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Members of the family include the pyruvate dehydrogenase complex PDHC, which catalyzes the conversion of pyruvate to acetyl-CoA and so links glycolysis and the citric acid cycle; the 2-o

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the archaeon Thermoplasma acidophilum ) recombinant expression, assembly and characterization

Caroline Heath1, Mareike G Posner1, Hans C Aass1, Abhishek Upadhyay2, David J Scott3,

David W Hough1and Michael J Danson1

1 Centre for Extremophile Research, Department of Biology and Biochemistry, University of Bath, UK

2 Department of Biology and Biochemistry, University of Bath, UK

3 National Centre for Macromolecular Hydrodynamics, School of Biosciences, University of Nottingham, Sutton Bonington, UK

In aerobic bacteria and eukaryotes, a family of

2-oxoacid dehydrogenase multi-enzyme complexes

(OADHCs) functions in the pathways of central

metabolism The complexes are responsible for the

oxi-dative decarboxylation of 2-oxoacids to their

corre-sponding acyl-CoAs Members of the family include

the pyruvate dehydrogenase complex (PDHC), which

catalyzes the conversion of pyruvate to acetyl-CoA

and so links glycolysis and the citric acid cycle; the

2-oxoglutarate dehydrogenase complex (OGDHC),

which catalyzes the conversion of 2-oxoglutarate to

succinyl-CoA within the citric acid cycle; and the

branched-chain 2-oxoacid dehydrogenase complex (BCOADHC), which oxidatively decarboxylates the branched-chain 2-oxoacids produced by the transami-nation of valine, leucine and isoleucine The complexes comprise multiple copies of three component enzymes: 2-oxoacid decarboxylase (E1), dihydrolipoyl acyl-trans-ferase (E2) and dihydrolipoamide dehydrogenase (E3) [1–3] E2 forms the structural core of the complex, with multiple polypeptide chains associating into octa-hedral (24-mer) or icosaocta-hedral (60-mer) configurations, depending on the particular complex and the source organism [2,4] E1 and E3 bind noncovalently to the

Keywords

Archaea; metabolism; multi-enzyme

complex; 2-oxoacid dehydrogenase;

thermophile

Correspondence

M J Danson, Centre for Extremophile

Research, Department of Biology and

Biochemistry, University of Bath, Bath,

BA2 7AY, UK

Fax: +44 1225 386779

Tel: +44 1225 386509

E-mail: M.J.Danson@bath.ac.uk

(Received 29 June 2007, revised 23 August

2007, accepted 24 August 2007)

doi:10.1111/j.1742-4658.2007.06067.x

The aerobic archaea possess four closely spaced, adjacent genes that encode proteins showing significant sequence identities with the bacterial and eukaryal components comprising the 2-oxoacid dehydrogenase multi-enzyme complexes However, catalytic activities of such complexes have never been detected in the archaea, although 2-oxoacid ferredoxin oxidore-ductases that catalyze the equivalent metabolic reactions are present In the current paper, we clone and express the four genes from the thermophilic archaeon, Thermoplasma acidophilum, and demonstrate that the recombi-nant enzymes are active and assemble into a large (Mr¼ 5 · 106) multi-enzyme complex The post-translational incorporation of lipoic acid into the transacylase component of the complex is demonstrated, as is the assembly of this enzyme into a 24-mer core to which the other components bind to give the functional multi-enzyme system This assembled complex

is shown to catalyze the oxidative decarboxylation of branched-chain 2-oxoacids and pyruvate to their corresponding acyl-CoA derivatives Our data constitute the first proof that the archaea possess a functional 2-oxo-acid dehydrogenase complex

Abbreviations

BCOADHC, branched-chain 2-oxoacid dehydrogenase complex; CoASH, coenzyme-A; DLS, dynamic light scattering; E1, 2-oxoacid

decarboxylase; E2, dihydrolipoyl acyl-transferase; E3, dihydrolipoamide dehydrogenase; FOR, ferredoxin oxidoreductase; IPTG, isopropyl thio-b- D -galactoside; Mr, relative molecular mass; OADHC, 2-oxoacid dehydrogenase complex; OGDHC, 2-oxoglutarate dehydrogenase multienzyme complex; PDHC, pyruvate dehydrogenase complex; TPP, thiamine pyrophosphate.

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E2 core E1 may occur as a homodimer or as an a2b2

hetero-tetramer, depending upon the source and the

type of complex, although in all cases E3 is a dimer of

identical subunits

E2 also forms the catalytic core of the complex; a

lipoyl moiety, covalently attached to a lysine residue in

the lipoyl domain of the E2, serves as a swinging arm,

connecting the active sites of each enzyme and

chan-nelling substrate through the complex [2,3] Thus, E1

catalyzes the thiamine pyrophosphate (TPP)-dependent

decarboxylation of the 2-oxoacid and the transfer

of the resulting acyl group to the lipoic acid of E2

E2 then transfers the acyl-group to coenzyme-A

(CoASH), after which E3 serves to reoxidize the

dihydrolipoyl moiety It does so by the reduction of

the noncovalently bound cofactor FAD, in conjunction

with a protein disulfide bond and an amino acid base,

all of which are themselves then reoxidized by NAD+

to form NADH

In Archaea [5] and anaerobic bacteria, the

equiva-lent oxidation of 2-oxoacids is catalyzed by an

un-related, and structurally more simple, family of

2-oxoacid ferredoxin oxidoreductases (FORs) This

comprises the pyruvate FOR, the 2-oxoglutarate FOR

and the 2-oxoisovalerate FOR, which catabolize the

oxidative decarboxylation of pyruvate, 2-oxoglutarate

and the branched-chain 2-oxoacids, respectively [6–8]

