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MercuryII binding to metallothioneinsVariables governing the formation and structural features of the mammalian Hg-MT species A`ngels Leiva-Presa, Merce` Capdevila and Pilar Gonza`lez-Du

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Mercury(II) binding to metallothioneins

Variables governing the formation and structural features of the mammalian

Hg-MT species

A`ngels Leiva-Presa, Merce` Capdevila and Pilar Gonza`lez-Duarte

Departament de Quı´mica, Facultat de Cie`ncies, Universitat Auto`noma de Barcelona, Spain

With the aim of extending our knowledge on the reaction

pathways of Zn-metallothionein (MT) and apo-MT species

in the presence of Hg(II), we monitored the titration of

Zn7-MT, Zn4-aMT and Zn3-bMT proteins, at pH 7 and 3,

with either HgCl2or Hg(ClO4)2by CD and UV-vis

spectr-oscopy Detailed analysis of the optical data revealed that

standard variables, such as the pH of the solution, the

binding ability of the counter-ion (chloride or perchlorate),

and the time elapsed between subsequent additions of Hg(II)

to the protein, play a determinant role in the stoichiometry,

stereochemistry and degree of folding of the Hg-MT species

Despite the fact that the effect of these variables is unques-tionable, it is difficult to generalize Overall, it can be con-cluded that the reaction conditions [pH, time elapsed between subsequent additions of Hg(II) to the protein] affect the structural properties more substantially than the stoi-chiometry of the Hg-MT species, and that the role of the counter-ion becomes particularly apparent on the structure

of overloaded Hg-MT

Keywords: mercury(II) binding; mercury-metallothionein; metallothionein; a-metallothionein; b-metallothionein

Mercury thiolates provide representative examples of the

structural diversity shown by the extensive family of metal

thiolates [1–4] The most striking features of mercury

thiolates in the solid phase are the different structures

obtained when Hg(II) is co-ordinated to very similar

thiolate ligands [5,6] and the distinctive behavior of Hg(II)

towards a particular thiolate compared with that of Zn(II)

or Cd(II) [7], which has been referred to as the zinc family

paradox [3] Moreover, correlations between solid-state and

solution complexes cannot be easily established Overall, the

diverse co-ordination preferences of Hg(II) ions (mainly

tetrahedral, trigonal-planar and digonal) and their

coexist-ence in polynuclear complex species, the various ligation

modes of the thiolate ligands (i.e terminal, l2-bridging or

l3-bridging) and the possibility of secondary Hg(II)–sulfur

interactions [8] make it difficult to anticipate the structure of

a particular mercury thiolate complex [1,3,9] This results

from the interplay of not only the above factors, but also the

reaction conditions Of these, the presence of additional

co-ordinating species, such as halide ions, make the bonding

situation for mercury even less straightforward than in the

case of homoleptic mercury thiolates [10,11]

The biological chemistry of mercury is dominated by co-ordination to cysteine thiolate groups in agreement with the preference of this metal ion for the soft sulfur ligands The high binding constants for binding of Hg(II) to cysteine residues account for the irreversible replacement of essential metals (Zn, Cu) in cysteine-containing metalloproteins and thus for the high toxicity of mercury to living systems Within the same context of the highly favored thermo-dynamically Hg-S bond, resistance to Hg(II) toxicity in several bacteria is based on an ensemble of proteins designated as Mer, most of which bind Hg(II) ions through cysteine residues ([3] and references therein) In mammals, detoxification of mercury by metallothioneins (MTs) occurs via cysteine complexation and sequestration [12] A major feature of this very large family of ubiquitous low molecular mass proteins is their extremely high content of cysteine residues, the binding of which to metal centers determines the 3D structure of the protein [13] Consideration of the high flexibility and multidentate ligand nature of the peptide chain in MTs together with the intrinsic complexity of mercury thiolate complexes suggests that elucidation of the stoichiometry and co-ordination geometries of mercury in solution Hg-MT species may be rather intricate

