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Tiêu đề Role of the surface charges D72 and K8 in the function and structural stability of the cytochrome c6 from Nostoc sp. PCC 7119
Tác giả Christian Lange, Irene Luque, Manuel Hervás, Javier Ruiz-Sanz, Pedro L. Mateo, Miguel A. De la Rosa
Trường học Martin-Luther-Universität Halle-Wittenberg
Chuyên ngành Biochemistry
Thể loại Scientific report
Năm xuất bản 2005
Thành phố Halle
Định dạng
Số trang 11
Dung lượng 786,06 KB

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A series of mutant forms was generated to span the possible combinations of charge neutralization by mutation to alanine and charge inversion by mutation to lysine and aspartate, respect

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and structural stability of the cytochrome c6 from Nostoc

sp PCC 7119

Christian Lange1, Irene Luque2, Manuel Herva´s1, Javier Ruiz-Sanz2, Pedro L Mateo2and

Miguel A De la Rosa1

1 Instituto de Bioquı´mica Vegetal y Fotosı´ntesis, Centro de Investigaciones Cientı´ficas Isla de la Cartuja, Seville, Spain

2 Departamento de Quı´mica Fı´sica e Instituto de Biotecnologı´a, Universidad de Granada, Spain

In the oxygenic photosynthesis of cyanobacteria and

many unicellular algae, cytochrome c6 acts as a soluble

electron carrier between the cytochrome bf complex and

photosystem I (PS I) [1,2] In recent years, considerable

efforts have been undertaken to gain insight into the

structure–function relationships of this small heme

protein [3–7] The structures of the cytochromes c6from

various organisms have been determined [8–14] Study

of the mutant series has contributed to our

understand-ing of the functional roles of important individual

amino acid residues within the protein [15–17] NMR studies with mutant bacterial c-type cytochromes [18– 20] have provided important insights into the role of heme–protein interactions for the structural stability of this class of proteins

The mutant D72K of cytochrome c6 from Nostoc (formerly Anabaena) sp PCC 7119 (cyt c6) [21], was found to be a more reactive electron donor towards

PS I than the wild-type [16] However, D72K was shown to have considerably reduced stability against

Keywords

cytochrome c 6 ; electron transfer;

electrostatic interactions; protein folding;

protein stability

Correspondence

Christian Lange, Martin-Luther-Universita¨t

Halle ⁄ Wittenberg, Institut fu¨r

Biotechnologie, Kurt-Mothes-Str 3,

06120 Halle (Saale), Germany

Fax: +49 345 552 7013

Tel: +49 345 552 4948

E-mail: christian.lange@biochemtech.

uni-halle.de

(Received 10 February 2005, revised 21

April 2005, accepted 3 May 2005)

doi:10.1111/j.1742-4658.2005.04747.x

We investigated the role of electrostatic charges at positions D72 and K8

in the function and structural stability of cytochrome c6 from Nostoc sp PCC 7119 (cyt c6) A series of mutant forms was generated to span the possible combinations of charge neutralization (by mutation to alanine) and charge inversion (by mutation to lysine and aspartate, respectively) in these positions All forms of cyt c6 were functionally characterized by laser flash absorption spectroscopy, and their stability was probed by urea-induced folding equilibrium relaxation experiments and differential scan-ning calorimetry Neutralization or inversion of the positive charge at position K8 reduced the efficiency of electron transfer to photosystem I This effect could not be reversed by compensating for the change in global charge that had been introduced by the mutation, indicating a specific role for K8 in the formation of the electron transfer complex between cyt c6 and photosystem I Replacement of D72 by asparagine or lysine increased the efficiency of electron transfer to photosystem I, but destabilized the protein D72 apparently participates in electrostatic interactions that stabil-ize the structure of cyt c6 The destabilizing effect was reduced when aspar-tate was replaced by the small amino acid alanine Complementing the mutation D72A with a charge neutralization or inversion at position K8 led to mutant forms of cyt c6 that were more stable than the wild-type under all tested conditions

Abbreviations

cyt c 6 , cytochrome c 6 from Nostoc sp PCC 7119; DSC, differential scanning microcalorimetry; E mpH 7, midpoint redox potentials at pH 7 and

at 25 C; DG int , interaction Gibbs energies; kbim, bimolecular reaction rate constant; N, native folded state; PS I, photosystem I; U, ensemble

of unfolded states; [urea] 50 , transition midpoint for urea-induced unfolding.

