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Fax: + 41 1 733 4659, Tel.: + 41 1 733 4642, E-mail: jennings@cytos.com Abbreviations: GNA, genome-derived Neisseria antigen; LPSS, lipo-polypeptide signal sequence; MipA, MltA-interact

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GNA33 from Neisseria meningitidis serogroup B encodes

a membrane-bound lytic transglycosylase (MltA)

Gary T Jennings1*, Silvana Savino1*, Elisa Marchetti1, Beatrice Arico`1, Thomas Kast2, Lucia Baldi1, Astrid Ursinus2, Joachim-Volker Ho¨ltje2, Robert A Nicholas3, Rino Rappuoli1and Guido Grandi1

1

I.R.I.S., Chiron S.p.A., Siena, Italy;2Max Planck Institute fur Entwicklungsbiologie, Abteilung Biochemie, Tubingen, Germany;

3

Department of Pharmacology, University of North Carolina at Chapel Hill, NC, USA

In a previous study, we used the genome of serogroup B

Meningococcusto identify novel vaccine candidates One of

these molecules, GNA33, is well conserved among

Men-ingococcusB strains, other Meningococcus serogroups and

Gonococcusand induces bactericidal antibodies as a result of

being a mimetic antigen of the PorA epitope P1.2 GNA33

encodes a 48-kDa lipoprotein that is 34.5% identical with

membrane-bound lytic transglycosylase A (MltA) from

Escherichia coli In this study, we expressed GNA33, i.e

MeningococcusMltA, as a lipoprotein in E coli The

lipo-protein nature of recombinant MltA was demonstrated by

incorporation of [3H]palmitate MltA lipoprotein was

purified to homogeneity from E coli membranes by

cation-exchange chromatography Muramidase activity was

con-firmed when MltA was shown to degrade insoluble murein sacculi and unsubstituted glycan strands HPLC analysis demonstrated the formation of 1,6-anhydrodisaccharide tripeptide and tetrapeptide reaction products, confirming that the protein is a lytic transglycosylase Optimal muramidase activity was observed at pH 5.5 and 37C and enhanced by Mg2+, Mn2+and Ca2+ The addition of Ni2+ and EDTA had no significant effect on activity, whereas

Zn2+ inhibited activity Triton X-100 stimulated activity 5.1-fold Affinity chromatography indicated that MltA interacts with penicillin-binding protein 2 from Meningo-coccusB, and, like MltA from E coli, may form part of a multienzyme complex

Neisseria meningitidis is a Gram-negative, capsulated

b-proteobacterium capable of causing severe meningitis

and septicemia with a fatality rate of  10% [2] The

complete 2 272 351-bp genomic sequence of Meningococcus

serogroup B (strain MC58) has been determined and used

by us to identify novel vaccine candidates against this

pathogenic organism [1,2] We amplified, cloned and

expressed in Escherichia coli selected ORFs encoding

teins with predicted surface exposure Recombinant

pro-teins were purified, immunized in mice, and the resultant

sera analysed by FACS, ELISA, and bactericidal assay

GNA33 was positive in all three analyses and highly

conserved (99.2± 0.7%) among 22 strains of

Meningococ-cusB, nine strains from Meningococcus serogroups A, C, Y,

X, Z, W135, and 95.8% conserved in Neisseria gonorrhoeae

[1] Further study revealed that GNA33 elicits protective

antibodies to meningococci by mimicking a surface-exposed

epitope on loop 4 of porin A in strains with serosubtype

P1.2 [3]

The ORF of GNA33 encodes a protein 441 amino acids

in length with an N-terminal 20-amino-acid lipopolypep-tide signal sequence (LPSS) with a consensus lipoprotein-processing site, LAAC [4] Sequence comparison showed that GNA33 is 34.5% identical and 41.3% homologous with the 38-kDa membrane-bound lytic transglycosylase A (MltA) from E coli (Fig 1) In E coli, four additional exo-specific lytic transglycoylases (MltB, MltC, MltD, and Slt70) have been identified and/or characterized [5–8] These lytic transglycosylases exhibit no significant sequence homology with each other With the exception

of Slt70 (soluble lytic transglycosylase), they are all lipoproteins that attach to the outer membrane [7–10] Homologues of all these lytic transglycosylases have been identified in Meningococcus B [2], which, like their E coli counterparts, also exhibit little sequence conservation with each other