To date, optical spectroscopy (UV-vis and CD) has played a major role in the study of the mercury-binding properties of mammalian MTs, for which several Hg-MT stoichiometries have been reported [14] Thus, a detailed analysis of the electronic spectra of Hg(II)-reconstituted MT led Vasˇa´k et al [15] to propose that Hg(II) in Hg7-MT is co-ordinated at sites with tetrahedrally related geometry Subsequent studies by Johnson & Armitage [16] of the UV spectral data obtained in the titration of Cd(II)7-MT with Hg(II) showed that Hg(II) initially occupies tetrahedral sites but, above a Hg/MT stoichiometry of four, there is a shift

to linear co-ordination However, on the basis of X-ray

Correspondence to M Capdevila, Departament de Quı´mica, Facultat

de Cie`ncies, Universitat Auto`noma de Barcelona, E-08193 Bellaterra,

Barcelona, Spain Fax: + 34 935813 101, Tel.: + 34 935813 323,

E-mail: merce.capdevila@uab.es

Abbreviations: MT, metallothionein; TDPAC, time differential

per-turbed angular correlation of c-rays; UV-vis, ultraviolet-visible

elec-tronic absorption; t, stabilization time allowed for the co-ordination of

Hg(II) to the protein; X, counter-ion of the Hg(II) salt added as

titrating agent.

(Received 19 July 2004, revised 21 October 2004,

accepted 25 October 2004)

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absorption studies conducted on some of the species

observed in the titration of either apo-MT or Zn7-MT with

Hg(II), monitored by optical spectroscopy, Lu & Stillman

[17] proposed a distorted tetrahedral co-ordination for

Hg(II) in Hg7-MT with two short (2.33 A˚) and two long

(3.4 A˚) Hg-S distances [18] Previous extended X-ray

absorption fine structure (EXAFS) results for Hg7-MT

were consistent with a Hg-S bond length of 2.42 A˚ and

suggested that Hg(II) was in a three-co-ordinate thiolate

environment [19]

Although the protective role of MTs against Hg(II)

toxicity provides particular interest for the study of the

Hg(II)-MT system, most existing results are difficult to

reconcile With the aim of finding new strategies for this

study, we now report on the effect of two variables, the

reaction time and the presence of chloride ions, on

the stoichiometry, stereochemistry and degree of folding

of the Hg(II)-MT species formed by either the binding of

Hg(II) to apo-MT or Zn/Hg replacement in Zn7-MT

Materials and methods

Protein preparation and characterization

Fermentator-scale cultures, purification of the

glutathione-S-transferase-MT fusion proteins, and recovery and

ana-lysis of the recombinant mouse Zn7-MT1, Zn4-aMT1 and

Zn3-bMT1 domains were performed as previously described

[20,21] The Zn7-MT, Zn4-aMT and Zn3-bMT species were

obtained in both Tris/HCl and Tris/HClO4buffer (50 mM,

pH 7) [22] The protein concentration was 0.1 mMin the

six solutions, which were diluted to a final concentration of

10 lM (MT) or 20 lM (aMT and bMT fragments) with

MilliQ-purified and Ar-degassed water before being titrated

with Hg2+solutions at 25C

The apoproteins were prepared by acidification of the

recombinant material with 10 mMHCl or HClO4,

respect-ively, until pH 3 At pH values lower than 3.5 the Zn7-MT,

Zn4-aMT and Zn3-bMT species are entirely devoid of

metal, according to their respective CD spectra In contrast,

Hg(II) remains bound to SCys at this pH

Metal solutions

Glassware and solutions used in metal ion-binding studies

were prepared as described [20] A Riedel-de Hae¨n atomic

absorption spectrometry Hg2+standard of 1000 p.p.m was

used as the HgCl2 solution The Hg(ClO4)2 solution was

prepared from the corresponding salt in MilliQ-purified

water, and the Hg(II) concentration was quantified by

atomic absorption spectrometry using a Perkin–Elmer 2100

atomic absorption spectrometer In both cases the Hg(II)

concentration of the titrating agents was in the 1–10 mM

range

Metal ion-binding reactions

Metal-binding experiments were carried out by sequentially

adding molar-ratio aliquots of concentrated Hg(II) stock

solutions to single solutions of either the holoproteins or

apoproteins and followed spectropolarimetrically (CD) and

which differ in the time elapsed between subsequent additions of Hg(II) to the protein, were carried out In one set, the standard titration procedure [22] was followed, whereas in the other consecutive additions of Hg(II) were made every 24 h The electronic absorption and CD measurements were performed and corrected as already described [22]