The pyruvate FOR from the halophilic archaeon

Halo-bacterium halobium is an a2b2 structure [9], whereas in

Sulfolobus solfataricus and Aeropyrum pernix it is an

ab dimer, and an octamer (a2b2c2d2) in Pyrococcus

furiosus, Methanothermobacter thermoautotrophicum

and Archaeoglobus fulgidus [reviewed in 5,8] The

cata-lytic reaction of FORs does not involve a lipoic acid

moiety or NAD+; rather, the acyl-moiety formed on

decarboxylation of the 2-oxoacid is handed on directly

to CoASH, and the reducing equivalents to ferredoxin

via the enzyme’s iron-sulfur centre [6–8]

No OADHC activity has ever been detected in any

archaeon [5] However, detection of E3 and lipoic acid

in various archaea [10–12] led to the discovery of a

putative OADHC operon in Haloferax volcanii [13]

and our subsequent detection of similar putative

ope-rons in the genome sequences of the aerobic archaea

Thermoplasma acidophilum, S solfataricus, Sulfolobus

acidocaldarius, A pernix, Pyrobaculum aerophilum,

Halobacterium NRC1 and Ferroplasma acidophilum

(M G Posner, unpublished data)

We have previously expressed the E1a and E1b

genes of the putative OADHC from T acidophilum in

Escherichia coli and shown the recombinant proteins

to assemble into an a2b2 enzyme that catalyzes the

decarboxylation of the branched-chain 2-oxoacids and

pyruvate [14] In the current paper, we report the clon-ing and expression of the E2 and E3 genes of the same operon from T acidophilum, and the in vitro assembly and characterization of an active 2-oxoacid dehydro-genase complex

This, then, is the first evidence that the putative OADHC operon in an archaeon encodes a 2-oxoacid dehydrogenase multi-enzyme complex that is func-tional in vitro and therefore may have physiological significance

Results

Expression and purification of the E1, E2 and E3 components

The E1 component The E1 a2b2 recombinant enzyme was produced as described previously, and was shown to be catalyti-cally active with the branched-chain 2-oxoacids 4-methyl-2-oxopentanoate, 3-methyl-2-oxopentanoate and 3-methyl-2-oxobutanoate, and with pyruvate [14]

By dynamic light scattering (DLS), its Mr was found

to be 168 000 (± 6000), consistent with the value

of 165 000 determined by gel filtration [14] and the expected value of 157 000 from the protein sequences

The E2 component The gene encoding the E2 component was PCR-ampli-fied from T acidophilum genomic DNA and cloned into the pET28a expression vector, as described in Experimental procedures The E2 protein was then expressed in two host systems: E coli BL21(DE3) cells,

in medium supplemented with lipoic acid but without isopropyl thio-b-d-galactoside (IPTG) induction, and

E coliBL21(DE3)pLysS cells without supplementation but with IPTG induction Both methods yielded solu-ble E2 protein, although the level of expression was significantly greater in the pLysS cells In each case, E2 was purified to > 95% homogeneity using His-Bind affinity chromatography followed by anion exchange chromatography

The E2 Mrvalues predicted from the published gene sequence are 46 276 for unlipoylated protein and

46 464 for the polypeptide possessing a single lipoyl residue Accordingly, mass spectrometric analysis revealed that the E2 expressed in E coli grown in lipoic acid-supplemented medium comprised an approximately equimolar mixture of unlipoylated (Mr¼ 46 273) and lipoylated (Mr¼ 46 461) protein Furthermore, from MS-analysis of tryptic fragments,

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lipoylation was shown to have occurred at K42, which

by sequence comparisons corresponds to the lipoylated

lysine residue in bacterial E2 components (Fig 1)

However, the E2 protein produced by expression in

induced cells, without lipoic acid supplement to the

growth medium, was < 5% lipoylated As reported

below, consistent with these data is the observation

that only the complex assembled using the lipoylated

E2 component showed detectable catalytic activity in

the overall complex assay

The E3 component

The gene encoding the E3 component was

PCR-amplified from T acidophilum genomic DNA and

cloned into the pET28a expression vector, as

described in Experimental procedures Expression of

the E3 gene was carried out in E coli BL21(DE3)

cells Small-scale expression trials with induced versus

uninduced host cells revealed a higher E3 activity in

the soluble cell extract from uninduced cells, and this

was confirmed by SDS⁄ PAGE The soluble protein

was purified to > 95% homogeneity by heat

precipi-tation at 60C and His-Bind affinity

chromatogra-phy The absorption spectrum of the purified protein

showed peaks at 375, 450 and 475 nm that are

char-acteristic of the presence of FAD in the enzyme;

using a molar absorption coefficient for FAD of

11 300 m)1Æcm)1 at 455 nm [15], the flavin content

was calculated to be 1.0 (± 0.1) FAD per

polypep-tide (Mr¼ 49 867) Analytical gel filtration revealed

an Mr¼ 100 000 for the purified enzyme, and DLS

gave a similar value (117 000 ± 2000), suggesting a

dimeric structure, as has been found for the bacterial

and eukaryotic enzymes The maximal specific activity

of the enzyme was found to be 22 (± 1) lmolÆ

min)1Æmg)1, a value that is considerably higher than

the overall complex activity (see below)

