystal structures have been elucidated [28,29] are

much smaller in size, so that knowledge of their

struc-tures cannot be generalized to plant PLDs In this

art-icle, the first information on the spatial structure of a

plant a-type PLD has been obtained on the basis of

recombinantly produced PLDa2 from cabbage SAXS

analysis (Fig 2) and analytic size exclusion

chromato-graphy indicate unequivocally that native PLDa2 from

cabbage is a monomeric protein The surface structure

of PLDa2 indicates a longish molecule with loosely

structured regions at the two ends of the molecule

(Fig 3) An assignment of these relaxed structures to

sequence regions of PLDa2 has not yet been possible

According to the volume estimation on the basis of the

partial specific volume of a protein (0.73 mgÆg)1) [30],

the C2 domain comprising residues A2 to E153 should

occupy 16% of the molecular volume, and therefore

seems too large to represent the lid-like structure at

the top of the left view in Fig 3 We speculate that the

loosely structured region on the opposite side belongs

to the C2 domain (141 amino acids) with its extended

loops, whereas the lid-like region at the top represents

another flexible part of the structure Assuming that

the core protein containing the two essential HKD

motifs (Fig 1) is similar in PLDa2 from cabbage (812 amino acids) and in PLD from Streptomyces sp (506 amino acids) with the known crystal structure [29], the C-terminal part of the plant enzyme is longer by approximately 60 amino acids and might form this part A PtdInsP2-binding domain, which has recently been desribed as a separate folding unit conserved in eukaryotic PLDs and comprises about 50 amino acids between the two HKD motifs [31], would also fit this lid-like region

The loosely structured parts of the molecule and the deviation from a spherical shape may be the reason why the experimentally determined Porod volume of PLDa2 (126.7 ± 3.5 nm3) is slightly larger than the molecular volume (111.45 nm3) calculated from the partial specific volume of a protein [30] This result is

in accordance with the smaller volume (99 nm3) deduced from the radius of gyration (Rg: 2.9 nm), which considers the distances between scattering mas-ses of the molecule

Spectroscopic properties of PLDa2 reflect an ordered tertiary structure with a high content of b-structure

The first UV-absorption (Fig 4A), fluorescence (Fig 4B) and CD spectra (Fig 4C,D) of a plant PLD reflect the properties of a common protein Obviously, tyrosine, and particularly tryptophan, residues (Fig 1) dominate the absorption spectra of PLDa2 from cab-bage, with a maximum at 280 nm (Fig 4A) The fluor-escence spectra of PLDa2 with a maximum at 334 nm (Fig 4B) indicate a hydrophobic environment for most

or possibly all tryptophan residues Therefore, trypto-phan residues are probably mainly located in the core

of the protein The tyrosine residues contribute to the fluorescence spectra by fluorescence resonance energy

A

C B

Fig 7 Influence of the calcium concentration on PLDa2 activity (A) Relative activity as function of calcium chloride (black) and calcium acet-ate (gray) concentration, respectively (B) Double hyperbolic plot of the data from (A) in the range 0–100 m M Ca2+ (C) Modified Scatchard plot of the data from (B) DA corresponds to the change in relative activity The PLDa2 activity was measured against PpNp in sodium acet-ate buffer (pH 5.5) at 30 C.

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transfer This energy transfer seems to be very effective