All manipulations involving the protein and metal ion solutions were performed in Ar atmosphere, and the titrations were carried out at least in duplicate to ensure the reproducibility of each point

The pH (7 or 3) for all experiments remained constant throughout At pH 7, the acidity of the Hg(II) solutions required the addition of appropriate buffer solutions of Tris/HCl or Tris/HClO4 (50 or 70 mM at pH 7), but no buffering was required for the titrations carried out at pH 3

Results and Discussion

In view of the well-known complexity of Hg(II)–thiolate systems, the difficulties we encountered in analyzing the results obtained through preliminary titrations of the Zn-MT proteins with Hg(II) were not a surprise They indicate that the nature of the counter-ion (X) and the time elapsed between subsequent additions of the Hg(II) solution (t) have a significant effect on the stoichiometry, stereo-chemistry and degree of folding of the species formed Thus,

to understand the reaction pathways followed by Zn-MT and apo-MT species in the presence of Hg(II), the effect of each of the previous variables was analyzed separately To this end, the titration of Zn7-MT, Zn4-aMT and Zn3-bMT proteins, at pH 7 and 3, with either HgCl2 or Hg(ClO4)2

were spectroscopically monitored

The CD and UV-vis spectroscopic techniques used in this work are currently used to study metal-binding features of

MT as they provide information on the co-ordinative features of the predominant metal-MT species present in solution at each titration point and on the number of species formed during the titration Furthermore, titration of the separate fragments provides information on the depend-ence/independence relationship between the two constitu-tive domains of the whole MT protein [21,23]

With regard to the two pH values, titrations at pH 7 allow the subsequent substitution of Zn(II) and thus formation of heterometallic Zn,Hg-MT species, and titrations at acidic

pH values provide information on the binding of Hg(II) to the corresponding apo-MT form [23] In addition, compar-ison of the two sets of data gives an indication of the role of Zn(II) in the Hg(II)-containing species formed at physiolo-gical pH The use of two different Hg(II) salts allowed analysis of the possible role of the physiologically relevant chloride anion, which has a strong tendency to co-ordinate and bridge Hg(II) ions, in the degree of folding and 3D structure of the Hg-MT species The perchlorate anion is well known for its low co-ordinating ability towards metal centers

As regards the time variable, the spectroscopic changes observed in the titrations of Zn7-MT, Zn4-aMT and

Zn3-bMT with Hg(II), after different times were allowed for the reaction between the MT protein and the added Hg(II) ions, were indicative of a strong dependence of the

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with HgCl2were carried out at two different times, t¼ 0 h

and t¼ 24 h, whereas those with Hg(ClO4)2 were only

performed at t¼ 24 h The t ¼ 0 h label denotes that the

titration was performed under kinetic control conditions,

which means that, for each addition, the protein sample was

allowed to react with the metal ion until subsequent CD

spectra were essentially coincident [22] However, for most

samples, if the CD spectrum was recorded again after 24 h,

it showed significant differences from that recorded at t¼

0 h For this reason, titrations labeled t¼ 24 h denote those

carried out under thermodynamic control conditions, where

each molar-ratio aliquot of Hg(II) was added every 24 h, as

longer time intervals showed no further changes in the

spectroscopic features

Overall, evaluation of all the variables in the Hg-MT

system required the performance and analysis of 18

titrations and the corresponding duplicates The detailed and comparative analysis of the set of CD, UV-vis and difference electronic absorption spectra recorded for each titration (provided as Supplementary Material) provides information on the species formed by the Zn-MT peptides in the presence of Hg(II) under the different experimental conditions assayed and has allowed us to propose the reaction pathways (Schemes 1–3) for Zn/Hg replacement in Zn-MT species (pH 7) and for the binding of Hg(II) to apo-MT (pH 3) that are discussed below