Assembly of OADHC from the recombinant components

Complex assembly When E1, E2 and E3 were incubated at 55C for

10 min in 20 mm sodium phosphate buffer, pH 7.5, containing 2 mm MgCl2 and 0.2 mm TPP, prior to assay, whole complex activity was subsequently detected with the branched-chain 2-oxoacids 4-methyl-2-oxopentanoate, 3-methyl-2-oxopentanoate and 3-methyl-2-oxobutanoate, and with pyruvate The 10-min incubation is necessary to allow E1-TPP bind-ing [16], but no increase in rate was seen when the incubation, after subunit mixing, was extended to 1 h

at 4C, 25 C or 55 C

With an E2 : E3 molar ratio fixed at 1 : 1 (E2 poly-peptide to E3 dimer), titration with E1 resulted in an increase in whole complex activity until a maximum was reached at a molar ratio (E1⁄ E2) of approximately 2–3 : 1 [E1 a2b2 tetramer to E2 polypeptide] (Fig 2) However, a reduction of the E3 ratio did not cause a significant change in whole complex activity, and by investigating the mixing of various amounts of the complex components it was found that maximum OADHC activity was achieved when the E1, E2 and E3 subunits were mixed in a molar stoichiometry of

3 : 1 : 0.1 However, as described below, this stoichio-metry does not equate to the amounts of the three enzymes in the assembled complex

B subtilis PDHC

B subtilis BCOADHC

Tp acidophilum OADHC

E coli OGDHC

E coli PDHC (lipoyl domain 3)

Fig 1 Alignment of various E2 sequences around the lipoylated

lysine residue The T acidophilum E2 protein sequence was aligned

with those of the E2 components of the following OADHCs using

the CLUSTALW multiple sequence alignment program: Bacillus subtilis

PDHC; B subtilis BCOADHC; E coli OGDHC; E coli PDHC (lipoyl

domain 3) Residues 27–53 of the T acidophilum sequence are

shown, along with the aligned regions of the other E2 sequences,

and the lysine residue that is lipoylated in each sequence is marked

by a (*).

0 0.01 0.02 0.03 0.04 0.05 0.06 0.07 0.08 0.09 0.1

Molar Ratio of E1:E2

Fig 2 Whole complex activity as a function of the E1 : E2 ratio Lipoylated E2 and E3 were mixed in a molar ratio of 1 : 1 (E2 poly-peptide to E3 dimer), and to this mixture varying amounts of E1 were added The mixture was then incubated at 55 C for 10 min

in the presence of 2 m M MgCl2and 0.2 m M TPP, following which samples were taken and assayed for whole complex activity (expressed as A (absorbance units).min)1) using the substrate 3-methyl-2-oxopentanoate The molar ratio of E1 : E2 is expressed

as E1 a2b2tetramer to E2 polypeptide.

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OADHC activity

The whole complex activity detected with

4-methyl-2-oxopentanoate, 4-methyl-2-oxopentanoate,

3-methyl-2-oxobutanoate, and pyruvate, but not with

2-oxogluta-rate, is entirely consistent with the substrate specificity

observed for the recombinant E1 enzyme in the

absence of the other complex components [14] The

relative activities are given in Table 1, along with those

for the isolated E1 component and for the BCOADHC

from bovine kidney Using 3-methyl-2-oxopentanoate

as substrate, the assembled T acidophilum complex

exhibited a hyperbolic dependence of velocity on the

2-oxoacid concentration, with KM¼ 250 (± 40) lm

and Vmax¼ 4 (± 0.1) lmolÆmin)1Æmg)1(E2) This

spe-cific activity is comparable to that of the Bacillus

stearothermophilus PDHC [8–10 lmo1Æmin)1Æmg)1(E2)

[17]

Relative molecular mass of the E2 core and the

assembled complex

Analytical centrifugation and DLS were used to

deter-mine the Mr of both the E2 core and the assembled

complex

E2 core

Sedimentation velocity analysis was carried out at

40C as described in Experimental procedures on

recombinant E2 that was 50% lipoylated and had been

purified by His Bind (Novagen, Merck Biosciences

Ltd., Nottingham, UK) and then anion-exchange

chro-matography The sedimentation coefficient

distribu-tions showed a major symmetrical peak constituting

95% of the total protein (Fig 3) Analysis of the data

by direct fitting using the finite element solution of the Lamm equation in sedfit [18], gave a sedimentation coefficient (corrected to water at 20C and infinite dilution; s20,w)¼ 27 (± 1) S (Svedberg units; 1S =