in PLDa2, because no separate tyrosine fluorescence is

detectable

The far-UV CD spectrum of PLDa2 with the

maxi-mum at 192 nm and the broad minimaxi-mum at 208–

220 nm (Fig 4C) refers to both a-helix and b-sheet

conformations As the signal of a-helices is more

intense [32], the spectrum suggests that b-sheet

structures dominate This assumption was confirmed

by the calculation of the a-helix and b-strand contents

of the protein with the online programs dichroweb

[25] and k2d [26], respectively

The well-structured near-UV CD spectrum of PLDa2

(Fig 4C) points to a tertiary structure with tight

pack-ing of the aromatic side chains in an asymmetric

envi-ronment As all eight cysteine residues of PLDa2 should

be half-cysteines [33], no influence of disulfide bonds on

the near-UV CD spectrum must be taken into account

The relatively low signal intensity can probably be

attributed to the compensation of positive and negative

signals of the individual aromatic residues

PLDa2 is stable at low ionic strengths

The low stability of purified cabbage PLD was shown

to originate from a high aggregation propensity of the

enzyme under physiologic conditions Inactivation and

precipitation of PLDa2, the latter being followed by

SDS⁄ PAGE or decreasing fluorescence intensity, were

accelerated with growing salt concentrations (Table 1,

Fig 5) In the comparison of the presence of NaCl

and of CaCl2, the ionic strength was more important

for inactivation or precipitation than the individual

ions Hydrophobic interactions, which are known to

be favored by rising salt concentrations, are probably

the reason for this tendency The fact that EDTA

effects a marked stabilization (Table 1), however,

indi-cates an additional destabilizing effect by calcium ions

Destabilization of PLDa2 by calcium ions was also

indicated by the proteolytic sensitivity of PLDa2 [34]

Calcium-induced decrease of stability and biological

activity due to facilitated aggregation was also

repor-ted for a-crystallin [35]

Although the incubation with salts in the

inactiva-tion experiments was performed at higher PLDa2

con-centrations than in the fluorescence measurements, the

observed inactivation was slower than the observed

fluorescence decrease due to protein precipitation This

discrepancy could be due to the different experimental

conditions Whereas the fluorescence decreases were

measured in situ, the remaining activities were

deter-mined after dilution, and therefore partial

resolubiliza-tion of precipitates is possible We assume that the

precipitation is followed by (small) structural altera-tions in a consecutive aggregation reaction that cause irreversible inactivation

It is not clear whether the destabilizing effects of calcium ions and other salts have any physiologic rele-vance However, the finding that pure plant PLDs may

be more stable in the absence of calcium and other ions

at room temperature than in their presence and at lower temperatures is of considerable practical importance

PLDa2 binds calcium ions at two affinity levels

CD spectroscopy in the near UV-region proved to be the only spectroscopic method able to detect specific binding of calcium ions to PLDa2 (Fig 4D) The sig-nal increases in this spectrum caused by calcium ions indicate stiffening of the PLDa2 molecule Binding curves obtained with this method (Fig 6A) are similar

to the curves of PLDa2 activity as a function of cal-cium ion concentration (Fig 7B), showing that the well-known effect of calcium ions on activity closely correlates with conformational changes of the enzyme These results unambiguously show that activation of PLDa2 by calcium ions is due to the binding of cal-cium ions to the enzyme, and not (or not only) to bet-ter structuring of the substrate aggregates

From both the CD and the activity data, two differ-ent calcium-binding evdiffer-ents can be derived The corres-ponding dissociation constants differ by about two orders of magnitude Even the higher affinity (with the dissociation constant in the range of 0.1 mm) is still relatively low for biospecific interactions We assume that calcium ions are involved in enzyme activation by guiding the protein to the membrane, mediating sub-strate binding, or adjusting the charge distribution at the active site Unfortunately, the number of calcium ions bound to the enzyme cannot be deduced from these data The binding event with the dissociation constant in the range of 0.1 mm might be associated with calcium binding to the C2 domain For the sepa-rately expressed C2 domain of PLDa from Arabidopsis thaliana, one to three low-affinity calcium-binding sites with dissociation constants in the range of 0.5 mm were estimated from isothermal titration calorimetry [36] The C2 domains of other proteins showed cal-cium-binding affinities in the range of 1–50 lm [37,38]

As the C2 domain of PLDa2 from cabbage lacks two conserved residues that are probably responsible for the calcium binding [8], we hypothesize that this bind-ing event takes place at the C2 domain

A second calcium-binding site of lower affinity at the C2 domain (corresponding to the dissociation constant in the range 10–20 mm) cannot be excluded It

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is more likely, however, that the calcium-binding event

of lower affinity is attributable to the catalytic site of

PLDa2, as found for PLDb from A thaliana [39]