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unfolding by urea [22], and preliminary experiments

indicated that its thermal stability was affected in a

similar way Electrostatic interactions play a critical

role in guiding and stabilizing functional

protein–pro-tein interactions [6], as well as in the structural stability

of proteins [23–25]

Inspection of a preliminary structural model of

cyt c6, based on the known structure of cytochrome c6

from Synechococcus elongatus [11] and NMR data,

revealed a spatial proximity between the side chain of

D72, which is located in the C-terminal a helix, and a

positively charged residue in the protein’s N-terminal

helix, K8 In S elongatus cytochrome c6, the conserved

residues K8 and D72 are located near the crossing

region of the helices, and the Nx atom of K8 is found

at a distance of 6.2 A˚ from the nearest side-chain

oxy-gen of D72

Taking the functionally and structurally interesting

mutant D72K as a material starting point, we aimed

to study the contribution of the electrostatic charges at

positions D72 and K8 to the interaction of cyt c6 with

PS I, as well as to its structural stability For this

pur-pose, a series of mutant forms of cyt c6 was generated

that spans the possible combinations of charge

neutral-ization (by mutation to alanine) and charge inversion

(by mutation to lysine and aspartate, respectively) at

positions D72 and K8 After functional

characteriza-tion by laser-flash absorpcharacteriza-tion spectroscopy,

urea-induced folding equilibrium relaxation experiments

and differential scanning microcalorimetry (DSC) were

used to assess the changes in the stability against

denaturant-induced folding⁄ unfolding as well as against

thermal unfolding

Results and Discussion

Functional characterization of wild-type cyt c6

and its mutants

Wild-type cyt c6 and its mutant forms were

success-fully expressed in Escherichia coli strain GM119 and

purified to homogeneity The UV⁄ Vis spectra of

wild-type and mutants were virtually identical (not shown)

Their midpoint redox potentials at pH 7 (EmpH 7) were

very similar throughout (Table 1), as expected for the

mutation of surface residues located far from the heme

moiety Thus, the thermodynamic driving force for the

reaction of cyt c6 with PS I was essentially unaltered

by the introduction of the mutations Eventual

differ-ences in reactivity, therefore, have to be ascribed to

structural factors that influence the formation and

productivity of the encounter complex Indeed, such

differences were observed All forms of cyt c6 were

highly active electron donors to PS I (Fig 1) The determined values for the bimolecular rate constant (kbim) for wild-type cyt c6 and the mutant D72K were

in excellent agreement with the values that had been reported previously [16] Overall, a good correlation (R¼ 0.83) between the proteins’ net charge and their reactivity towards PS I was observed (Fig 1) This confirms the importance of long-range charge interac-tions for the electron carrier function of cyt c6 How-ever, closer inspection of the data revealed interesting deviations from the general trend

A reversal of the charge effect of the mutation K8D

in the mutant D72K⁄ K8D did not lead to recovery of wild-type reactivity The same holds for the mutant pair K8A and D72A⁄ K8A All three variants carrying the mutation K8D showed very similar kbim values, and the same was observed for all variants carrying

Table 1 Redox potentials of wild-type cyt c6and its mutant forms.

EmpH 7 (mV)

0 5 10 15 20 25 30

WT

K8D

D72K

D72N D72A KA KD

AA AD

k bim

7 M

-1 s

-1 )

relative nominal charge

K8A

Fig 1 Bimolecular rate constants, k bim , for the reduction of PS I The kbimvalues were determined as described in the text Data points are marked with the name of the corresponding mutants Error bars represent errors from the fit to determine k bim The solid line represents a linear fit to the data points, dashed lines mark the 95% confidence intervals Double mutants are abbreviated with the first letter representing the residue at position 72 and the second letter the one at position 8.