10)13 seconds) and an Mr¼ 1.1 (± 0.1) · 106 From the E2 polypeptide Mrof 46 276, the E2 protein there-fore comprises 23.8 polypeptides; that is, it assembles into a core of 24 subunits possessing octahedral sym-metry

DLS analysis at 55C, the optimum growth temper-ature of T acidophilum, gave an E2 Mr value¼ 1.0 (± 0.1) · 106, in good agreement with the value deter-mined by analytical centrifugation This E2 sample was nonlipoylated, demonstrating that lipoylation is not a prerequisite for assembly of the core Interest-ingly, the Mr of the same E2 at 25C, with no prior heat treatment at 55C, was estimated by DLS to be

55 000, close to the sequence-predicted monomer value (46 276); this indicates that the assembly of E2 into a 24-mer core is temperature dependent

The assembled complex Sedimentation velocity analysis at 40C of assembled complex, created by mixing the components in a

3 : 1 : 0.1 (E1 a2b2: E2 polypeptide: E3 a2) molar ratio, revealed three discrete protein peaks with s20,w values of 50S (24% of total protein), 19S (8%) and 6S

Table 1 Substrate specificities of the T acidophilum 2-oxoacid

dehydrogenase complex The T acidophilum assembled complex

was assayed as described in Experimental procedures For

3-methyl-2-oxopentanoate, Vmax¼ 4 lmolÆmin –1 Æmg –1 (E2), and

KM ¼ 250 l M ; other activities were determined at saturating

sub-strate concentrations.

2-Oxoacid substrate

Ratio of specific activities

T acidophilum

Bovine kidney BCOADHC b Assembled

a Data from [14] b Data from [25].

Fig 3 Sedimentation coefficient distributions of the E2 protein Sedimentation velocity of lipoylated E2 protein was carried out at

40 C as described in Experimental procedures The sedimentation velocity distribution was obtained by the c(s) method [34] using the program SEDFIT , and the data were then directly fitted using the finite element solution of the Lamm equation in SEDFIT [18] to give values of the sedimentation coefficient in the buffer of sedimenta-tion [20 m M Tris ⁄ HCl (pH 8.5), 0.4 M NaCl and 1 m M phenyl-methanesulfonyl fluoride].

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(68%), respectively Unfortunately, attempts to fit

these data using the finite element solution of the

Lamm equation in sedfit [18] were unsuccessful, thus

failing to give Mr values for these proteins Using the

relationship that s (Mr)2⁄ 3 for globular proteins, and

incorporating the values of Mr¼ 6.1 · 106 and

s20,w¼ 60S for the E coli PDHC [19], an

approxi-mate value of Mr¼ 4.7 · 106 was calculated for what

is assumed to be an assembled Thermoplasma complex

of 50S

DLS is better able to deal with the polydispersity in

the sample of assembled complex Analysis of the

auto-correlation curve using the volume distribution

algo-rithm gives an Mrof 5.0 (± 0.2)· 106for the complex

at 55C, in close agreement with that estimated by

sed-imentation velocity experiments described above

To investigate the identity of the species in the

assembled complex mixture, analytical gel filtration

on SuperdexTM200 (GE Healthcare, Chalfont St Giles,

UK) was carried out Three protein species were

observed (Fig 4), one eluting in the column exclusion

volume (where Mr> 1.3· 106), one of Mr 160 000,

and a third minor peak at Mr 100 000 Whole

com-plex activity was only detected in fractions at the

exclusion volume, whereas E1 activity was detected in

the second peak and E3 in the third SDS⁄ PAGE of

protein from the exclusion volume peak revealed three

protein bands, corresponding to E1a, E1b and E2⁄ E3

(the last two proteins run together due to their similar

polypeptide size) The second peak contained

predomi-nantly excess E1 protein, whilst the third minor peak comprised E1 and E3 protein that had not been com-pletely separated In repeat experiments, uncomplexed E3 was not always detectable

Thus it is concluded that the species of Mr¼ 5 · 106

is assembled, catalytically active whole complex Given that the molar ratio of E2 : E3 (E2 polypeptide: E3 a2)

is likely to be 1 : 0.1 at a maximum (that is, the ratio

of mixed components), then an Mr of 5.0· 106 would correspond to an approximate stoichiometry (E1 a2b2: E2 polypeptide: E3 a2) of 1 : 1 : 0.1 The other major peak in the sedimentation velocity analysis (6S) is pre-sumably excess E1 The minor 19S species remains unidentified, although it should be noted that a 19.8S species was also observed in the assembled E coli PDHC, where it was concluded that it had the proper-ties of an incomplete aggregate of the component enzymes based on a trimer of the E2 chain [19]

Discussion

As described in the introduction, the genomes of aero-bic archaea contain four genes whose translated pro-tein products show sequence identities to the E1a, E1b, E2 and E3 components of the 2-oxoacid dehydro-genase multi-enzyme complexes of aerobic bacteria and eukarya [reviewed in 5] Furthermore, the genes appear to be arranged in an operon, transcriptional evidence for which has recently been gained in the hal-ophilic archaeon, H volcanii [20] The presence of

Elution volume (mL)