Lytic transglycosylases are a unique class of lysozyme-like enzymes that catalyze cleavage of the b-1,4-glycosidic bond between N-acetylmuramic acid (MurNAc) and N-acetyl glucosamine (GlcNAc) However, unlike lysozyme where the glycosyl moiety is transferred to H2O, cleavage by lytic transglycosylases is followed by an intramolecular transgly-cosylation [10] In this reaction, the glycosidic linkage between the muramyl and glucosaminyl residues is trans-ferred to the C6 position of the muramyl residue to form terminal 1,6-anhydromuramic acid-containing products [10] By virtue of their ability to cleave the polysaccharide backbone of the peptidoglycan layer, lytic transglycosylases are thought to play a role in synthesis and degradation of the murein sacculus It has been proposed that lytic transglycosylases play important roles in cellular elongation,

Correspondence to G T Jennings, Cytos Biotechnology AG,

Wagistrasse 25, CH-8952 Zu¨rich-Schlieren, Switzerland.

Fax: + 41 1 733 4659, Tel.: + 41 1 733 4642,

E-mail: jennings@cytos.com

Abbreviations: GNA, genome-derived Neisseria antigen; LPSS,

lipo-polypeptide signal sequence; MipA, MltA-interacting protein; MltA,

membrane-bound lytic transglycosylase A; PBP, penicillin-binding

protein.

*Note: these authors contributed equally to this work.

(Received 29 March 2002, revised 14 June 2002,

accepted 20 June 2002)

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septation, recycling of muropeptides, and pore formation

[7,10,11]

Current models of cell wall synthesis in Gram-negative

bacteria predict the necessity for murein synthases and

lytic enzymes to interact in a co-ordinated and controlled

manner [10] Indeed, interactions between lytic

cosylases (MltA, MltB and Slt70), bifunctional

transgly-cosylase-transpeptidases (PBP1A, PBP1B, PBP1C),

transpeptidases (PBP2, PBP3), and endopeptidases

(PBP4 and PBP7) of E coli have been reported [12,13]

In particular, affinity chromatography and/or surface

plasmon resonance have shown interactions between

MltA, PBP1B, PBP1C, PBP2, PBP3 and a newly

identi-fied scaffolding protein, MipA [14] It is thought that,

through such interactions, the enzymes required for cell

wall metabolism associate and form a multienzyme

complex [10,14] An enzyme complex would not only

provide a means for regulating peptidoglycan synthesis but

would also provide a way to control the potentially

autolytic activity of proteins such as MltA To date, no

evidence of these associations in Neisseria species has been

reported

In this study we cloned GNA33 (MltA) from

Meningo-coccus serogroup B The recombinant lipoprotein was

expressed in E coli, purified, and assayed for its

muram-idase and lytic transglycosylase activity In addition, we used

affinity chromatography to investigate the hypothesis that

MltA associates with other enzymes involved in

peptido-glycan metabolism and thus may be part of a multienzyme

complex

E X P E R I M E N T A L P R O C E D U R E S

Vector construction Three versions of meningococcal mltA were amplified by PCR and cloned into the expression vector pET21b+ (Novagen) via 5¢ NdeI and 3¢ XhoI restriction sites These included a full-length form incorporating its endogenous 20-amino-acid LPSS, a form containing a 19-amino-acid LPSS from an unrelated Meningococcus B lipoprotein, GNA1946 [1], and a truncated form lacking any leader sequence (Fig 1)

Full-length mltA was amplified using a forward primer containing an NdeI restriction site (5¢-CGCGGATCCCA TATGAAAAAATACCTATTCCGC-3¢) incorporating the ATG start codon The reverse primer (5¢-CCCGCTC GAGTTACGGGCGGTATTCGG-3¢) contained a XhoI restriction site and was used for all three constructs The construct containing the GNA1946 LPSS was made using a forward primer (5¢-GGGAATTCCATATGAAAACCTT CTTCAAAACCCTTTCCGCCGCCGCGCTAGCGCT CATCCTCGCCGCCTGCCAAAGCAAGAGCATC-3¢) spanning the entire leader of GNA1946 and containing 18 nucleotides overlapping the mltA sequence A conservative double nucleotide substitution (underlined) was made in a region of the primer encoding the GNA1946 LPSS This substitution introduced an NheI restriction and was designed to allow the GNA1946 LPSS to be ligated into any of the meningococcus genes that we have previously expressed in pET-21b[1] This restriction site was not used