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the mutation K8A This clearly indicates a specific

functional significance of the charge in amino acid

position 8 for the formation of a productive encounter

complex during the electron transfer from cyt c6 to

PS I K8 is located at the edge of the contact surface

of cyt c6 that directly interacts with PS I [26], and a

positive charge in this position might be expected to

play an important role by establishing specific

electro-static interactions during complex formation with PS I

The variant carrying the single mutation D72N

showed an increased kbim value compared with cyt c6

wild-type, whereas for the mutant D72A, which has

the same net charge, no change in kbim was observed

This result implies that changes in amino acid position

72 have additional specific effects on the interaction of

cyt c6with PS I, independent of the influence of global

net charge

Urea-induced folding⁄ unfolding of cyt c6:

equilibrium stability

Preliminary experiments had shown that cyt c6 has

maximum stability against unfolding by heat and

denaturants around pH 5.5, in its physiological

work-ing range [27] Oxidized cyt c6 could not be fully

unfol-ded by urea at pH 5 and 30C Therefore, we chose

to observe the urea-induced folding⁄ unfolding of

oxi-dized cyt c6 and its mutant forms at pH 7 The study

was carried out by performing folding equilibrium

relaxation experiments In Fig 2, the results of typical

experiments with wild-type cyt c6 and the mutant

forms D72K and D72A⁄ K8D are shown as examples,

along with the derived equilibrium unfolding curves

(Fig 2D) Analysis of all performed experiments

yielded a set of parameters for comparison of the

sta-bilities of wild-type and mutants (Table 2)

As previously reported [22], the transition midpoint

for urea-induced unfolding ([urea]50) of the mutant

D72K was shifted to significantly lower urea

concen-trations ([urea]), and its Gibbs energy of unfolding at

0 [urea] (DGU0) was significantly reduced (D[urea]50¼

)2.4 ± 0.2 m, DDGU0¼)2.7 ± 1.6 kJÆmol)1) The mutant protein D72N was similarly affected (D[urea]50¼ )1.9 ± 0.1 m, DDGU0¼)3.1 ± 2.9 kJÆmol)1) All other single mutations, including D72A, had a comparably minor effect Charge neutralization at position K8 has no significant effect on the structural

0 1 2 3 4

wild type

A

B

C

D

0 1 2 3

AD

D72K

0.0 0.3 0.6 0.9 1.2 1.5 1

2 3 4

time (s)

0 2 4 6 8 10 0

20 40 60 80 100

[urea] (M)

Fig 2 Folding equilibrium relaxation experiments The represented

experiments were performed with wild-type cyt c 6 (A), D72K (B)

and D72A ⁄ K8D (AD) (C) Arrows on the right indicate increasing

[urea] final (0–9.8 M ) Percentages of unfolded protein at equilibrium

as determined from the experiments shown in (A) to (C) for

wild-type cyt c6(squares), D72K (circles) and AD (triangles) are plotted

as a function of [urea] in (D) The lines represent fits of two state

transitions to the data for wild-type cyt c 6 (solid), D72K (dashed)

and AD (dotted) Double mutants are abbreviated with the first

let-ter representing the residue at position 72 and the second letlet-ter

the one at position 8.

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stability of the protein, whereas inversion of the charge

at position 72 considerably reduces the stability against

urea-induced unfolding, i.e electrostatic interactions of

the negative charge at position D72 seem to play an

important role for the stability of cyt c6 It is interesting

to note that charge neutralization with a

hydrogen-bond-forming asparagine residue leads to

destabiliza-tion of the protein, whereas neutralizadestabiliza-tion with a small

hydrophobic alanine residue does not

Partial or total neutralization of the effect of the

mutation D72K on the protein’s global charge was not

sufficient to fully reverse the negative effect on the

stability of cyt c6 The apparent stability of the

mu-tants D72K⁄ K8A (D[urea]50¼)1.7 ± 0.1 m, DDGU0¼

)1.4 ± 2.1 kJÆmol)1) and D72K⁄ K8D (KD) (D[urea]50¼

)1.4 ± 0.1 m, DDGU0¼ +0.2 ± 2.8 kJÆmol)1) against

urea-induced unfolding was still reduced when

com-pared with wild-type cyt c6 This indicates that the

elec-trostatic interactions of the side-chain of D72 that

contribute to the stability of cyt c6 are at least partially

local, and that the adverse effects of the mutations

D72K and D72N cannot be entirely ascribed to global

electrostatic repulsion within the positively charged

protein

However, although mutation D72A did not lead to

a significant change in stability, the additional

elimin-ation of the positive charge K8 in the double mutants

D72A⁄ K8D and D72A ⁄ K8A resulted in an increased

apparent stability against urea-induced unfolding, as

well as an increased Gibbs energy of unfolding of

these mutants (D[urea]50¼ +0.2 ± 0.1 m, DDGU0¼

+3.5 ± 2.4 kJÆmol)1 and D[urea]50¼ +0.2 ± 0.1 m,

DDGU0¼ +0.5 ± 1.7 kJÆmol)1, respectively)