Mercury content in the Hg(II)-MT species at each titration point has traditionally been established by assu-ming that, in solution, only one species is present, the metal content of which coincides with the number of Hg(II) equivalents (eq) added To validate the previous assumptions as well as to quantify the Zn content in the Zn,Hg-MT species observed at pH 7 (Schemes 1A, 2A and 3A), we unsuccessfully devoted much effort to obtaining ESI-MS data Thus, information on the Zn(II) content was retrieved from CD data and it is mainly of a qualitative nature

Reaction of recombinant mouse Zn7-MT with Hg(II) Analysis of the CD, UV-vis and UV-vis difference spectra obtained in the titration of Zn7-MT with Hg(II) at pH 7 (Fig 2, S1 and S2) and pH 3 (Figs S3–S5) for each set

of X and t values led to the reaction pathways shown

in Scheme 1

Comparative analysis of the three sets of data indicates that the stoichiometry of the species formed along the three titrations at pH 7 depends on neither the stabilization time,

t, nor the nature of the counter-ion The unique exceptions

Fig 1 Evolution with time of the CD spectra corresponding to the

addition of the tenth Hg(II) to Zn 7 -MT at pH 7.

Scheme 1 Proposed reaction pathways for Hg(II) binding to recombinant Zn 7 -MT at pH 7 (A) and at pH 3 (B), under thermodynamic (t ¼ 24 h)

or kinetic (t ¼ 0 h) control conditions, using HgCl 2 or Hg(ClO 4 ) 2 as titrating agents The  and „ symbols denote similarity and difference, respectively, between the structure of two species compared.

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to this rule are: (a) Zn,Hg2-MT, observed as an intermediate

species only at t¼ 24 h; (b) the stoichiometries of the fully

loaded species, Hg15-MT and Hg16-MT Conversely, the

chirality of the species is highly dependent on the previous

variables, t¼ 24 h and X ¼ Cl–affording the most chiral

species, as shown by the intensity of the CD bands of the

Hg(II)-MT species formed under these conditions (Fig 2)

Similarly, t and X have a significant effect on the structure

of the Hg-MT aggregates, with a Hg to MT ratio equal or

higher than 7, as evidenced by the comparison of the CD

spectra of isostoichiometric species obtained under different

conditions The contribution of the counter-ion to the 3D

structure of the Hg-MT aggregates is demonstrated by the

outstanding example of Hg11-MT, which becomes one of

both kinetic and thermodynamic control conditions (Fig 3)

Another relevant feature is the formation of hetero-metallic Zn,Hg5-MT and Zn,Hg7-MT, both present in the three titrations The former shows a very specific CD fingerprint The significance of the latter lies in the Hg(II) stoichiometry, as previous studies proposed formation of homometallic Hg7-MT species [17,24] Under the experi-mental conditions used, the evolution of the CD spectra is fully consistent with the presence of heterometallic Zn,Hg7-MT as an intermediate species between Zn,Hg5

-MT and Hg9-MT Overall, the information obtained using the optical techniques allows Zn,Hg5-MT and Hg11-MT to

be considered the hallmark species formed in the Zn/Hg

Fig 2 (A) CD, (B) absorption UV-vis, and (C) difference absorption UV-vis spectra obtained by subtracting the successive spectra of (B), corresponding

to the titration of recombinant mouse Zn 7 -MT1 with HgCl 2 at pH 7 and t ¼ 24 h The Hg(II) to MT molar ratios are indicated within each frame.