Fig 1 Amino acid sequence of MltA from

N meningitidis serogroup B: comparison with

MltA from E coli The amino-acid sequence

of MltA from Meningococcus B (strain 2996)

(NmMltA) was compared with MltA from

E coli (EcMltA) using the GAP program

included in the Genetics Computer Group

(GCG) Wisconsin Package version 10.0 The

20-amino-acid LPSS is underlined The LPSS

was identified using the program PSORT

avail-able at http://psort.nibb.ac.jb The

19-amino-acid LPSS from the Meningococcus B gene

GNA1946 (GNA1946L), was used to replace

the MltA leader peptide and is shown above

the meningococcal sequence Amino acids are

identified by the standard single letter code.

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in this study The truncated gene lacking the 20-amino-acid

leader peptide was amplifed using the forward primer,

5¢-CGCGGATCCCATATGCAAAGCAAGAGCATCC

AAA-3¢

PCR was performed in a reaction volume of 100 lL

comprising 10 mM Tris/HCl (pH 8.3), 50 mM NaCl,

1.5 mMMgCl2, 0.8 mMdNTPs, 40 lMeach oligonucleotide

primer, and 2.5 U TaqI DNA polymerase (PerkinElmer,

Boston, MA, USA) Template DNA for the reaction was

200 ng genomic DNA from Neisseria meningitidis B 2996

The primary denaturation step was performed at 94C for

3 min and the remainder of the first five cycles with

denaturation, annealing and polymerization conditions of

94C for 40 s, 52 C for 40 s and 72 C for 1 min,

respectively The annealing temperature was increased to

65C for the next 30 cycles, and a final 7 min extension at

72C completed the reaction PCR products were purified

using the Qiagen Gel Extraction Kit Ligations and

transformations into E coli DH5 were performed as

described by Sambrook et al [15] After selection,

amplifi-cation and purifiamplifi-cation, the plasmids were used to transform

E coli BL21(DE3) (Novagen, Madison, WI, USA) The

genomic sequence of Meningococcus B is known for the

strain MC58 [2] The nucleotide sequence of mltA from

strain 2996 has 17 nucleotide substitutions (of which 16 are

silent) with respect to mltA from strain MC58 Only one of

these base changes results in an amino-acid substitution,

Ser312 to Ala

Expression and purification of recombinant MltA

E coli BL21(DE3) cells harboring the three versions of

pET21b-MltA (see above) were grown at 30C in Luria–

Bertani medium containing 100 lgÆmL)1 ampicillin until

the D550 reached 0.6–0.8 Isopropyl thio-b-D-galactoside

was added to a final concentration of 1.0 mM, and the

culture shaken for an additional 3 h Cells were collected by

centrifugation at 8000 g for 15 min at 4C All subsequent

procedures were performed at 4C

For purification of lipidated MltA, cells were

resuspend-ed in 25 mL 50 mM phosphate/300 mM NaCl, pH 8.0,

containing complete protease inhibitor (Roche, Basel,

Switzerland) Bacteria were disrupted by osmotic shock

with two or three passages through a French Press (SLM

Aminco) Unbroken cells were removed by centrifugation

at 5000 g for 15 min, and membranes sedimented by

centrifugation at 100 000 g for 45 min The pellet was

resuspended in 20 mM Tris/HCl (pH 8.0)/1.0M NaCl

containing complete protease inhibitor, and the suspension

mixed for 2 h After centrifugation at 100 000 g for

45 min, the pellet was resuspended in 20 mM Tris/HCl

(pH 8.0) containing 1.0MNaCl, 5.0 mgÆmL)1Chaps, 10%

(v/v) glycerol and complete protease inhibitor The solution

was stirred overnight, centrifuged at 100 000 g for 45 min,

and the supernatant dialysed for 6 h against 20 mMBicine

(pH 8.5)/120 mM NaCl/5.0 mgÆmL)1 Chaps/10% (v/v)