The equilibrium urea interaction parameter (meq),

which represents the steepness of the unfolding

transition with respect to [urea] and may be interpreted

as a measure of the change in solvent-accessible area

upon unfolding [28], was affected by changes at position D72, but not at position K8 It was significantly increased for all mutants in which position 72 had been modified, with the exception of D72A⁄ K8A This find-ing might be partially explained by a prevalence of more extended conformations in the unfolded ensemble of states due to local electrostatic repulsion in the vicinity

of the mutated position 72

Urea-induced folding⁄ unfolding of cyt c6: kinetic parameters

The performed folding relaxation experiments also allowed for the determination of kinetic parameters (Table 2) The most thermodynamically unstable mutants, D72N and D72K, were found to have the highest unfolding rate constant in absence of denatu-rant (kU0¼ 0.075 and 0.080 s)1, respectively), while the mutant with the highest DGU0 value, D72A⁄ K8D, was found to show the lowest unfolding rate (kU0¼ 0.023 s)1) The value for wild-type cyt c6 lay between these extremes (kU0¼ 0.035 s)1) (Table 2) In general,

a good correlation (R¼ –0.73) was found between log

kU0 and the Gibbs energy of unfolding at 0 [urea] (DGU0) In the mutant series, the overall height of the energy barrier for the rate-determining step of the fold-ing⁄ unfolding transition is mainly determined by the overall difference in Gibbs energy between the native state (N) and the ensemble of unfolded states (U), in agreement with a single transition state with a disor-dered (unfolded-like) structure [28] This indicates that the folding⁄ unfolding transition proceeds along a sim-ilar pathway for wild-type cyt c6and for all mutants When the folding⁄ unfolding traces were analysed individually, and the apparent rate constants (k) for the individual traces were plotted against [urea] in Chevron plots, pronounced deviations from linearity

Table 2 Evaluation of urea-induced folding equilibrium relaxation experiments Data represent means ± SD from 2–4 experiments for each protein.

[Urea]50 (M)

DG U0 (kJÆmol)1)

meq (kJÆmol)1Æ M )1)

log (k U0 Æs)1)

mk1 (kJÆmol)1Æ M )1)

mk2 (kJÆmol)1Æ M )2)

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(‘roll over’ and ‘roll down’) were observed (not

shown) These deviations were interpreted as indicative

of a Hammond shift [29] in the structure of the

trans-ition state  with increasing denaturant concentration

For the global analysis, this was taken into account by

introducing the parameter mk2 From the fit

parame-ters, a values were calculated (as a function of urea)

according to Eqn (3) (see Experimental procedures)

These values may be interpreted as a measure of

native-like structure in the transition state [22,28]

Whereas a¼ 1 would indicate an all native-like

trans-ition state, a¼ 0 would indicate an all unfolded-like

one Wild-type cyt c6 and all mutant forms showed a

transition state shift to higher a-values with increasing

[urea] (not shown) The single mutants D72K and

D72N, as well as the double mutants D72K⁄ K8D and

D72K⁄ K8A, showed the steepest increase in a with

[urea] (i.e a higher mk2 value), and therefore

signifi-cantly higher a-values at high denaturant

concentra-tions than wild-type cyt c6 and the other mutant

forms Their kinetic properties were clearly more

sus-ceptible to the effect of urea and the structure of their

transition state shifted more strongly towards the

native conformation under the influence of

destabiliza-tion of the latter

Microcalorimetry studies

In order to obtain the thermodynamic parameters of

the thermal unfolding of cyt c6 and its mutants, DSC

was performed

At pH 7, oxidized cyt c6 was found to be

redox-unstable in the absence of oxidizing agents, whose

presence would affect the calorimetric trace of the

DSC experiment It was also observed that the heating

of reduced protein at pH 7 gave rise to complex

calori-metric traces, probably due to an oxidative process of

the protein upon thermal unfolding It was found that

at lower pH values ranging from 3.0 to 5.0, close to

the physiological working range of cyt c6, the oxidized

form was redox-stable in absence of oxidizing agents

during DSC experimental time Consequently, DSC

experiments were carried out at pH 3.0, 4.0 and 5.0

for all cyt c6variants In all cases, heat-induced

unfold-ing was highly reversible and independent of both

the scanning rate and the protein concentration All

calorimetric traces could be fitted very well to a

two-state equilibrium model (NfiU)

