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Tiêu đề Evidence for noncooperative metal binding to the a domain of human metallothionein
Tác giả Kelly E. Rigby Duncan, Martin J. Stillman
Trường học The University of Western Ontario
Chuyên ngành Chemistry
Thể loại Báo cáo khoa học
Năm xuất bản 2007
Thành phố London, ON, Canada
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Số trang 9
Dung lượng 761,3 KB

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Further interpretation of these data resulted in the proposal of positively cooperative metal binding as the primary metallation mechanism for each of the two domains [18–21].. 2A, addit

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a domain of human metallothionein

Kelly E Rigby Duncan and Martin J Stillman

Department of Chemistry, The University of Western Ontario, London, ON, Canada

Over the past several decades, significant advances

have been made in the field of protein folding [1–4]

However, the direct and specific involvement of metal

ions in the folding process of metalloproteins has

received far less attention, despite the fact that

one-third of all known enzymes require metal ions for

structural or functional purposes [5] Post-translational

metal-induced protein folding is a vital process that

still requires mechanistic elucidation Metalloproteins

that bind multiple metals introduce an additional layer

of complexity, in that cooperative metal-binding

mech-anisms are possible in which the complete multiple

metal-binding site forms in preference to partially filled

binding sites

Metallothionein (MT) is a metalloprotein found in

nearly all mammalian tissues coordinated to multiple

group 11 and 12 metal ions [6] The high capacity of

MT to bind both essential and nonessential metal ions

in vivo and in vitro strongly suggests a role in metal

ion storage, metabolism and trafficking of Cu and Zn,

as well as sequestration of Cd and Hg; however, the

exact function of MT remains undefined More recently, MT has been implicated in brain tissue repair through anti-inflammatory, antioxidant and antiapop-totic roles [7–11], as well as in chemotherapy resistance [12] Domain-independent but metal ion-directed fold-ing of MT results in the formation of discrete metal– thiolate clusters within each of the a and b domains with stoichiometries of [M4(Scys)11] and [M3(Scys)9], respectively, for divalent metal ions (M) [13–15] One of the most biologically important, and contro-versial, questions regarding the metallation of the two

MT domains is whether the metal-binding reaction proceeds by a positively cooperative mechanism The ramification of cooperative metal binding is that only the completely metallated and folded domains would have functional significance The metal-binding proper-ties of MT have been extensively investigated in the past, primarily as in vitro metallation reactions with different MT isoforms and varying metal ions [16–21] Although most of these publications are from 10–20 years ago, these reports still represent a common

Keywords

CD; cooperativity; metal-dependent protein

folding; metallothionein; MS

Correspondence

M J Stillman, Department of Chemistry,

Chemistry Building, The University of

Western Ontario, London, ON, Canada,

N6A 5B7

Fax: +1 519 661 3022

Tel: +1 519 661 3821

E-mail: martin.stillman@uwo.ca

Website: http://www.uwo.ca/chem/

(Received 22 December 2006, revised 2

February 2007, accepted 1 March 2007)

doi:10.1111/j.1742-4658.2007.05762.x

In the present study, we investigated the metal-binding reactivity of the isolated a domain of human metallothionein isoform 1a, with specific emphasis on resolving the debate concerning the cooperative nature of the metal-binding mechanism The metallation reaction of the metal-free

a domain with Cd2+ was unequivocally shown to proceed by a non-cooperative mechanism at physiologic pH by CD and UV absorption spectroscopy and ESI MS The data clearly show the presence of interme-diate partially metallated metallothionein species under limiting Cd2+ con-ditions Titration with four molar equivalents of Cd2+was required for the formation of the Cd4a species in 100% abundance The implications of a noncooperative metal-binding mechanism are that the partially metallated and metal-free species are stable intermediates, and thus may have a poten-tial role in the currently undefined function of metallothionein

Abbreviations

a-rhMT -1a, recombinant a domain of human metallothionein isoform 1a; MT, metallothionein.