glycerol The dialysate was cleared by centrifugation at

13 000 g for 20 min and applied to a Mono S FPLC

ion-exchange column (Pharmacia, Uppsala, Sweden) at a flow

rate of 0.5 mLÆmin)1 Elution was performed using a

stepwise NaCl gradient

The protein was also expressed and purified in a form

lacking the LPSS After expression and harvesting, cells

were resuspended in 20 mMBicine (pH 8.5)/20 mMNaCl/ 10% (v/v) glycerol containing complete protease inhibitor and disrupted with a Branson Sonifier 450 The sonicate was centrifuged at 8000 g for 30 min to remove unbroken cells, and MltA was precipitated from the supernatant by the addition of saturated (NH4)2SO4 solution MltA was precipitated between 35% and 70% saturation and was collected by centrifugation at 8000 g for 30 min The pellet was dissolved in 20 mMBicine (pH 8.5)/20 mMNaCl/10% (v/v) glycerol and dialysed against this buffer overnight The dialysate was centrifuged at 13 000 g for 20 min, and the supernatant was applied to an FPLC Mono S ion-exchange column at a flow rate of 0.5 mLÆmin)1 The protein was eluted from the column with a stepwise NaCl gradient Purifications were analysed by SDS/PAGE [16], and protein concentration determined by the Bradford method West-ern-blot analysis was performed using polyclonal antisera as described previously [1]

Palmitate labelling Palmitate incorporation by recombinant MltA was con-firmed as described by Kraft et al [17] Briefly, E coli BL21(DE3) harbouring one of the three pET21b-MltA constructs were grown at 30C in Luria–Bertani medium containing 100 lgÆmL)1 ampicillin and 5 lCiÆmL)1 [3H]palmitate (Amersham) until the D550nm reached 0.4–0.8 Expression of recombinant protein was induced for 1 h by the addition of isopropyl b-D-thiogalactoside (final concentration 1 mM), and the bacteria harvested by centrifugation at 3000 g for 15 min Cells were washed twice with cold NaCl/Pi, suspended in 20 mMTris/HCl (pH 8.0)/

1 mMEDTA/1.0% (w/v) SDS, lysed by boiling for 10 min, and centrifuged for 10 min at 13 000 g Cold acetone was added to the supernatant, and, after 1 h at)20 C, protein was collected at 13 000 g for 10 min Protein was resus-pended in 1.0% (w/v) SDS, boiled with SDS/PAGE sample buffer, and subjected to SDS/PAGE using a 12.5% separating gel Gels were fixed for 1 h in 10% (v/v) acetic acid, and soaked for 30 min in Amplify solution (Amer-sham) The gel was vacuum-dried under heat and exposed

to Hyperfilm (Kodak) overnight at)80 C

Assay for muramidase activity Purified, recombinant MltAs expressed with the GNA1946 LPSS or without an LPSS were assessed for their ability to degrade insoluble murein sacculi into soluble muropeptides

by the method of Ursinus & Holtje [18] Murein lysis activity was determined using peptidoglycan radiolabelled with meso-2,6-diamino-3,4,5-[3H]pimelic acid as substrate Enzyme (3–10 lg total) was incubated for 45 min at 37C

in a total volume of 100 lL comprising 10 mMTris/maleate (pH 5.5), 10 mM MgCl2, 0.2% (v/v) Triton X-100 and [3H]diaminopimelic acid-labelled murein sacculi ( 10 000 c.p.m.) The assay mixture was placed on ice for 15 min with 100 lL 1.0% (w/v) N-cetyl-N,N,N-trime-thylammonium bromide, and the precipitated material separated by centrifugation at 10 000 g The radioactivity

in the supernatant was measured by liquid-scintillation counting The E coli lytic transglycosylase Slt70 was used as

a positive control for the assay, and the negative control comprised the above assay solution without enzyme

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Assay for lysis of poly(MurNAc-GlcNAc) glycan strands

The ability of MltA to utilize purified glycan strands as

substrate was determined by the method described by

Ursinus & Holtje [18] Poly(MurNAc-GlcNAc)n>30,

labelled with N-acetyl-D-1-[3H]glucosamine, was incubated

with 3 lg MltA in 10 mM Tris/maleate (pH 5.5)/10 mM

MgCl2/0.2% (v/v) Triton X-100 for 30 min at 37C The

reaction was stopped by boiling for 5 min, and the pH of

the sample adjusted to 3.5 by addition of 10 lL 20% (v/v)