The experimental DSC curves, together with their

best fits, for the thermal unfolding of wild-type cyt c6,

and for the mutants D72K and D72A⁄ K8D at pH 5.0

are shown in Fig 3A as typical examples The effect

of pH on thermal unfolding of wild-type cyt c6 is

shown in Fig 3B The Gibbs energy of unfolding as a function of temperature, DGU(T), could be obtained using the thermodynamic parameter values from the multiple fits of the DSC traces at the studied pH con-ditions The values of DGU(T) at 30C (DG30  C

U ) for wild-type were 54.8 kJÆmol)1 at pH 5.0, 49.3 kJÆmol)1

at pH 4.0 and 34.5 kJÆmol)1at pH 3.0 It is clear from these results that there is a pronounced pH effect on the stability of cyt c6 Taking into account the value of 21.4 kJÆmol)1 obtained at pH 7.0 by the urea-induced folding⁄ unfolding experiments (Table 2), it could be confirmed that the maximum stability of wild-type cyt c6 is around pH 5.0 As it is shown in Table 3, this behaviour was common to all studied mutants

A similar dependence on the pH was observed for the Tm values obtained for all proteins (Table 3) By contrast, the effect of pH on the unfolding enthalpies

30 50 70 90 110 10

20 30 40 50 60

temperature (ºC)

temperature (ºC)

30 50 70 90 110 10

20 30 40 50 60

A

B

C p

-1 ·mol

-1 )

C p

-1 ·mol

-1 )

Fig 3 Temperature dependence of the partial molar heat capacity

of cyt c6 (A) DSC traces at pH 5.0 for wild-type (h), D72K (s) and D72A ⁄ K8D (n) (B) DSC traces for wild-type at pH 5.0 (h), pH 4.0 (s) and pH 3.0 (n) Symbols correspond to experimental data, for clarity every third data point is plotted Solid lines correspond to best fits to the two-state equilibrium model.

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seemed to be more complex (Fig 4) For many

pro-teins the dependence of DHU,m on Tmis linear,

indica-ting an entropic origin of the differences in stability

[30–32] The slope of such a representation

corres-ponds to DCp,U In our case, as shown in Fig 4, this

dependence was not linear for many of the studied

forms of cyt c6 Moreover, in the mutants for which

a linear dependence was observed, e.g K8D, the

obtained slope values were much greater than the

DCp,U values calculated from the global analysis of

the calorimetric traces As may be observed in Fig 4,

the enthalpic variation with pH is most pronounced

between pH 3 and 4 for the wild-type and most

mutants, with the exception of D72A, for which the

biggest pH effect was observed between pH 4 and 5

These results indicate that the stability differences

found are not only of entropic nature but that there is

a considerable enthalpic contribution Because the

ionic strength was fixed in all experiments, the pH

effects are exclusively due to changes in the

electro-static interactions The enthalpic contributions of

pro-tonation⁄ deprotonation events are small compared

with the changes in enthalpy observed in these mutants

(up to 60 kJÆmol)1) So, it is likely that these ionization

events are responsible for some kind of structural

rear-rangement that is associated with enthalpic changes

The changes in the thermodynamic parameters of

unfolding of each mutant with respect to the wild-type

protein are summarized in Fig 5 To avoid

extrapola-tion over a large temperature range, the values of

DDGU and DDHU are reported at 75C, which is at

approximately the median unfolding temperature At

all studied pH conditions, wild-type cyt c6had a

signi-ficantly higher Gibbs energy of unfolding than the

mutants, with the exception of D72A at pH 4 and 3,

and of the double mutants D72A⁄ K8D and

Table 3 Thermal unfolding transition of wild-type cyt c6and its mutant forms For each protein, thermodynamic parameters were deter-mined by global fits of the two-state equilibrium model to the DSC traces recorded at all three pH conditions Tmvalues refer to the trans-ition midpoint and DG 30  C

U values represent Gibbs energies of unfolding extrapolated to 30 C The reported values are estimated to be accurate within ±0.4 C for T m and ±10% for DG 30  C