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view of metal binding to MT and have been cited

regularly in recent reports The data presented in these

papers clearly show domain-specific binding for M2+

(M¼ Zn, Cd) initially to the a domain, thereby

lead-ing to formation of the M4a cluster prior to formation

of the M3b cluster, demonstrating that the individual

binding constants of divalent metal ions for the

a domain are larger than those for the b domain

Further interpretation of these data resulted in the

proposal of positively cooperative metal binding as the

primary metallation mechanism for each of the two

domains [18–21] Closer inspection of the previously

published data, however, brings the claim of positive

cooperativity into question, as there is no direct

evi-dence to show that coordination of the first metal ion

to the a domain enhances the binding of the second

metal ion and so forth Indeed, other published reports

present data showing that partially metallated species

of Cd–MT or Zn–MT exist under limiting metal ion

conditions, suggesting a noncooperative mechanism

[22,23] Recent kinetic results for As3+ binding to the

two isolated domains were also interpreted in terms of

a series of noncooperative bimolecular reactions [24]

The fact that Cd2+has been shown to coordinate to

the two-domain ba-MT in a domain-specific manner,

with a preference for the a domain, has been construed

as being an indicator of cooperative metal binding to

the a domain This study focuses on the metallation of

the isolated a domain, with the purpose of clarifying

this point Additionally, the reported concurrent

metal-lation of both domains in the two-domain protein by

Co2+[25] and Cd2+[23] provides an excellent example

of the complexity introduced by the presence of the b

domain in efforts to elucidate the potentially

cooper-ative nature of the metal-binding reaction within each

of the domains Thus, the goal is to elucidate the

meta-llation mechanisms of the individual domains, in the

hope, initially, of simplifying the interpretation of

the metallation details of the two-domain protein The

results presented here allow successful and complete

interpretation of the previous data in terms of

non-cooperative, domain-specific metal binding

Results

Investigation into the metal-binding mechanism of the

isolated a domain was carried out on the

recombin-antly synthesized a domain fragment of human MT

isoform 1a (a-rhMT-1a) The recombinant protein was

prepared by overexpression in Escherichia coli as an

S-tag fusion protein in the presence of Cd2+ (see

Experimental procedures for a full description of the

protein preparation and purification details) Following

isolation and purification, the S-tag fusion peptide was cleaved from the domain, generating the isolated

a domain, the sequence of which is shown in Fig 1A The four divalent metal ions are labeled 1a)4a, and the 11 cysteinyl sulfurs are labeled 1–11, starting from the N-terminus Figure 1B shows the space-filling and ball-and-stick representations of Cd4a-rhMT-1a, emphasizing the wrapping of the polypeptide backbone

in a left-handed coil around the metal–thiolate cluster, which is shown in the space-filling model to be located

in the center of the domain Figure 1C shows the iso-lated Cd4(Scys)11 cluster, where each cadmium ion (green spheres) coordinates tetrahedrally to four cystei-nyl sulfurs (yellow spheres), such that five of the 11 cysteinyl sulfurs act as bridging ligands between two metal centers, and the remaining six act as terminal ligands by coordinating to a single metal center The numbering of the cadmium ions and the cysteinyl sul-furs in Fig 1C corresponds with that in the sequence shown in Fig 1A Demetallation to produce the metal-free apo-a-rhMT was carried out by eluting the cadmium-containing domain through a size exclusion column equilibrated with a low-pH eluant

The term ‘positive cooperativity’ refers to an increase in equilibrium constant (K) for each step of a sequential reaction; in other words, coordination of the first metal ion facilitates the binding of the second metal ion, and so forth Experimentally, this translates into the detection of only the initial species, in this case the metal-free protein, and the final species, which

is the fully metallated holoprotein, with no detectable intermediate species Thus, with substoichiometric additions of Cd2+to apo-a-rhMT , the metal-free pro-tein will be detected together with a corresponding fraction of the metal-saturated Cd4a species if the met-allation mechanism proceeds by a positively cooper-ative pathway Alterncooper-atively, the partially filled Cd1a,