1

3 1

3 1

2

3 1

2

3

Enzyme activity

Complex E1 E3

45.0

31.0

21.5

66.2 97.4 116.3 210.0

M 1 2 3

E2 and E3 E1α E1 β

A

280

Fig 4 Analytical gel filtration and SDS ⁄ PAGE analysis of assembled OADHC Assembled OADHC was created by mixing the recombinant protein components in a 3 : 1 : 0.1 (E1 a2b2: E2 polypeptide: E3 a2) molar stoichiometry, followed by incubation at 55 C for 10 min in the presence of 2 m M MgCl2 and 0.2 m M TPP (A) Gel filtration of the assembled complex was carried out at 25 C as described in Experimental procedures, and the fractions were assayed for whole complex, E1 and E3 catalytic activity Active fractions are indicated by bars above the elution profile (B) Fractions were also analyzed by SDS ⁄ PAGE M, marker proteins with their Mr values given in kDa Lanes 1–3 correspond

to protein peaks 1–3 from the gel filtration; the identity of the component polypeptides is indicated alongside the gel.

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these genes is unexpected, as all the archaea possess

ferredoxin oxidoreductases that catalyze the equivalent

oxidation of the same 2-oxoacids as those used by the

bacterial and eukaryal dehydrogenase complexes;

moreover, activity of the 2-oxoacid dehydrogenase

complexes has never been detected in any archaeon

The obvious question raised by these observations is

whether or not the archaeal ‘OADHC’ genes actually

encode functional proteins that assemble into a

multi-enzyme complex The E1 component defines the

sub-strate specificity of the whole complex, and we have

previously reported heterologous expression of the

a2b2 E1 enzyme from T acidophilum and shown it to

be catalytically active with the branched-chain

2-oxo-acids and pyruvate [14] In the current paper, the E2

and E3 genes have also been successfully cloned and

expressed as soluble proteins in E coli, and their

cata-lytic activities have been demonstrated

Generation of an active E2 enzyme requires

tion of a specific lysine residue In E coli the

lipoyla-tion of its own E2 components can occur via two

routes [21,22] The endogenous pathway involves the

covalent attachment of a C-8 intermediate of fatty acid

biosynthesis to the target lysine on E2 by enzyme LipB;

subsequently, LipA catalyzes the incorporation of

sul-fur atoms to generate the lipoic acid moiety However,

if lipoic acid is supplied in the growth medium, E coli

preferentially uses its exogenous pathway, which

employs lipoate protein ligase A; this enzyme catalyzes

the adenylation of lipoic acid after uptake into the cell

and its subsequent transfer to the E2 lysine residue

Knowing that the lipoylation process can take place

across the species barrier, albeit with varying

efficien-cies [2, and references therein], lipoylation of

recombi-nantly expressed Thermoplasma E2 was tested and

optimized Up to 50% lipoylation was achieved when

the rate and level of expression in E coli was slowed

down by decreasing the growth temperature and

avoid-ing induction, whilst at the same time supplementavoid-ing

the growth medium with lipoic acid

Clearly, therefore, the E coli machinery is able to

rec-ognize the lipoyl-domain of the Thermoplasma E2

enzyme, the target lysine of which is flanked by D and V

residues, as it is in the E2 protein of the E coli OGDHC

and of the Bacillus subtilis BCOADHC (Fig 1)

How-ever, in addition to the identity of the neighbouring

residues, it is the exact positioning of the lysine in the

lipoyl domain that is fundamental to target lysine

recog-nition [23], implying that the fold of the Thermoplasma

enzyme has been conserved in this region

Whilst the Thermoplasma recombinant E2 has not

been assayed for catalytic activity in isolation,

assem-bly of the whole active complex from its individually

expressed components shows that it is indeed a func-tional enzyme This assembly process, studied by both analytical ultracentrifugation and DLS, has been dem-onstrated to involve the formation of a 24-mer E2 core, which binds E1 and E3 components to give a complex that has the same substrate specificity as that determined for the isolated E1 enzyme; namely, it is a branched-chain 2-oxoacid dehydrogenase complex that

is also active with pyruvate An E2 core that comprises

an assembly of 24 polypeptide chains is consistent with other branched-chain 2-oxoacid multi-enzyme com-plexes from bacteria and eukarya [24,25], some of which also have activity with pyruvate Additionally, the E1 subunit in those branched-chain complexes is also an a2b2 oligomer [24,25] What is particularly interesting is that the assembly of the E2 core in the Thermoplasma enzyme is temperature dependent, incu-bation to at least 40C (the temperature of the ultra-centrifugation) being required

The data in Fig 2 show that overall complex activ-ity increased linearly with the ratio of E1 : E2 mixed together, as was found with the E coli PDHC for example [26], until maximal activity was achieved at a mixing ratio of 2 : 1 However, both ultracentrifuga-tion and DLS estimate the Mr of the assembled com-plex to be around 5· 106, closely fitting the tentative conclusion of an E1(a2b2)⁄ E2 ⁄ E3(a2) stoichiometry of