U The DG U0 values for pH 7.0 from Table 2 are included for comparison.

pH 7.0 DG U0

(kJÆmol)1) Tm(C)

pH 5.0 DG 30  C

U (kJÆmol)1) Tm(C)

pH 4.0 DG 30  C

U (kJÆmol)1) Tm(C)

pH 3.0 DG 30  C

U (kJÆmol)1)

65 70 75 80 85 300

330 360 390 420

H U,m

-1 )

H U,m

-1 )

65 70 75 80 85 300

330 360 390 420

A

B

Fig 4 Temperature dependence of DH U,m Temperature depend-ence of the unfolding heat effect for wild-type cyt c 6 and its mutant forms Symbols correspond to the DH U,m and Tm values obtained

by multiple fits of the DSC traces at the three pH conditions for (A) wild-type ( ), K8A (s), D72A ⁄ K8D (n), D72K ⁄ K8D (,) and D72A ⁄ K8A (e), and for (B) K8D ( ), D72K (s), D72N (n), D72A (,) and D72K ⁄ K8A (e) The lines correspond to the DH U (T) functions obtained by multiple fits for wild-type (A) and for K8D (B) at pH 5.0 (solid line), pH 4.0 (dashed line) and pH 3.0 (dotted line).

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D72A⁄ K8A at all three pH values (Fig 5A) This

ten-dency was also observed when comparing the Tm

val-ues (Fig 5B) These results are in good agreement

with the apparent order of stabilities obtained from

the urea-induced unfolding experiments (Table 3) It is

interesting to note that the stabilizing effect of

substi-tuting D72 to alanine (in single and double mutants)

was neither observed when the position 72 was

mutated to a charged lysine residue, nor when it was

changed to the neutral and hydrogen bond forming

asparagine

With respect to DDHU75C values (Fig 5C) two

groups of mutants could be distinguished The point

mutations at position 8, for which no significant

enthalpic difference was observed, and the rest (where

position 72 is mutated), which presented lower

enthal-pies of unfolding than the wild-type protein

Inspection of the values obtained for the Gibbs

ener-gies of unfolding of the mutant forms of cyt c6

revealed significant nonadditive effects in the stabilities

of the double mutants when compared with the

stabili-ties of the respective single mutants The interaction

Gibbs energies (DGint) at 30C for the different double

mutants were estimated by double-mutant cycle

analy-sis [33,34] and are summarized in Table 4 At pH 5.0,

theDGint values obtained when K8 was substituted by

aspartate were  5 kJÆmol)1higher than when K8 was

substituted by alanine, independent of the nature of

the substitution at amino acid position 72 This

addi-tional interaction energy was reduced to 2 kJÆmol)1

(for the double mutants of D72K⁄ K8D and

D72K⁄ K8A) or even abolished (for the double

mutants D72A⁄ K8D and D72A ⁄ K8A) at pH 3.0 Assuming a standard pKa value for the carboxyl group, the aspartate residue introduced at position 8 would be almost completely neutralized at pH 3.0 Thus, replacement of K8 with a negatively charged residue resulted in stronger destabilizing interactions than a neutral residue, when the negative charge at position 72 was removed

The influence of the nature of the introduced muta-tions and the complex pH dependence of the DGint values for the different mutant pairs strongly suggest that much more complex effects (multiple interactions and⁄ or structural rearrangements) than a direct elec-trostatic interaction between the residues at amino acid positions 8 and 72 play a role A refined model for the structure of cyt c6, incorporating NMR data, has become available during revision of this work [35] In this model (Fig 6), K8 is located relatively far from other charged residues, and its side chain is highly solvent exposed It forms backbone hydrogen bonds

AA

AD

KA

KD

D72A

D72N

D72K

K8A

K8D

∆∆G U75 ºC

(kJ mol-1)

∆T m(K)

AA AD KA KD D72A D72N D72K K8A K8D

AA AD KA KD D72A D72N D72K K8A K8D

Fig 5 Effect of mutations on the thermodynamic parameters of unfolding Difference of the thermodynamic parameters DDGU75C(A), Tm (B) and DDH U75

 C

between wild-type and each mutant Black bars correspond to pH 5.0, grey bars to pH 4.0 and light grey bars to pH 3.0 Double mutants are abbreviated with the first letter representing the residue at position 72 and the second letter the one at position 8.