Cd2a and Cd3a intermediate species will be detected in the case of a noncooperative metallation mechanism The metallation rate of either the cooperative or non-cooperative process would depend on the preliminary conformation of the protein and the coordination properties of the incoming metal ions

Metallation of apo-a-rhMT-1a with Cd2+ was car-ried out at pH 7.3 by raising the pH of the apo-MT solution prior to the addition of the cadmium ions Previous kinetic data reported by Ejnik et al [26] showed metallation of MT with Cd2+ to be complete within the 4 ms mixing time of the stopped-flow instru-ment at room temperature From this, the metallation

of the a domain with Cd2+can be considered a nearly instantaneous reaction In addition, no evidence has been reported to show that any change occurs to the

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metal speciation after a few seconds of equilibration.

The spectroscopic data were acquired in this study

after a 2–5 min equilibration period at room

tempera-ture, to ensure that thermodynamic equilibrium was

achieved The CD spectra measured during the

metal-binding reaction (Fig 2A) at pH 7.3 show a

concomit-ant increase in CD signal intensity at 250 and 263 nm

with the addition of up to 2.4 molar equivalents of

Cd2+ before a derivative-shaped signal, with band

maximum at 263 nm, begins to dominate at 3.2

equiv-alents of Cd2+ (Fig 2A, inset) Finally, the full

com-plement of 4.0 molar equivalents of Cd2+ is required

for the strong derivative signal to be observed with

DA220 reaching positive values The UV absorption

spectra (Fig 2B) show an incremental increase in

sig-nal intensity at 250 nm with the addition of Cd2+ to the protein solution, reaching a maximum intensity at 4.0 molar equivalents of Cd2+, thus confirming the metal-binding ratio of Cd4(Scys)11

Previous reports have shown that the intermediate

Cd1a, Cd2a and Cd3a species each result in a mono-phasic CD spectrum with positive extrema at 250 nm, whereas the Cd4a species results in a derivative-shaped signal with positive and negative extrema at 260 nm and 240 nm, respectively, and a point of inflection at

250 nm, which was explained as being due to exciton splitting between the symmetric pairs of [Cd(Scys)4]2 groups in the Cd4(Scys)11binding site [27] As noncoop-erative metal binding is predicted to result in the for-mation of intermediate, partially metallated, species,

ala ala ala ala lys gly met ser gly

A M4(Scys)11 Domain of Recombinant Human MT

1

2 7 6

11

8 3

10 9

3a

2a 4a

1a

B

C

Fig 1 (A) Sequence of the a domain of

rhMT-1a, showing the connectivities of the

four divalent metal cations to the 11

cystei-nyl sulfurs The numbering of the cysteines

(1–11 starting from the N-terminus) and the

four divalent metals (1a )4a) are consistent

with the metal–thiolate cluster shown in (C).

(B) Space-filling and ribbon representations

of the Cd4a-rhMT, emphasizing the

left-han-ded wrapping of the polypeptide backbone

around the metal–thiolate cluster (C)

Isola-ted Cd 4 (S cys ) 11 cluster present in the

a domain of human MT-1a The numbering

of the cadmium and sulfur atoms

corres-pond to those in the amino acid sequence

shown in (A) Gray ¼ C; white ¼ H; blue ¼

N; red ¼ O; green ¼ Cd; yellow ¼ S.

Diagram adapted from Chan et al [44].

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these are qualitatively identifiable in the CD spectrum.