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Data obtained at pH 3 show a strong influence of

tand X on the stoichiometry and structure of the species

formed, as shown in Scheme 1B, and thus, the three

reaction pathways followed at this pH are remarkably

different Notwithstanding this, there is a minor effect of

tand X at the beginning and end of the titration Thus,

the addition of the first 4–6 of Hg(II) to apo-MT gives

rise to Hg-MT species of comparable stoichiometry and

structure, i.e Hg4-MT and Hg5)6-MT, and also the

presence of an excess of Hg(II) cation leads invariably to

Hg18-MT Furthermore, within the previous range [from

4–6 to 18 Hg(II)], subsequent additions of Hg(II) led to

low-chirality Hg-MT species under all conditions The

only exception is Hg13-MT, formed at t¼ 0 h and X ¼

Cl–, which shows a well-defined CD fingerprint, also

indicative of a highly chiral species Concerning the role

of the counter-ion, the differences observed in the CD

spectra of overloaded Hg-MT species, such as Hg10-MT

and Hg18-MT, formed at t¼ 24 h, provide evidence for the interaction of the chloride anion with Hg(II), as already found at pH 7

Fig 3 Role of the chloride anion in the degree of folding of Hg-MT

species observed by comparing the CD spectra of the Hg 11 -MT species

obtained in the titration of Zn 7 -MT with either HgCl 2 (in black) or

Hg(ClO 4 ) 2 (in grey), both at pH 7 and t ¼ 24 h.

Scheme 2 Proposed reaction pathways for Hg(II) binding to recombinant Zn 4 -aMT at pH 7 (A) and at pH 3 (B), under thermodynamic (t ¼ 24 h)

or kinetic (t ¼ 0 h) control conditions, using HgCl 2 or Hg(ClO 4 ) 2 as titrating agents The  and „ symbols denote similarity and difference, respectively, between the structure of two species compared.

Fig 4 CD spectra of (A) the Zn 2 Hg 4 -aMT (in black) and Hg 5 -aMT (in grey), and Zn,Hg 4 -aMT (in black) and Zn,Hg 5 -aMT (in grey) species, respectively, obtained in the titrations of Zn 4 -aMT with HgCl 2 (solid lines) or Hg(ClO 4 ) 2 (dashed lines), both at pH 7 and t ¼ 24 h and (B) the

Hg 11 -aMT species obtained in the titrations of Zn 4 -aMT with HgCl 2 (in black) or Hg(ClO 4 ) 2 (in grey), both at pH 3 and t ¼ 24 h.

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Reaction of recombinant mouse Zn4-aMT with Hg(II)

Consideration of the optical spectroscopic data obtained in

the titrations of Zn4-aMT with Hg(II) at pH 7 (Figs S6–S8)

and pH 3 (Figs S9–S11) allows the proposal of the reaction

pathways shown in Scheme 2

Analogously to Zn7-MT, the stoichiometry of the

Hg-aMT species formed at pH 7 (Scheme 2A) along the

three titrations does not depend on t and X

Notwith-standing this, the Hg7-aMT species is absent in the

presence of Cl–at t¼ 24 h, and the species containing the

highest Hg(II) content, Hg11-aMT, is only obtained if

t¼ 0 h and X ¼Cl– Conversely, the structure and

chirality of the various Hg-aMT species are significantly

influenced by t and X, as evidenced by their CD spectra

Thus, the species with a Hg to aMT molar ratio higher

than 6–7 became more chiral if formed in the presence of

Cl–, among which, those formed at t¼ 0 h show the

highest degree of chirality Exceptionally, only the

Zn,Hg4-aMT species are comparable with respect to their

chirality and structure under the three sets of experimental

conditions

Interestingly, concerning the Zn,Hg4-aMT species, the

244(+) nm CD band recorded after the addition of 4 Hg(II)

to Zn4-aMT under all sets of conditions not only gives a

clear indication of the presence of Zn(II) in the aggregate,

but its intensity also suggests that the highest Zn(II) content

is found when X¼ ClO4 (Fig 4A) A similar analysis

reveals the presence of Zn(II) in the Hg5-aMT species

formed with X¼ ClO4 but its absence for X¼ Cl–

Chelex-100 treatment [23] of an aliquot of the

correspond-ing sample and subsequent analysis of the Zn and Hg

content by inductively coupled plasma atomic emission spectroscopy and inductively coupled plasma mass spectro-metry allowed us to unequivocally establish the Zn2Hg4 -aMT and Hg5-aMT stoichiometries for the species formed

at t¼ 24 h and X ¼ Cl– Overall, all previous data indicate that the replacement of Zn(II) by Hg(II) in Zn4-aMT proceeds more efficiently in the presence of Cl–than in the presence of ClO4