phosphoric acid The components of the assay were then

separated by RP-HPLC on a Nucleosil 300 C18column as

described by Harz et al [19] The E coli lytic

transglycos-ylase MltA was used as a positive control in the assay A

negative control was performed in the absence of enzyme

Analysis of reaction products

The nature of the reaction products resulting from the

digestion of unlabelled E coli murein sacculus were

deter-mined by RP-HPLC as described by Glauner [20] Murein

sacculi digested with the muramidase Cellosyl were used to

calibrate and standardize the Hypersil ODS column

Gel filtration

The molecular masses of the recombinant proteins were

estimated using either FPLC Superose 12 (H/R 10/30) or

Superdex 75 gel-filtration columns (Pharmacia) The

buf-fers were 20 mM Bicine (pH 8.5) with and without

5.0 mgÆmL)1Chaps, respectively In addition, each buffer

contained 150–200 mM NaCl and 10% (v/v) glycerol

Proteins were dialysed against the appropriate buffer and

applied in a volume of 200 lL Gel filtration was performed

with a flow rate of 0.5–2.0 mLÆmin)1 and the eluate

monitored at 280 nm Fractions were collected and

analysed by SDS/PAGE Blue Dextran 2000 and the

molecular-mass standards ribonuclease A,

chymotryp-sin A, ovalbumin A, and BSA (Pharmacia) were used to

calibrate the columns The molecular mass of the sample

was estimated from a calibration curve of Kav vs log

(molecular mass) of the standards

Preparation of membrane extracts for affinity

chromatography

A detergent-solubilized membrane extract was prepared

from an acapsulated N meningitidis strain, M7 An

over-night culture of strain M7 was inoculated into 2 L

Muller-Hinton broth containing 0.25% (w/v) glucose, and grown at

37C in an atmosphere of 5.0% CO2 When the D550

reached 0.6, the culture was cooled on ice and harvested by

centrifugation at 8000 g; all the following steps were

performed at 4C The pellet was resuspended in 10 mM

Tris/HCl (pH 8.0) containing complete protease inhibitor

and DNase (10 lgÆmL)1), and the cells were disrupted with

a French Press Membranes were spun down at 100 000 g

for 45 min and resuspended in 10 mM Tris/maleate

(pH 6.8) containing 2.0% (v/v) Triton X-100, 10 mM

MgCl2, 150 mMNaCl and EDTA-free complete protease

(buffer I) After stirring overnight, membrane debris was

removed by centrifugation (100 000 g for 45 min), and the

supernatant containing solubilized protein stored at)20 C

Affinity chromatography Purified leaderless MltA (10 mgÆmL)1gel) was coupled to CNBr-activated Sepharose 4B (Pharmacia) according to the manufacturer’s protocol CNBr-activated Sepharose 4B prepared without protein and where the functional groups were neutralized with Tris was used as a control for nonspecific binding to the resin Disposable columns containing either control or MltA-coupled resin were prepared and equilibrated with 20 col vol buffer I Solu-bilized membrane extract was applied to both columns at a flow rate of 0.25 mLÆmin)1, then washed with 5· 1.0 mL buffer I Retained proteins were eluted by increasing the NaCl concentration in a stepwise fashion Salt concentra-tions of 300 mM, 600 mMand 1.0Min buffer I were applied

in 5· 1.0 mL aliquots, and the eluates retained for analysis

by SDS/PAGE, penicillin-binding assay, and Western blot Penicillin-binding assay

Penicillin-binding proteins (PBPs) were identified using the

125I-labelled Bolton–Hunter derivative of ampicillin pre-pared as described previously [21] Briefly, 4 lL (2.4 lg total) of the labelled ampicillin derivative was incubated for

30 min at 37C with 40 lL of the fractions eluted from control and MltA-coupled affinity columns The reaction was stopped by the addition of 4 lL penicillin G (60 mgÆmL)1), and the reaction complexes separated by SDS/PAGE and visualized by autoradiography

Preparation of antisera to PBP2 Recombinant PBP2 from N gonorrhoeae was purified as a soluble, active form PBP2 was expressed in the cytoplasm

of E coli as a fusion protein to maltose-binding protein (MBP) with a His6tag at its N-terminus Codons 44–581, which encode the entire periplasmic domain of PBP2, were fused in-frame to the C-terminus of MBP via an interven-ing tobacco etch virus (TEV) protease site The fusion protein was overexpressed in E coli, purified on a Ni2+/ nitrilotriacetate column, and cleaved with His6–TEV protease (fusion protein/TEV protease, 20 : 1, w/w) in