As is clearly observed in Fig 2A, addition of less than

4.0 molar equivalents of Cd2+ results in CD spectra

consistent with those observed for partially metallated

domain species, supporting the model of a

noncooper-ative metallation mechanism Although a distinction

between partially metallated intermediates and the

fully metallated holoprotein can be made on the basis

of the acquired CD spectra, quantitative analysis of

the exact species being formed in the metallation

reac-tion requires supplementary MS analysis

Figure 3 shows the corresponding MS data for the

titration of apo-a-rhMT-1a with Cd2+ at pH 7.8

fol-lowing a 2–5 min equilibration period at room

tem-perature following each metal addition The spectra on

the left side of Fig 3 are the original mass spectra,

with mass⁄ charge (m ⁄ z) values on the x-axis

illustra-ting the charge state distributions of the protein

spe-cies The spectra on the right side of Fig 3 are the

deconvoluted spectra showing the mass and identity of

the species detected The deconvoluted spectra on the

right side of Fig 3 clearly show the formation of

inter-mediate Cd1a, Cd2a and Cd3a species, with the Cd4a

species forming only after > 3 equivalents of Cd2+

have been titrated Addition of 4.0 equivalents is

required for 100% abundance of the Cd4a species

(Fig 3F), which correlates well with the sharp

deriv-ative signal in the corresponding CD spectrum At

each molar equivalent addition of Cd2+, the ratio of

the relative abundances of all cadmium-coordinated

species to the total abundance of protein detected in

the ESI mass spectrum correlated well with the total

amount of Cd2+ added, confirming that all of the

Cd2+that was titrated into the solution was

coordina-ting to the protein

Discussion

In this report, we have unequivocally shown by CD spectroscopy and ESI MS that metal binding to the a domain of human MT-1a is a noncooperative process

at physiologic pH This implies that the four equilib-rium constants describing the sequential metallation reaction are decreasing in magnitude (K1> K2>

K3> K4), albeit only marginally, as the reaction does proceed to completion upon addition of 4.0 equiva-lents of Cd2+ The previously described metallation of the two-domain protein by Co2+ indicated a simulta-neous metallation of the a and b domains, with two metal ions populating the a domain, and one in the b domain [25] All three of these metal ions were shown

to bind to independent tetrahedral tetrathiolate sites within the two domains This was followed by coordi-nation of the fourth and fifth metal ions to the a domain for completion of the metallation of this domain prior to filling of the b domain This work, as well as previous work on the metallation of MT with

Cd2+ [23], indicates that the mechanism may be sim-ilar to that of Co2+ The fact that the equilibrium con-stants for the a domain are greater than those for the

b domain may be a factor in explaining the observed metal ion distribution After coordination of the first two metal ions to the a domain in independent tetra-thiolate sites, the choice for the third incoming metal ion would be to form a bridging interaction in the

a domain or to form another independent tetrathiolate site in the b domain It is probable that the equilib-rium constant for the coordination of the first metal ion in the b domain (K1b) as an independent tetrathio-late site is greater than the equilibrium constant for the third metal ion in the a domain (K3a) with bridging

Fig 2 CD (A) and UV (B) absorption spectra

of the titration of apo-a-rhMT-1a with Cd 2+

at pH 7.3 Spectral changes were recorded

as up to 4.0 equivalents of Cd 2+ (3.3 m M ) were titrated into a solution of apo-a-rhMT-1a (15 l M ) at 22 C Spectra were recorded

at molar equivalent values of 0.0, 0.8, 1.6, 2.4, 3.2 and 4.0 of Cd 2+ at 22 C Inset: Plot

of changes in CD intensity monitored at

223, 240, 250 and 263 nm as a function of molar equivalents of Cd 2+ up to a maximum

of 4.0 equivalents.