1 : 1 : 0.1 These experiments indicate that not all the E1 molecules may be tightly bound to the E2 core and⁄ or that assembly might be substrate enhanced Whilst uncertainties remain over the exact subunit composition of the assembled complex, the important conclusion from our data is that the four OADHC ORFs in the archaeon T acidophilum encode the com-ponents of a functional 2-oxoacid dehydrogenase multi-enzyme complex, the first to be identified in this domain of life Thus, OADHCs were probably present

in the common ancestor to the Bacteria and Archaea, and have been retained in aerobic members of each domain The Thermoplasma enzyme possesses catalytic activity with branched-chain 2-oxo acids and pyruvate, but it remains to be established whether other archaeal OADHCs have the same or different substrate specific-ities However, whatever specificity is found, the physi-ological role of these OADHCs in the archaea remains

a mystery given the presence of active 2-oxoacid FORs that catalyze the equivalent chemical reactions

In studies of the OADHC from the halophilic archa-eon H volcanii, we could find no growth substrate that would induce the expression of OADHC activity [20], nor was any physiological defect apparent in this organism when the E3 gene was inactivated by inser-tional mutagenesis [27] Interestingly, Wanner & Soppa

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[28] have found an additional gene cluster in H

volca-nii comprising three genes that would appear to code

for OADHC E1a and E1b subunits, and an

unat-tached lipoyl domain; however, no genes for a

com-plete E2 or an E3 were present Evidence for a

function during nitrate-respirative growth on

Casami-no acids was presented, although the metabolic

sub-strate could not be identified

In conclusion, with respect to the archaeal four-gene

OADHC cluster that we have studied in this paper, it

is highly unlikely that the genes would have been

retained in a highly sophisticated and functional state

without a physiological role We suggest that

proteo-mic studies on this thermoacidophile need to be

insti-tuted to reveal this role

Experimental procedures

Materials

Bacteriological media were purchased from Sigma-Aldrich

(Poole, UK) or Fisher Scientific (Loughborough, UK)

Expression vector pET28a, E coli expression strain

BL21(DE3), BugBuster Protein Extraction Reagent and

Benzonase nuclease were purchased from Novagen-Merck

(Nottingham, UK) E coli JM109 cells, pGEM-T vector,

restriction endonucleases, T4 DNA ligase and Taq

polymer-ase were purchpolymer-ased from Promega (Southampton, UK)

Vent DNA polymerase was from New England Biolabs

(Hitchin, UK) Lipoic acid, phenylmethanesulfonyl fluoride

and antibiotics were purchased from Sigma-Aldrich

SDS⁄ PAGE molecular mass markers were from Bio-Rad

(Hemel Hempstead, UK)

Plasmids pET19b-E1a and pET28a-E1b, which,

respec-tively, coexpress the a and b subunits of the T acidophilum

E1, have been described previously [14]

Bioinformatics

The putative OADHC operon was identified in the T

aci-dophilumDSM1728 genome from the ENTREZ Nucleotide

database (http://www.3.ncbi.nlm.nih.gov) E1a: Ta1438;

E1b: Ta1437; E2: Ta1436; and E3: Ta1435

Recombinant DNA techniques

E2 and E3 gene amplification

Preparation of genomic DNA from T acidophilum strain

DSM 1728 has been described previously [29] The E2 and

E3 genes were PCR-amplified from this genomic

DNA using primers that engineered restriction sites into the

5¢- and 3¢ ends of the gene products: NdeI and XhoI for the

E2 gene, and NheI and EcoRI for E3 Oligonucleotides

were as follows (restriction sequences are underlined):

E2 forward: CGCCATATGTACGAATTCAAACTGC CAGACATAGG

E2 reverse: CCGCTCGAGTCAGATCTCGTAGAT TATAGCGTTCGG

E3 forward: CTACGAGAGCTAGCATGTACGATGC AATAATAATAGGTTC

E3 reverse: TTTAAAAATGGAATTCAATGAGAT GGT

PCR amplification was carried out using Vent polymer-ase, and A-tails were added to the products with Taq poly-merase Both genes were then separately cloned into the intermediate vector pGEM-T using T4 DNA ligase, and the clones were amplified in E coli strain JM109 grown in Luria–Bertani LB media [1% (w⁄ v) tryptone, 1% (w ⁄ v) NaCl, 0.5% (w⁄ v) yeast extract] supplemented with carben-icillin (50 lgÆmL)1) Plasmids were extracted using the BD Biosciences (Palo Alto, CA) NucleoSpin Plasmid kit, and the genes were sequenced for fidelity The E2 and E3 genes were then excised from pGEM-T, using the appropriate restriction endonucleases, purified by electrophoresis in a 0.8% (w⁄ v) agarose gel, and extracted from the gel using the Qiagen (Hilden, Germany) Qiaex II Gel Extraction kit

Construction of expression vectors pET28a-E2 and pET28a-E3

Expression vector pET28a was prepared for recombinant ligation by NdeI⁄ XhoI restriction endonuclease digestion for E2, and NheI⁄ EcoRI digestion for E3, and purified by gel electrophoresis and gel extraction as already described E2 and E3 genes were separately ligated into the vectors using T4 DNA ligase, generating the recombinant expression vec-tors pET28a-E2 and pET28a-E3 This pET28a vector thus introduced a 20- and a 23-amino acid sequence at the N-ter-mini of the E2 and E3 recombinant protein products, respec-tively, with each containing a 6-histidine tag sequence Expression and purification of OADHC components