50 mM Tris/HCl (pH 8.0)/500 mM NaCl/10% glycerol After digestion, PBP2 was again purified by metal chelate affinity chromatography to remove uncut fusion protein, His6–MBP and the protease PBP2 was not eluted in the flow through, which contained unrelated contaminant proteins, but was eluted from the column with 10 mM imidazole Purified PBP2 was judged to be at least 95% pure by SDS/PAGE The protein was concentrated to

6 mgÆmL)1and stored at)80 C Purified PBP2 was used

to immunize mice, and antisera were collected as described

b y Pizza et al [1]

Western blot Fractions eluted from the MltA-coupled affinity column were separated by discontinuous SDSPAGE using a 12.5% separating gel [15] Proteins were electroblotted onto a nitrocellulose membrane and probed with antisera to PBP2 diluted 1 : 1000 Immunoreactive proteins were detected using the enhanced chemiluminescent method (Amersham, Chicago, IL, USA) and fluorography

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R E S U L T S

Cloning and expression inE coli

Expression of MltA in E coli was observed when the

gene was cloned with either its own 20-amino-acid LPSS

or the 19-amino-acid LPSS from an unrelated

Meningo-coccus lipoprotein, GNA1946 However, the level of

expression was much lower when the native leader

peptide was used (result not shown) Hence, for purposes

of purification and characterization, we used the clone

incorporating the LPSS from GNA1946 MltA cloned

without a leader peptide was expressed very efficiently

and represented about 20% of total cellular protein as

judged by densitometry This truncated, soluble form of

the protein was used for affinity chromatography (see

below)

MltA incorporating the LPSS from GNA1946 was

routinely expressed at 30C because expression of the

recombinant protein at 37C resulted in lysis of host

cells Lysis at 37C was observed within 60 min of

induction of expression and could be prevented by the

addition of 12% (w/v) sucrose and 10 mM MgSO4

Overexpression of E coli MltA also results in formation

of spheroplasts and cell lysis [9] However, in contrast

with our results, lysis due to overexpression of E coli

MltA occurs at 30C, but not at 37 C With E coli

MltA, this effect is due to the temperature sensitivity of

its muramidase activity, which exhibits maximum activity

at 30C and a 93% reduction in activity at 37 C It also

has been reported that a 55-fold overexpression of E.coli

lytic transglycosylase MltB resulted in rapid cell lysis at

37C [8] Similar to our observation with Meningococcus

MltA, autolysis induced by overexpression of E coli

MltB was also prevented by osmotic protection during

growth

Purification of recombinant proteins

Recombinant MltA lipoprotein was purified from the

membrane fraction of E coli as described in

Experimen-tal Procedures Analysis of the purification by SDS/

PAGE showed that MltA lipoprotein was localized in

the membrane fraction (Fig 2, lane 2) Western-blot

analysis with polyclonal sera raised against MltA failed

to detect MltA in any of the soluble fractions obtained

before Chaps extraction, demonstrating exclusive

local-ization of the lipoprotein to the membrane fraction

(result not shown) After solubilization of MltA with

Chaps, it was necessary to maintain NaCl at a minimum

concentration of 120 mM to prevent the lipoprotein from

precipitating The predicted pI for MltA is 10.5 The

basic nature of the protein enabled FPLC

cation-exchange chromatography to be performed under

condi-tions that allowed almost complete removal of

contam-inating proteins in a single step (Fig 2, lane 4) Similarly,

this property was exploited to perform a simple two-step

procedure for the purification of the truncated version of

MltA, which involved salting out and cation exchange

The leaderless form is found exclusively in the cytosolic

fraction of E coli and was purified to homogeneity as

judged by SDS/PAGE with Coomassie blue staining

(Fig 2, lane 5)

Molecular mass The molecular masses of the lipoprotein and truncated forms of MltA were determined under denaturing condi-tions by SDS/PAGE (Fig 2) The two forms of the protein migrate to the same position in the gel (Fig 2), and, from a calibration plot of log mass vs relative mobility of protein standards, the masses of both forms of MltA were calculated to be 44.5 kDa This is in agreement with the molecular mass of 45 869 Da predicted from the amino-acid composition of the protein excluding the first 19-amino-acids of the leader peptide As the lipoprotein expressed with its 2138-Da leader sequence migrates to the same position as leaderless MltA, it is reasonable to conclude that the signal peptide is cleaved when this clone

is expressed The presence of detergent in the purification prevented an accurate estimation of molecular mass for MltA lipoprotein using molecular exclusion chromatogra-phy As truncated MltA lacking its LPSS was purified in the absence of detergent, we determined the native molecular mass using this form of the protein (see Experimental