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ligands, especially as the noncooperative metal binding

dictates that the Keqmust be decreasing as the

sequen-tial reaction proceeds Finally, K3a and K4a for the a

domain would have to be greater than K2band K3bfor

the b domain, to explain the observed filling of the

a domain prior to that of the b domain

Although the metal-binding reaction has been shown

to proceed noncooperatively, this does not mean that

a distinct order of metal binding to each of the four

sites in the domain does not still exist The fact that

the polypeptide backbone adopts only one

conforma-tion around the metal–thiolate cluster with specific

connectivities does suggest that both the sequential

metal-binding and metal-dependent protein-folding

mechanisms occur in an energy-directed way The fact

that we have been able to detect the intermediate

spe-cies in the metallation reaction indicates that the order

of metal binding will one day be elucidated In fact,

strong evidence already exists for the site of the initial metallation reaction, a proposal first made by Robbins

et al upon elucidation of the crystal structure of rat liver MT-2 [15] They stated that the most likely metal-lation site for the coordination of the first metal ion would be the four cysteine residues at the C-terminus

of the protein, which are the only four consecutive cysteines to coordinate a single metal ion within the metal–thiolate cluster This hypothesis was further sup-ported in a study by Munoz et al [28] through investi-gation of a small peptide fragment corresponding to the C-terminal residues 49–61 of rabbit liver MT-2a, which encompassed the four consecutive cysteine resi-dues The results showed the ability of the peptide to coordinate a single metal ion, which induced a metal-dependent fold of the peptide in the same configur-ation as the holoprotein Finally, results from a computational molecular dynamics study carried out

A

B

C

D

E

F

Fig 3 ESI mass spectra of the titration of

apo-a-rhMT-1a with Cd2+at pH 8.0 Spectral

changes were recorded as aliquots of Cd 2+

(3.3 m M ) were titrated into a solution of

apo-a-rhMT-1a (21 l M ) at 22 C Spectra

were recorded at Cd 2+ molar equivalent

val-ues of (A) 0.0, (B) 0.8, (C) 1.6, (D) 2.4, (E)

3.2, and (F) 4.0 The left side of the figure

shows the measured mass spectra labeled

with the charge states of the molecular

spe-cies The right side of the figure shows the

deconvoluted spectra with the

reconstruc-ted masses that correspond to the

meas-ured spectra Calculated mass: Cd4a-rhMT,

4083.0 Da; Cd 1 a-rhMT, 4193.4 Da;

Cd2a-rhMT, 4303.8 Da; Cd 3 a-rhMT,

4414.2 Da; Cd4a-rhMT, 4524.6 Da.

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on the a domain of human MT-1a [29] showed that