The decrease in PLD activity at concentrations

above the optimal calcium concentration (100 mm),

as demonstrated in Fig 7A, is scarcely reported in the

literature [7] In contrast to the activation effect of

calcium ions, inactivation at high calcium ion

concen-trations is dependent on the counterion In contrast

to the stabilizing effects of salts according to the

Hofmeister series, the chloride salt is less destabilizing

than the acetate salt As discussed above, the

inactiva-tion by salts is connected with aggregainactiva-tion and

precipi-tation of PLDa2 Obviously, the anion is specifically

involved in this process

In summary, we conclude that calcium ions bind

specifically at two sites of PLDa2 and activate the

enzyme in two steps As discussed above, the resulting

conformational changes destabilize the molecule

How-ever, at higher salt concentrations, precipitation

occurs, and destabilization by calcium ions is therefore

no longer specific

Experimental procedures

Materials

Bactotryptone and yeast extract were from Difco (Detroit,

MI, USA) All other chemicals were the purest ones

com-mercially available

Production of PLDa2

The E coli strain BL21 (DE3) containing plasmids pUBS520

and pld2pRSET5a [8] was grown without preculture in a

200 mL culture of 2· YT medium (2% bactotryptone, 1%

yeast extract, and 1% NaCl, pH 7.0) with 100 lgÆmL)1

amp-icillin and 50 lgÆmL)1 kanamycin at 30C for 15 h At an

absorbance of 1–2 at 600 nm, the temperature was shifted to

15C and the cells were grown to maximum cell density (24–

48 h) without induction Cells were harvested by

centrifuga-tion at 4C and 6000 g for 10 min (Avanti J-25 centrifuge,

Beckman Coulter, JA-10 rotor), and stored at) 20 C

Purification of PLDa2

The pellet from a 1.2 L culture was suspended in 37 mL of

buffer (30 mm Pipes, pH 6.2, 10 mm EDTA), and the cells

were disrupted by high-pressure homogenization (APV

Ho-mogeniser; Gaulin, Lu¨beck, Germany) The cell debris was

separated by centrifugation at 4C and 48 000 g for

20 min (Avanti J-25 centrifuge, JA-30.50 rotor) Calcium

chloride was added to the supernatant (final concentration

50 mm), and after centrifugation (at 4C, 4800 g, 10 min, Rotofix 32 centrifuge, Hettlich, 1620A rotor), the protein solution was loaded onto an Octylsepharose column (Amersham Biosciences, Piscataway, NJ, USA) equilibrated with 30 mm Pipes (pH 6.2) containing 50 mm CaCl2 The column was carefully washed with equilibration buffer, and then the protein was eluted with 0.1 mm EDTA in 5 mm Pipes buffer (pH 6.2) The PLDa2-containing fractions were pooled and Tris⁄ HCl buffer (pH 7.5) was added to a final concentration of 20 mm After filtration (0.2 lm; WiCom, Heppenheim, Germany), the solution was applied

to a Source 15Q column (Amersham Biosciences) Elution was performed using a linear gradient of 50 mL of 15–35%

1 m NaCl in Tris⁄ HCl buffer (pH 7.5)

The fractions with highest catalytic activity and homo-geneity in SDS⁄ PAGE were pooled, dialyzed twice (cut-off

20 kDa; Roth, Karlsruhe, Germany) against a 100-fold vol-ume of 10 mm Pipes buffer (pH 7.0), and stored at) 20 C

Determination of protein concentration The concentration of PLDa2 in the range between

75 lgÆmL)1 and 1 mgÆmL)1 was determined spectrophoto-metrically, using the molar extinction coefficient e280 nm¼

123 720 m)1Æcm)1 [40] Other PLDa2 concentrations were measured by the BCA assay (Pierce, Rockford, IL, USA) with BSA as standard

SDS⁄ PAGE SDS⁄ PAGE was performed according to the method of Laemmli [41] Gels [10% (w⁄ v) acrylamide] were stained with Coomassie Brilliant Blue G250 and quantified by densitometric evaluation at 595 nm (CD60; Desaga, Darm-stadt, Germany)

Small angle X-ray solution scattering with synchrotron radiation

Data were collected with the EMBL beamline X33 at the DORIS storage ring, Desy, Hamburg Measurements were performed at a camera length of 2 m, using a Mar345 image plate detector (Marresearch, Norderstedt, Germany),

at a wavelength of 1.5 A˚, a temperature of 12C, and PLDa2 concentrations between 2 and 4.7 mgÆmL)1 in