Fig 2 SDS/polyacrylamide gel showing the purification and molecular mass of recombinant forms of MltA Proteins were separated by SDS/ PAGE on a 12.5% separating gel and stained with Coomassie Brilliant Blue Lane M, molecular-mass standards; lane 1, bacterial lysate after expression; lane 2, membrane fraction after 100 000 g centrifugation; lane 3, soluble fraction after extraction of membrane fraction with 0.5% CHAPS; lane 4, an aliquot from the peak fraction from Mono S FPLC ion-exchange chromatography; lane 5, truncated MltA (expressed without the LPSS) after Mono S FPLC ion-exchange chromatography.

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procedures) Truncated MltA was eluted with a Kav

corresponding to a molecular mass of 31 600 Da This

value is low compared with that of the denatured protein

suggesting either an interaction with the column or a smaller

than expected Stokes’ radius Nevertheless the native

molecular mass of the truncated form of MltA is more

indicative of a monomer than a dimer

Confirmation that MltA is a lipoprotein

To test if recombinant MltA expressed with either its

endogenous LPSS or GNA1946 LPSS was lipidated, the

ability of the proteins to incorporate [3H]palmitate was

examined Proteins extracted from cells grown in the

presence of the radiolabel were examined by SDS/PAGE

and autoradiography (Fig 3) A labelled band with a

molecular mass of 44 kDa was observed for MltA cloned

with either its own leader or the leader from GNA1946 The

radiolabel was not incorporated when MltA lacking an

LPSS was expressed

MltA is a muramidase Both the purified lipoprotein and truncated form of MltA showed muramidase activity when assayed for their ability

to degrade murein sacculi to soluble muropeptides How-ever, the activity observed with the lipoprotein form was 21.6-fold higher than the activity of the truncated form For this reason, the lipoprotein was chosen for further kinetic analyses The activity of MltA lipoprotein was enhanced 5.1-fold by the addition of 0.2% (v/v) Triton X-100 to the assay, whereas Triton X-100 had no measurable effect on the activity of the truncated soluble form of the protein Biochemical and kinetic properties of the enzyme The effect of pH on muramidase activity was determined in Tris/maleate buffer over the pH range 5.0–8.0 The optimal

pH for the reaction was determined to be 5.5 (data not shown) The optimum pH for lytic transglycosylase activity

b y MltA from E coli is 4.5 [18] Enzyme activity was measured over the temperature range 18–42C Maximum activity was observed at 37C (data not shown) As we observed that MltA has 77% of the activity at 30C as it does at 37C, the stability of cells expressing Meningococcus MltA at 30C is unlikely to be due solely to a temperature-dependent decrease in murein lytic activity as previously described for E coli MltA (see above)

The effect of ions on muramidase activity was determined

by performing the reaction with a variety of bivalent cations, at a final concentration of 10 mM Maximum activity was found with Mg2+, which stimulated activity 2.1-fold Mn2+and Ca2+stimulated enzyme activity to a similar extent, whereas Ni2+and EDTA had no significant effect on activity In contrast, Zn2+significantly inhibited enzyme activity (data not shown)

Initial-rate kinetic analyses were performed with sub-strate concentrations ranging from 2.6 to 52.0 mgÆL)1 An analysis of the Michaelis–Menten curve (data not shown) showed that the enzyme exhibits typical first-order and zero-order kinetics As the substrate for the reaction is insoluble,

it is not possible to determine the Km for the reaction in molar terms [18] However, the apparent Kmof 8.2 mgÆL)1 determined from a double-reciprocal Lineweaver–Burk plot

is slightly lower than the value (52.6 mgÆL)1) ob tained previously for MltA from E coli [18]

Substrate specificity and reaction product The ability of MltA to lyse isolated glycan strands comprising poly(MurNAc-GlcNAc)n>30was demonstrated when we separated 1,6-anhydrodisaccharide subunit reac-tion products from the oligosaccharide substrate by HPLC (Fig 4) The same elution profile was observed when we assayed E coli MltA in a control experiment (result not shown) The use of isolated glycan strands as a substrate further demonstrates homology with E coli MltA, which is also capable of utilizing both murein sacculi and isolated glycan strands [18,22]