the single remaining metal ion in the demetallation

reaction was the C-terminal metal ion, indicating that

occupancy of this metal site resulted in the least strain

on the complex, and thus the lowest strain energy The

subsequent metal-binding order of the remaining three

metal ions in the a domain still requires elucidation

The detection of stable, partially metallated domain

intermediates in the sequential metallation pathway of

MT is sufficient evidence to implicate a potential role

for these species in vivo Specifically, reconstitution of

apo-Zn enzymes by Zn7-MT has been shown to occur

readily in vitro, the most well-studied being

apo-car-bonic anhydrase [30–33], and has been predicted to

occur in vivo on the basis of analysis of the Zn2+pools

in Erlich cells [34,35]; however, the fate of MT after

metal ion donation has not been determined

Degrada-tion by cooperative demetallaDegrada-tion of the remaining six

metal ions following the loss of the first Zn2+ would

be, overall, an energetically expensive process, and

would therefore be expected to be highly unfavorable

However, the demonstrated stability of the partially

metallated species in this study provides support for

the alternative scenario in which the partly

demetall-ated MT product persists in vivo following metal ion

donation But if this is true, then what happens to the

remaining metal ions that are bound to the MT

mole-cule? Investigation into how the domain reacts in the

event of metal ion donation will be of significant value

for understanding the role of MT in the cellular

meta-bolism of Zn2+ Despite the relatively large

thermo-dynamic stability of the metal–thiolate clusters in MT,

the metals have been shown to be kinetically labile in

terms of both intramolecular and intermolecular metal

exchange reactions [36] Thus, it is probable that a

spe-cific metal site is more labile than the others, and will

therefore be the preferred site of demetallation Kinetic

studies of Zn2+ extraction from Zn7ba-MT and

Zn4a,Ag6b-MT demonstrated that the two domains

differ with respect to the lability of the zinc ions and

that, despite the increased thermodynamic stability of

the a domain with Zn2+over the b domain, the Zn2+

sites in the a domain were shown to be more labile

[37] It is possible that upon loss of the first metal ion,

the three remaining metal ions in the a domain

rear-range, either independently or in conjunction with the

b domain, to position another metal ion into the more

labile site in preparation for donation to another

metal-requiring apo-enzyme

A considerable amount of effort has been directed in

the recent past to understanding the mechanism of

metal ion donation to apo-Zn2+-requiring enzymes,

with the most detailed proposal involving a redox cycle

in which oxidative release of Zn2+ from Zn7-MT occurs by the formation of disulfide or S–O bonds upon interaction with cellular oxidants [38–40] This proposal, however, is based on the assumption that the metallation mechanism of apo-MT is cooperative, and as such, only the metal-free and fully metallated holoprotein are present in vivo [41] Although strong evidence exists for a critical balance between the

MT⁄ thionein pair [42,43] the evidence presented in this article demonstrates that alternative mechanisms for

Zn2+ probably exist Moreover, the highly reducing environment of the cell, in which concentrations of reduced glutathione as high as 3 mm have been detec-ted, supports the theory generated by the data presen-ted, in which partially metallapresen-ted, yet reduced, forms

of MT can readily exist in the cell In fact, the non-cooperative metallation and the subsequently decrea-sing equilibrium constants indicate that, from a coordination chemistry point of view, it is not only acceptable, but probable, that MT exists with a vacant site in vivo in the presence of limiting concentrations of free group 11 and 12 metal ions Thus, it is proposed that MT only resides in the fully metallated holopro-tein upon influx of excess free metal ions into the cell Upon overproduction of the metal-free protein in response to the influx, redistribution of the metal ions results in an average of less than the full complement

of seven metals, a situation encountered in prepara-tions of rabbit liver MT, where excess metals are used for induction and subsequent isolation The implica-tion of this proposal is that those metal ions that are sequestered by the protein could be holding the poly-peptide in a stable conformation, allowing the free thi-olate ligands to carry out vitally important chemistry

in the cell Specifically, MT has been implicated more recently in antioxidative, antiapoptotic and anti-inflammatory roles in vivo through reaction of the cysteine sulfur groups with reactive oxygen species, primarily in the brain and heart organs [7–11]

In summary, the metal-binding reactivity of the iso-lated a domain of human MT-1a was investigated, with specific emphasis on resolving the debate concern-ing the cooperative nature of the metal-bindconcern-ing mech-anism The metallation reaction of the metal-free a domain with Cd2+ was determined to proceed by a noncooperative mechanism by the detection of parti-ally metallated intermediate species under limiting

Cd2+conditions These species are predicted to be sta-ble in vivo and may even be the predominant form of

MT in the cell, due to the very strict regulation of free metal ions The vacant metal site(s) in the partially metallated species offer free cysteinyl thiolate ligands

in the reducing environment of the cell for scavenging

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of damaging reactive oxygen species, which supports

the proposal of MT as a potent antioxidant and

anti-apoptotic protein

Experimental procedures

Materials

The chemicals used were: cadmium sulfate (Fisher Scientific,

Ottawa, ON, Canada); ultrapure Tris buffer (ICN

Biomole-cules, Irvine, CA, USA); ammonium formate buffer

(Ald-rich, Oakville, ON, Canada); isopropyl-b-d-thiogalactoside

(Sigma-Aldrich, Oakville, ON, Canada); ammonium

hydrox-ide (BDH Chemicals⁄ VWR, Mississauga, ON, Canada);

for-mic acid (J T Baker Chefor-mical Co., Phillipsburg, NJ, USA);

and hydrochloric acid (Caledon, Georgetown, ON, Canada)