10 mm Pipes buffer (pH 7.0) Calibration of the momentum transfer axis (s) was done using collagen or tripalmitin as standards The experimental data were normalized to the intensity of the incident beam and corrected for the detec-tor response, the buffer scattering was substracted, and the statistical errors were calculated using the program primus [23] To obtain the forward scattering intensity I(0) and the radius of gyration (Rg), the data were processed with the program gnom [22] The molecular mass was calculated

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from the ratio of the forward scattering intensity of the

sample and that of the molecular mass standard BSA The

ab initio deconvolution of the SAXS profiles to restore a

low-resolution shape of PLDa2 from the experimental data

was executed using the program dammin [24] The final

model was computed by superposition of 10 individual

models using the program damaver [42]

Size exclusion chromatography

A Superdex 200 HR 10⁄ 30 FPLC column (Amersham

Bio-sciences) was equilibrated with 10 mm Pipes buffer (pH 7.0)

and 140 mm NaCl Proteins were eluted with the same

buf-fer at a flow rate of 0.5 mLÆmin)1at 4C, and detected by

the protein absorbance at 280 nm Aldolase (150 kDa),

ovalbumin (45 kDa), chymotrypsinogen A (25 kDa), and

cytochrome c (12.3 kDa) (Serva, Heidelberg, Germany)

were used as molecular mass standards

Absorption and CD spectroscopy

A Jasco V-560 spectrophotometer (Jasco, Gross-Umstadt,

Germany) and a 10 mm quartz cuvette were used in UV

absorption measurements CD spectra were obtained using

a Jasco J-810 spectropolarimeter The protein spectra were

measured in 10 mm (near-UV) and 0.1 mm (far-UV) quartz

cuvettes by scanning at 20 nmÆmin)1 with a resolution of

0.1 nm, a response time of 1 s, a bandwidth of 1 nm, and a

temperature of 20C An average of 10 scans was recorded

and corrected by subtracting the baseline spectrum of the

buffer The CD signal was converted to molar ellipticity

[Q]MRW(degÆcm2Ædmol)1) [43]

The ellipticity at 280 nm was used for monitoring

cal-cium binding The CD signal was recorded over 5 min

Then, calcium ions were added stepwise, and the CD signal

was recorded again The measured signal was corrected for

the protein dilution by calcium chloride addition

Fluorescence spectroscopy

Fluorescence experiments were performed at 20C with

a FluoroMax-2 spectrofluorimeter (Horiba Jobin Yvon,

Munich, Germany) using 10· 4 mm fluorescence quartz

cuvettes PLDa2 was excited at 278 nm (excitement of

tyrosine and tryptophan residues) or at 295 nm (excitement

of tryptophan residues only) The slit width was 5 nm for

excitation and emission The signal was acquired with a

res-ponse time of 1 s, and the wavelength increment was 1 nm

The fluorescence signal of the blank buffer was substracted

Enzyme assays

The hydrolytic activity of PLDa2 was determined by

meas-uring the p-nitrophenol release from PpNp (synthesized as

described by D’Arrigo et al [44]) at 405 nm [8] In general, PLDa2 was incubated in 220 lL of 65 mm sodium acetate buffer (pH 5.5) containing 50 mm CaCl2at 30C With the addition of the substrate solution [10 mm PpNp, 5% Triton X-100 (v⁄ v), and 5 mm SDS], the reaction was started After 10 min of incubation, which is in the linear range of the progress curve, the reaction was stopped with 60 lL of

1 m Tris⁄ HCl buffer (pH 8.0) containing 0.1 m EDTA One unit (U) of PLDa2 corresponds to the release of 1 lmol p-nitrophenolÆmin)1

Acknowledgements

The authors thank Ch Kuplens and Dr R Scho¨ps for assistance with protein purification and for preparation

of the PpNp The financial support of the Kultus-ministerium des Landes Sachsen-Anhalt and the Graduiertenkolleg 1026 of the Deutsche Forschungsge-meinschaft, Bonn (Germany), and the support of the European Community, Research Infrastructure Action under the FP6 ‘Structuring the European Research Area Specific Programme’ to the EMBL Hamburg Outsta-tion, Contract Number RII3-CT-2004-506008, are gratefully acknowledged

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