E2 expression and purification Two different methods of expression were used Several col-onies of E coli strain BL21(DE3), freshly transformed with plasmid pET28a-E2, were picked from LB agar plates and used to inoculate 2 L of LB medium supplemented with kanamycin (30 lgÆmL)1) and 0.2 mm dl-lipoic acid Incu-bation was at 30C for 20 h in darkness, with no induction

by IPTG, after which cells were harvested by centrifugation

at 6000 g Alternatively, an overnight culture (20 mL,

A6000.6) of freshly transformed E coli BL21(DE3)pLysS cells was used to inoculate 1 L of LB medium supple-mented with kanamycin (30 lgÆmL)1) After induction with IPTG (at A6000.6) and subsequent overnight incubation at

37C, cells were harvested as described before The former

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method allows production of recombinant E2 of which up

to 50% is lipoylated, whereas in the latter method only 5%

of the E2 is lipoylated

Purification of the recombinant E2 was carried out at

25C, unless otherwise stated Samples were analyzed by

SDS⁄ PAGE on a 10% (w ⁄ v) polyacrylamide gel at each

step of the purification, and protein concentrations were

determined from A280 values Frozen cells were disrupted

by resuspension in BugBuster (5 mLÆg)1 wet cells)

supple-mented with Benzonase nuclease (1 lLÆmL)1), incubated on

ice with gentle agitation for 30 min, and centrifuged at

16 000 g for 20 min at 4C to pellet cell debris The

solu-ble cell extract was subjected to His Bind Resin

chroma-tography, and fractions containing E2 protein were pooled

and dialyzed overnight into 20 mm Tris⁄ HCl buffer,

pH 9.0, 10% (v⁄ v) glycerol The protein was then subjected

to anion exchange chromatography on an Amersham

Bio-sciences (Chalfont St Giles, UK) A¨kta FPLC system, using

a 5 mL Q-Sepharose Hi-Trap column equilibrated with

50 mm Tris⁄ HCl buffer, pH 8.5 Protein was eluted over a

0–0.8 m gradient of NaCl in the same buffer, at a flow rate

of 1 mLÆmin)1 over 60 min Fractions containing E2 were

stored at 4C in the elution buffer supplemented with

1 mm phenylmethanesulfonyl fluoride

E3 expression and purification

For expression of the E3 enzyme, a 20 mL overnight

cul-ture of transformed BL21(DE3) (A6000.6) was used to

inoculate 1 L of LB medium supplemented with kanamycin

(30 lgÆmL)1) Cells were incubated at 37C until 5 h after

the A600had reached 0.6 (with no induction by IPTG), and

were then collected by centrifugation Cell disruption was

carried out as described for the purification of recombinant

E2 The soluble cell extract was subjected to heat

precipita-tion at 65C for 5 min, and precipitated material removed

by centrifugation at 16 000 g for 20 min at 4C E3 in the

remaining soluble fraction was purified by His-Bind Resin

chromatography, dialyzed overnight into 20 mm Tris⁄ HCl

buffer, pH 8.4, and then stored at 4C

Assembly of the OADHC multi-enzyme complex

OADHC was assembled in vitro by mixing together

recom-binant E1a, E1b, E2 and E3 proteins at 55C for 0–1 h

Molar ratios to enzyme E2 varied from 0.5 to 6.0 (E1a2b2)

and 0.01–1.0 (E3a2) Each assembled complex was assayed

for overall complex activity as described below

SDS-PAGE

Analysis of protein purity and determination of polypeptide

Mr values were carried out by SDS⁄ PAGE in a resolving

gel containing 10% (w⁄ v) acrylamide [30]

Enzyme assays E1 enzymic activity was assayed spectrophotometrically by following the 2-oxoacid-dependent reduction of 2,6-dichlo-rophenolindophenol (DCPIP) at 595 nm [31] Assays were carried out at 55C in 20 mm potassium phosphate (pH 7.0), 2 mm MgCl2and 0.2 mm TPP Buffer and recom-binant E1a2b2 enzyme were pre-incubated at 55C for

10 min; 50 lm DCPIP was then added and the assay started by the addition of the 2-oxoacid substrate (pyru-vate, 2-oxoglutarate, 4-methyl-2-oxopentanoate, 3-methyl-2-oxopentanoate or 3-methyl-2-oxobutanoate)

E3 was assayed at 55C in 50 mm EPPS buffer (pH 8.0) containing 0.4 mm dihydrolipoamide and 1 mm NAD+ The reaction, in a final volume of 1 mL, was started by the addition of enzyme, and activity was monitored by measur-ing the production of NADH at 340 nm

Overall complex activity was assayed at 55C in 50 mm potassium phosphate buffer (pH 7.0) containing 2.5 mm NAD+, 1 mm MgCl2, 0.2 mm TPP, 0.13 mm CoASH and 2.6 mm cysteine-HCl [32] Buffer and assembled enzyme complex were pre-incubated at 55C for 10 min to allow binding of TPP to E1 The assay, in a final volume of