All solutions were made with >16 MWÆcm)1deionized water

(Barnstead Nanopure Infinity, Dubuque, IA, USA)

HiTrapTM SP HP ion exchange columns (Amersham

Bio-sciences⁄ GE Healthcare, Piscataway, NJ, USA), superfine

G-25 Sephadex (Pharmacia⁄ Pfizer, Oakville, ON, Canada)

and a stirred ultrafiltration cell (Amicon Bioseparations⁄

Millipore, Bedford, MA, USA) with a YM-3 membrane

(3000 MWCO) were used in the protein purification steps

Protein preparation

The recombinant a domain of human MT-1a (sequence

shown in Fig 1A) was produced by overexpression in

E coli BL21(DE3) cells as an S-tag fusion protein The

cells were grown at 37C in LB medium containing 50 lm

CdSO4and 50 lgÆmL)1of kanamycin Protein

overexpres-sion was induced at an A600 of 0.4–0.6 by the addition of

isopropyl-b-d-thiogalactoside (final concentration 0.7 mm)

The protein product was stabilized by the addition of

CdSO430 min after isopropyl-b-d-thiogalactoside induction

to a final concentration of 200 lm The cells were harvested

by centrifugation at 7459 g for 15 min using an Avanti

J-series centrifuge (Beckman Coulter, Mississauga, ON,

Canada) with JLA-9.1000 rotor, resuspended in 10 mm

Tris⁄ HCl buffer (pH 7.4), and lysed with a French press

The lysed cellular fraction was centrifuged at 20 442 g for

40 min using an Avanti J-series centrifuge with JLA-25.50

rotor to remove the cellular debris The supernatant was

loaded onto an SP ion exchange cartridge for protein

separ-ation, and the column was washed with argon-saturated

10 mm Tris⁄ HCl buffer (pH 7.4) The Cd2+

-substituted

MT was eluted with a gradient of 5–20% NaCl in 10 mm

Tris⁄ HCl (pH 7.4) Protein fractions were collected on the

basis of strong UV absorption at 250 nm corresponding to

the ligand-to-metal charge transfer transitions of the SfiCd

of the metal–thiolate clusters The pooled protein fractions

collected from the SP ion exchange column were

concentra-ted to a volume of 15 mL using the Amicon ultrafiltration

cell with a YM-3 cellulose membrane (3000 MWCO) under

N2 pressure The S-tag was cleaved from the concentrated protein fraction using a Thrombin CleanCleaveTM Kit (Sigma) by stirring the protein with the thrombin-coated beads under argon overnight at 4C The cleaved protein was separated from the thrombin beads, and eluted from a superfine G-25 Sephadex column with Ar-saturated 10 mm Tris buffer (pH 7.4) to desalt prior to loading onto the SP ion exchange column for purification The fractions collec-ted from the SP were pooled and concentracollec-ted to 8 mL, using the Amicon ultrafiltration cell

Further protein preparation for metal-binding studies

Metal-free apo-a-rhMT was prepared by eluting the throm-bin-cleaved Cd-bound protein from a G-25 column equili-brated with a low-pH eluant Apo-MT prepared for the

CD studies was eluted with 10 mm Tris⁄ HCl (pH 2.7), whereas the apo-MT prepared for the MS studies was

elut-ed with deionizelut-ed water adjustelut-ed with HCOOH to pH 2.8 Elution of the protein with a low-pH eluant effectively removes the metal ions from the protein; they separate from the protein band through the size-exclusion processes

on the column Preparation of apo-MT by this method sim-ultaneously desalts the solution by the same size-exclusion process As MT is devoid of aromatic amino acids, the metal-free protein fractions were detected by UV absorption

at 220 nm, which corresponds to the electronic transitions generated by the polypeptide backbone The apo-a-rhMT used for the metal-binding studies was found to have con-centrations ranging from 10 to 20 lm, as determined by