At pH 3 (Scheme 2B) neither t nor X has a substantial effect on the stoichiometry of the species formed during the titrations, except for the formation of two additional species, Hg3-aMT and Hg7-aMT, at t¼ 24 h and X ¼ ClO4 Conversely, the nature of the counter-ion strongly affects the chirality of the species This effect is remarkable for those species with a Hg(II) stoichiometry equal to or higher than 6, X¼ Cl– and t¼ 24 h In contrast, the Hg-aMT species formed in the presence of ClO4 show a very low degree of folding, indicating that Cl–ions strongly participate in the acquisition of the 3D structure of the Hg-aMT species (Fig 4B)

Reaction of recombinant mouse Zn3-bMT with Hg(II) The spectroscopic data obtained in the titrations of

Zn3-bMT with Hg(II) at pH 7 (Figures S12–S14) and pH

3 (Figures S15–S17) are consistent with the reaction pathways shown in Scheme 3 Comparison of the three sets of data recorded at pH 7 (Scheme 3A) reveals that the Hg:bMT stoichiometry of the species does not depend on the nature of the counter-ion Conversely, the stabilization time determines the Hg-bMT stoichiometry of most of the species formed and becomes particularly evident as the

Scheme 3 Proposed reaction pathways for Hg(II) binding to recombinant Zn 3 -bMT at pH 7 (A) and at pH 3 (B), under thermodynamic (t ¼ 24 h)

or kinetic (t ¼ 0 h) control conditions, using HgCl or Hg(ClO ) as titrating agents The  and „ symbols denote similarity and difference,

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nuclearity of the species increases Notwithstanding this,

saturation occurs in all cases for 10 Hg(II) On the other

hand, CD data indicate that the degree of chirality and the

structure of the species formed up to Zn,Hg3)4-bMT

depend on t and X, the most chiral species being those

obtained at t¼ 24 h and X ¼ Cl– As opposed to that

observed for the aMT fragment, the CD spectra reveal that

the presence of Cl–favors the Zn(II) ions remaining bound

to the bMT protein in the first stages of the titration

Titrations carried out at pH 3 (Scheme 3B) reveal that

the stoichiometries of the Hg-bMT species become

dependent on t and X after the formation of Hg7-bMT

Comparison of the three sets of CD data indicates that the

degree of chirality of the Hg-bMT species is generally

independent of t However, the chirality of the species

obtained in the presence of Cl– is much higher than that

achieved when X¼ ClO4, except for the Hg3-bMT

species, with a very low chirality in both cases, and the

Hg7-bMT species, which show comparable chirality for

X¼ Cl– and ClO4 (Fig 5) Comparison of the CD fingerprints of the Hg-bMT species formed along the three titrations shows that their 3D structure is strongly dependent on t and X, except for Hg3-bMT, which is poorly structured under all conditions

Co-ordination environments around Hg(II) in Hg-MT species

The complexity of the Hg(II)-MT system, which is mainly the result of its Hg-thiolate nature, makes it difficult to obtain information on the co-ordination geometry around Hg(II) in the Hg(II)-MT aggregates from optical techniques (CD and/or UV-vis spectra) by simple treatment of the data There are several reasons: (a) the presence of different chromophores in the same species including Zn and/or Hg

as metal ions and SCys and/or Cl– as ligands; (b) the absence of well-established relationships between most of the previous chromophores and the corresponding absorp-tion wavelengths [3]; (c) the overlapping of the absorpabsorp-tion bands corresponding to different chromophores, as shown

by the spectral envelopes in the difference UV-vis spectra Despite this, analysis of the difference UV-vis data, which discloses the effect of each Hg(II) addition, can give an insight into the evolution of the co-ordination geometry about Hg(II) in the MT species formed by either Zn/Hg replacement in Zn7-MT or the addition of Hg to apo-MT

By following this approach, comparison of the difference UV-vis spectra obtained in the titrations of Zn7-MT,