Table 4 Double-mutant cycle analysis Interaction Gibbs energies

at 30 C (DG int ) were calculated from the DGU30C-values reported

in Table 3 according to DG int (D72X ⁄ K8Y) ¼ DG 30  C

U (wild-type) + DG 30  C

U (D72X ⁄ K8Y) – DG 30  C

U (D72X) – DG 30  C

U (K8Y).

DG int (kJÆmol)1)

DG intpH5– DG intpH3 (kJÆmol)1)

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along the N-terminal a helix involving the amino acids

V4⁄ N5, and S11 ⁄ A12 The side chain of D72 is part of

an acidic patch, together with the residues D2 and

E68 It forms backbone hydrogen bonds along the

C-terminal a helix to E68 and Y76 Interestingly, one

of the side chain oxygens of D72 appears to be

hydro-gen-bonded to the backbone N atom of G6, bridging

the crossing between the N- and C-terminal a helices

of cyt c6 (Fig 6) Any mutation leading to charge

neutralization or inversion of a residue within this

helix-crossing region may cause rearrangements and a

reorganization of the local hydrogen-bond network It

is, for example, conceivable that upon replacement of

D72 by alanine one of the residues E68 or Q69 ‘takes

over’ in forming a stabilizing hydrogen bond to an

amino acid within a reoriented N-terminal a helix

However, any such interpretation of the experimental

data remains speculative until reliable structural

infor-mation for cyt c6 and its mutant forms becomes

avail-able

Conclusions

The results of this study stress the importance of

elec-trostatic interactions for the function, as well as for

the stability, of cyt c6 Neutralization or inversion of

the positive charge at position K8 significantly reduced

the efficiency of electron transfer to PS I This effect was not reversed when the global charge of the protein was restored by additional mutations at position 72 This implies that residue K8 plays a role in the forma-tion of the electron transfer complex between cyt c6 and PS I However, replacement of the negative charge

at position D72 by asparagine or lysine increased the efficiency of electron transfer to PS I, at least partly,

by favouring long-range electrostatic attraction between the reaction partners These mutations, however, were found to destabilize the protein significantly Again, this effect of the mutations could not be fully reversed

by restoring the global charge balance The negative charge at position D72 apparently participates in elec-trostatic interactions that stabilize the structure of cyt c6, as indicated by the reduced enthalpy of unfold-ing of the correspondunfold-ing mutants Interestunfold-ingly, the negative effect of its deletion was reduced, due to entropic contributions, when aspartate was not replaced by the isosteric asparagine, or by lysine, but

by the small amino acid alanine For the variants carrying the mutation D72A, the positive change in entropy upon unfolding was reduced with respect to other variants of cyt c6 This smaller unfolding entropy could be due to the effect of the mutation on the native state (higher flexibility and⁄ or lower exposure of hydrophobic area to the solvent in the mutant D72A) and⁄ or on the unfolded state (lower flexibility and ⁄ or higher solvation of hydrophobic surface area) Com-plementing the mutation D72A with a charge neutral-ization or inversion at position K8 led to mutant forms of cyt c6 that were more stable than the wild-type under all tested conditions Of all studied forms

of cyt c6, AD was the thermodynamically most stable

at pH 7, whereas AA was the most stable at pH 4 and

3 The price for this stabilization, however, was a reduction in catalytic efficiency by > 50%

Experimental procedures

Protein expression and purification Expression plasmids pEACwt and pEACD72K were kindly provided by F.P Molina-Heredia [16,36] Expression plas-mids for the other mutants were generated by site-directed mutagenesis according to the QuikChange method

wild-type and its mutant forms were expressed under aero-bic conditions in E coli GM119 cells that had been cotransfected with the plasmid pEC86 [37] (kindly provided

by L Tho¨ny-Meyer, ETH Zu¨rich) and were purified as des-cribed previously [16], with the exception of the mutants

Fig 6 Structural model of cyt c 6 , showing secondary structure

ele-ments The side chains of amino acids K8 (blue), E68 (light red),

Q69 (light green) and D72 (red), as well as the heme moiety

(orange), are depicted as stick models The H-bond from the

back-bone amide group of G6 to the carboxyl oxygen of D72 is shown

as dotted green line The image was generated with PYMOL 0.97

(DeLano Scientific, San Carlos, CA, USA) and is based on the

struc-tural model from [35].