UV absorption at 220 nm (e220¼ 40 000 LÆmol)1Æcm)1) and atomic absorption spectroscopy following complete metalla-tion with Cd2+ Cadmium solutions were prepared in

10 mm Tris⁄ HCl (pH 7.4) (for CD studies) or 25 mm ammonium formate (pH 7.4) (for MS studies) to a final concentration of 3.0–3.3 mm as determined by atomic absorption spectroscopy The final samples were thoroughly evacuated and Ar-saturated to remove the bulk of the oxy-gen from the solutions, in order to prevent oxidation of the metal-free protein upon raising of the pH for the metalla-tion studies

Metallation of apo-a-rhMT with Cd2+at pH 7

CD⁄ UV absorption spectroscopy The pH of apo-a-rhMT solution (13 lm) was raised from 2.7 to 7.3 by the addition of 10% NH4OH prior to the addition of Cd2+(3.3 mm) Cd2+was added in 0.8 molar equivalent increments up to 4.0 equivalents, with thorough mixing after each titration CD and UV absorption spectra were recorded at each addition after a 2–5 min delay, in which the reaction could reach equilibrium conditions

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The pH of apo-a-rhMT solution (20 lm) was raised from

2.8 to 7.8 by the addition of 10% NH4OH prior to the

addition of Cd2+ (3.3 mm) Cd2+ was added in 0.8 molar

equivalent increments up to 4.0 equivalents, with thorough

mixing after each titration Mass spectra were acquired at

each addition after a 2–5 min delay, in which the reaction

could reach equilibrium conditions

Analytical and spectroscopic measurements

CD spectroscopy

CD spectra were acquired on a Jasco J810

spectropolarime-ter in a 1 cm quartz cuvette at room temperature (22C)

and recorded using spectra manager v.1.52.01 (Jasco

Inc., Easton, MD, USA) software The wavelength range

of 200–300 nm was scanned continuously at a rate of

50 nmÆmin)1 with a bandwidth of 2 nm All spectra were

baseline corrected with 10 mm Tris⁄ HCl The spectral data

were organized and plotted using origin v.7.0383

UV absorption spectroscopy

UV spectra were acquired on a Cary 5G UV-Vis-NIR

spectrophotometer (Varian Canada Inc., Mississauga, ON,

Canada) in a 1 cm quartz cuvette at room temperature

(22C) and recorded using the cary win uv scan

soft-ware application The wavelength range of 200–300 nm

was scanned continuously All spectra were baseline

cor-rected with 10 mm Tris⁄ HCl The spectral data were

organized and plotted using origin v.7.0383

MS

Mass spectra were acquired on an ESI-TOF mass

spectro-meter (Waters Micromass Inc., Mississauga, ON, Canada)

at room temperature (22C), and recorded using the mass

lynxv.4.0 software package The ESI-TOF mass

spectro-meter was calibrated with a solution of NaI The scan

con-ditions for the spectrometer were: capillary, 3000.0 V;

sample cone, 39.0 V; RF lens, 450.0 V; extraction cone,

11.0 V; desolvation temperature, 20.0C; source

tempera-ture, 80.0C; cone gas flow, 51 LÆh)1; and desolvation gas

flow, 528 LÆh)1 The m⁄ z range was 500.0–1600.0, the scan

mode was continuum, and the interscan delay was 0.10 s

The observed spectra were reconstructed using the max

ent1 program from the mass lynx v.4.0 software package

Acknowledgements

We thank NSERC of Canada for financial support

(M J Stillman) and Postgraduate Scholarship (K E

Rigby Duncan) We also thank Professor R J

Pudde-phatt for use of the ESI mass spectrometer, funded by the Canada Research Chair program, and Doug Hair-sine for advice and discussion on the operation of the ESI mass spectrometer

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