Zn4-aMT and Zn3-bMT with HgCl2 at pH 7 and t¼

24 h (Fig 2, S6 and S12) indicates a parallel evolution of the co-ordination geometry about Hg(II) in the three peptides These spectra evolve according to the following pattern: (a) the addition of the first 7 Hg(II) eq to Zn7-MT, or the first 4 Hg(II) eq to any of the aMT and bMT fragments, causes initially the appearance of an asymmetric broad band

Fig 5 CD spectra of the Hg 7 -bMT species obtained in the titrations

of Zn 3 -bMT at pH 3 with HgCl 2 at t = 24 h (solid black line) or

t = 0 (solid grey line), or with Hg(ClO 4 ) 2 at t = 24 h (dashed grey

line).

Scheme 4 An insight into the evolution of the coordination geometries about Hg(II) in the Hg-MT species formed during the titrations of Zn 7 -MT,

Zn 4 -aMT and Zn 3 -bMT with HgCl 2 at t ¼ 24 h and pH 7 (A) or pH 3 (B) The different coloured areas have been deduced from the difference UV-vis spectra Preliminary TDPAC measurements on the Hg-MT species within a square enable correlation of each area with an specific coordination geometry about Hg(II).

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(230–340 nm), which eventually transforms into two new

broad overlapping bands with absorption maxima at 230

and 320 nm; (b) the next Hg(II) eq added to the three

peptides gives rise to a negative broad band with absorption

minima at  260 and 310 nm, together with a positive

absorption with a maximum intensity in the range 220–

230 nm; (c) further Hg(II) additions to Hg11-MT, Hg6-aMT

and Hg5-bMT cause the former envelope to turn into a

positive broad band with an absorption maximum at

 250 nm with a shoulder at  310 nm; (d) this profile

collapses in the last steps of the titrations to give rise to very

weak absorptions along the whole wavelength range This

common evolution of the three titrations gives force to

different scenarios (denoted differently in Scheme 4A),

which may be consistent with the presence of three different

sets of co-ordination environments around Hg(II) in MT

Although the UV-vis difference spectra also suggest the

existence of different scenarios in the binding of Hg(II) to

Zn7-MT, Zn4-aMT and Zn3-bMT at pH 3 and t¼ 24 h

(Figures S3, S9 and S15), their evolution for the three

peptides (Scheme 4B) does not show such good parallelism

as that found at pH 7 Thus, at the beginning and end of the

three titrations, the spectral envelopes compare well and

suggest two different scenarios The former includes all the

species formed up to Hg5-MT, Hg4-aMT and Hg4-bMT,

and consists of a positive very intense band with a maximum

at  220 nm and a shoulder at  290 nm The second

scenario, which includes the species with the highest Hg(II)

to MT ratios, is characterized by very low absorptions along

the whole wavelength range In addition, a broad band with

a maximum at  250 nm and a shoulder at  310 nm

denotes a third common feature apparent in different

intermediate stages of the three titrations However, only

MT and the aMT peptides give rise to a fourth common

profile showing negative absorptions at 260 and 310 nm

together with a positive absorption within the range 220–

230 nm

The evolution of the difference UV-vis spectra at pH 7

(Scheme 4A) and pH 3 (Scheme 4B) is consistent with

preliminary time differential perturbed angular correlation

of c-rays (TDPAC) measurements (A` Leiva-Presa, M

Capdevila, P Gonza`lez-Duarte & W Tro¨ger, unpublished

results) on several Hg-MT species These results not only

corroborate the proposals made from the difference UV-vis

spectra but also suggest the specific co-ordination

environ-ments about Hg(II) associated with each scenario The

correlation between optical and TDPAC data is summarized

in Scheme 4, where the influence of the pH on the

co-ordi-nation geometry about Hg(II) becomes apparent One main

difference is the predominance of tetrahedral geometry at pH

7 and digonal geometry at pH 3, both coexisting with other

co-ordination geometries at increasing Hg to MT molar

ratios Interestingly, TDPAC measurements disclose two

types of linear co-ordination environments about mercury:

[Hg(SCys)2] and [Hg(SCys)Cl] Further TDPAC studies,

now in progress, should provide definitive data on the

co-ordinative features of the Hg-MT species

Concluding remarks

The above results document the strong influence of standard

ability of the counter-ions) on the nature and structural features of the Hg(II)-MT species obtained by Zn/Hg replacement in recombinant Zn7-MT, Zn4-aMT and

Zn3-bMT Table 1 shows that this dependence is diverse and thus difficult to generalize However, it can be concluded that the reaction conditions (pH, t) affect the structural properties more substantially than the stoichiom-etry of the Hg-MT species, and that the effect of the counter-ion (X) is particularly apparent on the structure of overloaded Hg-MT Specific findings of this work are: (a) the high number of Hg-MT species observed (Schemes 1– 3); (b) the formation of heterometallic Zn,Hg-MT aggre-gates, which include species such as Zn,Hg7-MT and Zn,Hg4-aMT, where the Hg(II) content equals that tradi-tionally expected for bivalent metal ions; (c) the nonadditive behavior of the a and b fragments with respect to the whole

MT Moreover, the stoichiometry found for the Zn2Hg4 -aMT species indicates that the binding of one Hg(II) cation

to MT does not require the displacement of one Zn(II) from the protein No such findings have previously been reported Earlier reports including CD and UV-vis data for the titration of native apo-MT2 and Zn7-MT2 with Hg(II) at

pH 7 proposed formation of the same set of species, Hg7

-MT, Hg11-MT and Hg20-MT, along both titrations, the latter being replaced by Hg18-MT in the titration of apo-MT2 at pH 2 Similarly, the titration of both apo-apo-MT2 and

Zn4-aMT2 at pH 7 resulted in formation of Hg4-aMT and

Hg11-aMT exclusively [14,17] Possibly, the different source

of the protein and the different experimental conditions used account for the discrepancy between these results and those reported in this work Overall, the optical spectral data sets observed for Hg(II) binding to either Zn-MT or apo-MT confirm the requirement for accurate control of the experimental conditions

Particularly relevant is the time variable, which has been scarcely considered in previous metal-MT binding studies

On the one hand, it has often been considered that metal displacement reactions in MT are kinetically facile and are generally complete within a few seconds [25] Moreover, the kinetic lability and consequently continuous breaking and reforming of the metal-sulfur bonds are well documented for the group 12 metal thiolates in solution [26] On the

Table 1 Influence of the reaction time (t) and binding ability of the counter-ions (X) on the nature and structural features of the set of Hg(II)-MT species formed during the corresponding titration Variables

in bold denote that they have a strong influence on most of the Hg-MT species formed Variables underlined affect only a minority of the species Voids denote that no general conclusions can be drawn The effect of the pH can be deduced by comparing the data of the same protein at the two pH values.

Set of Hg-MT species

Set of Hg-aMT species

Set of Hg-bMT species

Trang 9

Hg(II) to MTs, which would determine its reaction rate, is

unreported Remarkably, our results show that not only

do the reaction pathways at t¼ 0 h and t ¼ 24 h differ

considerably, but also that the CD features of a particular

species formed along the titration at t¼ 0 h do not evolve

with time to those found for the isostoichiometric species at

t¼ 24 h

Acknowledgements

This work was supported by a grant from the Spanish Ministerio de

Ciencia y Tecnologı´a (BQU2001-1976) Dr Sı´lvia Atrian, who kindly

provided us with the recombinant proteins used in this work,

acknowledges the Spanish Ministerio de Ciencia y Tecnologı´a for

financial support (BIO2003-03892) We also acknowledge the Servei

d’Ana`lisi Quı´mica, Universitat Auto`noma de Barcelona (CD, UV-vis)

and the Serveis Cientı´fico-Te`cnics, Universitat de Barcelona (inductively

coupled plasma-atomic emission spectroscopy and inductively coupled

plasma mass spectrometry) for allocating instrument time.

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Supplementary material

The following material is available from http://www blackwellpublishing.com/products/journals/suppmat/EJB/ EJB4456/EJB4456sm.htm

Figs S1–S17

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