1 mL, was started by the addition of the 2-oxoacid substrate

as for the assay of E1, and OADHC activity was monitored

by measuring the production of NADH at 340 nm

Kinetic parameters were determined by the direct linear method of Eisenthal & Cornish-Bowden [33]

Gel filtration Analytical gel filtration was carried out at 25C on the Amersham Biosciences A¨kta FPLC system, using a Superdex 200 10⁄ 300 GL column Protein standards were: b-amylase (Mr¼ 200 000), alcohol dehydrogenase (150 000), BSA (66 000), carbonic anhydrase (29 000) and cytochrome c (12 400) For analysis of E3, the column was equilibrated with 20 mm sodium phosphate (pH 7.0), 0.1 m NaCl and 10% (v⁄ v) glycerol; peak fractions were assayed for E3 enzymic activity Analysis of assembled complex was carried out in 20 mm sodium phosphate (pH 7.0), 2 mm MgCl2, 0.1 m NaCl and 10% (v⁄ v) glycerol Peak fractions were assayed for E1, E3 and OADHC activity

Analytical ultracentrifugation All analytical ultracentrifugation experiments were carried out on a Beckman XL-A analytical ultracentrifuge (Beck-man-Coulter, CA) Sedimentation velocity experiments were carried out at 15 000 r.p.m., and cells were scanned every

5 min at 280 nm For sedimentation of E2, the buffer was

20 mm Tris⁄ HCl (pH 8.5), 0.4 m NaCl and 1 mm phen-ylmethanesulfonyl fluoride; for whole complex, the buffer was the same as that used in the analytical gel filtration

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analysis, 20 mm sodium phosphate (pH 7.0), 2 mm MgCl2,

100 mm NaCl and 10% (v⁄ v) glycerol The set temperature

on the centrifuge was 40C, and the solution densities were

directly measured at this temperature using an Anton-Paar

DMA 5000 high-precision density-meter Sedimentation

velocity distributions were obtained by the c(s) method [34]

using the program sedfit Data were then directly fitted

using the finite element solution of the Lamm equation in

sedfit [18] to give values of the sedimentation coefficient

and of Mr

Dynamic light scattering

All DLS measurements were performed using a Zetasizer

Nano S from Malvern Instruments Ltd (Malvern, UK)

Prior to DLS measurements, protein solutions

(1 mgÆmL)1) in 20 mm sodium phosphate buffer, pH 7.5,

10% glycerol (v⁄ v) and 0.1 m NaCl were filtered through

a 0.02 lm membrane filter (Whatman Anotop 10, Fisher

Scientific, Loughborough, UK) to remove dust particles

However, it was found necessary to filter enzyme E3

through a 0.22 lm membrane filter (Millipore, Watford,

UK) DLS measurements were carried out at 25C or

55C Mr values were derived from the measured

hydro-dynamic radii using the Protein Utilities feature of the

dispersion technology software, version 4.10, supplied

with the instrument

Mass spectrometry

Determination of the E2 polypeptide mass

A 100 pmol sample of recombinant E2 was injected on to

a MassPrep on-line desalting cartridge (2.1· 10 mm)

(Waters, Milford, MA), eluted with an increasing

acetoni-trile concentration [2 vol acetoniacetoni-trile + 98 vol aqueous

for-mic acid (1%, v⁄ v) to 98 vol acetonitrile + 2 vol aqueous

formic acid (1%, v⁄ v)] and delivered to an electrospray

ion-ization mass spectrometer (LCT, Micromass, Manchester,

UK) that had previously been calibrated using myoglobin

An envelope of multiply charged signals was obtained and

deconvoluted using maxent1 software to give the molecular

mass of the protein

Mapping the lipoylation of E2

Recombinant E2 (50 pmol) was dialyzed against 50 mm

ammonium bicarbonate on a VS membrane disc (Millipore)

for 30 min Sequencing grade, modified porcine trypsin

(Promega) (60 ng) was added and the sample incubated at

37C for 16 h A portion of the sample was diluted in 5%

(v⁄ v) formic acid and the peptides separated using an

Ulti-Mate nanoLC (LC Packings, Amsterdam, the Netherlands)

equipped with a PepMap C18 trap and column The eluant

was sprayed into a Q-Star Pulsar XL tandem mass

spec-trometer (Applied Biosystems, Foster City, CA) and ana-lyzed in Information Dependent Acquisition mode The

MS⁄ MS data generated were analyzed using the Mascot search engine (Matrix Science, London, UK), with lipoyla-tion selected as a possible lysine modificalipoyla-tion The MS⁄ MS spectrum corresponding to the modified peptide was also interpreted ‘manually’ using BioAnalyst (Applied Biosys-tems) tools

Acknowledgements

MJD and DWH thank the US Air Force Office of Sci-entific Research (Arlington, VA, USA) for generous financial support CH and MGP gratefully acknowl-edge the receipt of Postgraduate Studentships from the

UK Biotechnology and Biological Sciences Research Council and from the University of Bath, respectively

We thank Dr Jean van den Elsen (University of Bath, UK) for allowing us to use the DLS Zetasizer Nano S, and Dr Catherine Botting, BMS Mass Spectrometry and Proteomics Facility, University of St Andrews,

UK, for carrying out the MS analyses

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