Trang 9

purified by a combination of anion-exchange

chromatogra-phy and gel filtration In brief, the periplasmic extracts

con-taining the mutants K8D, K8A or AD were dialysed

against 0.5 mm sodium phosphate buffer pH 7, oxidized by

the addition of 50 lm potassium ferricyanide, and loaded

onto a DEAE cellulose column (50 mL) that had been

equilibrated with a 1 mm sodium phosphate buffer, pH 7

The mutant proteins were found in the flow-through After

concentration under nitrogen pressure in an Amicon 8050

ultrafiltration device fitted with YM 3 membranes

(Milli-pore, Bedford, MA), the fractions containing the mutant

FPLC column The running buffer for the gel filtration was

chroma-tography, the purified proteins were washed with 10 mm

preparations was > 95% as judged from the optical

absorbance ratio at 554 and 280 nm, and from Coomassie

Redox potentials

Redox potentials were determined by potentiometric

titra-tion with sodium dithionite and potassium ferricyanide as

described previously [38] The determinations were carried

Laser-flash absorption spectroscopy

Experiments were carried out as described previously [3]

The reaction mixture was buffered with 20 mm

from Nostoc sp PCC 7119 were measured at increasing

phases were not observed, and it was possible to analyse all

kinetic according to a simple bimolecular reaction

Stopped-flow experiments

Folding equilibrium relaxation experiments were carried

out as described previously [22] In brief, equal

sodium phosphate pH 7.0 (buffer) and in 9.8 m urea

buf-fered with 20 mm sodium phosphate pH 7.0 (bufbuf-fered urea

solution), both containing 50 lm potassium ferricyanide in

order to keep the protein in its oxidized state throughout

ratios (r) in a lSFM20 stopped-flow device (BioLogic SA, Grenoble, France) with a constant total flow rate of

fluores-cence Kinetic traces were recorded in duplicate or triplicate and averaged for analysis The data for all mutants were fitted globally to a two-state model assuming linear

concentration ([urea]) according to

according to

urea-dependent shift in transition state structure, a values were calculated from the fit parameters according to

The global fitting of the data was carried out with the non-linear analysis module of origin 5.0 (Microcal, Northamp-ton, MA, USA)

Microcalorimetry

was measured as a function of temperature with a VP-DSC differential scanning microcalorimeter (Microcal) Samples were dialysed overnight against the desired buffer and sub-sequently oxidized by addition of potassium ferricyanide to

a final concentration of 2.5 mm Immediately before load-ing the samples into the calorimetric cell, ferricyanide was removed by gel filtration on a PD-10 column (Amersham Biosciences, Little Chalfont, UK) The buffers used in the experiments were 60 mm sodium acetate, pH 5.0, 250 mm sodium acetate, pH 4.0, or 45 mm sodium phosphate,

pH 3.0, all giving rise to the same ionic strength (41 mm)

as the 20 mm sodium phosphate buffer, pH 7, which was

DSC experiments were performed at a heating rate of

scans were performed with the corresponding dialysis buffer loaded in both calorimetric cells The partial molar heat

Trang 10

After transforming the DSC traces into partial molar heat

capacity curves, they were subjected to individual and

glo-bal curve fitting using the nonlinear analysis module of

equations corresponding to a two state model (NfiU) The

temperature dependence of the heat capacity was described

as a linear and quadratic function for the native and

unfol-ded species, respectively [39] The corresponding parameters

were left to float during the curve fitting, with the exception

of the first- and second-order coefficients of the unfolded

heat capacity, which were fixed and evaluated from the

amino acid content as described previously [40,41] For

fitting of the DSC traces recorded at all three studied pH

values

Chemicals

Urea was SigmaUltra grade All other chemicals were

at least analytical grade All solutions were prepared with

MilliQ water

Acknowledgements

This work was supported by the Spanish Ministry of

Science and Technology (MCYT grants BMC

2000-444 and BIO2003-04274) and the Junta de Andalucı´a

(PAI, CVI-198) CL received a fellowship from the

European Union’s Research Training Network

pro-gram (HRPN-CT-1999-00095) IL was supported by a

research contract from the University of Granada and

is the recipient of a Ramo´n y Cajal research contract

from the Spanish Ministry of Science and Technology

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