HPLC analysis of the digestion products after incubation

of MltA with murein sacculi showed two major peaks eluted with retention times of 52.4 and 68.9 min (Fig 5) By comparing the elution profile of the calibration standard,

it was determined that these major reaction products

Fig 3 Demonstration that MltA is a lipoprotein E coli BL21(DE3)

harbouring pET21b-MltA cloned with its own LPSS, with the LPSS

from GNA1946, or without a leader sequence were grown in the

presence of [3H]palmitate Expression of recombinant protein was

induced for 1 h at 30 C by the addition of 1 m M isopropyl b- D

-thiogalactoside Cells were then washed, lysed and protein precipitated

as described in Experimental Procedures Proteins were separated by

SDS/PAGE using a 12.5% separating gel, and the labelled proteins

were visualized by autoradiography Lane 1, MltA cloned without an

LPSS; lane 2, MltA cloned with its own LPSS; lane 3, MltA cloned

with the LPSS from GNA1946 Molecular masses of marker proteins

are indicated on the left and the position of MltA is indicated by an

arrow.

Trang 7

corresponded to 1,6-anhydrodisaccharide tripeptide and

tetrapeptide, respectively The formation of the 1,6-anhydro

intramolecular bond within the muramic acid moiety

confirms that the enzyme is indeed a lytic transglycosylase

(Fig 5)

MltA–Sepharose affinity chromatography of membrane

proteins

The leaderless form of MltA was expressed, purified and

covalently bound to CNBr-activated Sepharose This

col-umn was used to isolate MltA-interacting proteins from a

membrane fraction of Meningococcus B Proteins were

eluted with a stepwise NaCl gradient and assayed for

penicillin-binding activity by incubation with 125I-labelled

ampicillin PBPs were visualized by SDS/PAGE and

auto-radiography (Fig 6) A control column prepared without

MltA was used to assess the specificity of binding The most

intensely labelled band at 62 kDa observed in the starting

material was retained by MltA–Sepharose during loading

and washing, but was completely eluted with 300 mMNaCl

In contrast, the intensely labelled 46-kDa band observed in

the starting material was not retained by the column and was

eluted in the flow through Vollmer et al [14] reported that

400 mMNaCl was sufficient to completely disrupt binding of

PBPs to E coli MltA When the autoradiograph and

Coomassie blue-stained gel were overlaid, it was not possible

to see a protein band corresponding to the 62-kDa

radioactive band This is characteristic of PBPs, which are

typically of low abundance; for example, E coli PBP2 is present at only 50 copies per cell [23,24] To date, four PBPs have been identified in Meningococcus B: PBP1, PBP2, PBP3 and PBP4 These proteins have predicted molecular masses of 88.9 kDa, 63.6 kDa 50.5 kDa and 34.1 kDa, respectively [25,26] Hence we reasoned that the 62-kDa PBP specifically retained during affinity chromatography is PBP2 To confirm this hypothesis, we analysed affinity-chromatography fractions by Western-blot analysis using polyclonal antisera raised against PBP2 from Gonococcus (Fig 7) Gonococcal PBP2 has 98% sequence identity with PBP2 from Meningococcus serogroup B Immunoblots showed an immunoreactive band with a molecular mass of

62 kDa in the starting material and in the fraction obtained after elution with 300 mM NaCl Moreover, this band migrated to the same position as purified gonococcal PBP2 The 88-kDa immunoreactive band observed in the starting material was not retained by the MltA affinity column Taken together these results demonstrate an interaction involving MltA and PBP2

D I S C U S S I O N

A genomics-based approach to vaccine discovery previ-ously identified GNA33 as a potential vaccine candidate

Fig 5 HPLC analysis of muropeptides after digestion of murein sacculi withMltA Isolated murein sacculi were digested with purified MltA and reduced with sodium borohydride The resulting muropeptides were separated by RP-HPLC on a Hypersil ODS column Elution was performed with a linear gradient from 50 m M sodium phosphate (pH 4.32) to 50% methanol in 50 m M sodium phosphate (pH 4.95) The column was calibrated and standardized with murein sacculi digested with the muramidase Cellosyl.

Fig 4 HPLC analysis demonstrating hydrolysis of isolated glycan

strands Poly(MurNAc-GlcNAc) n>30 was incubated without (A) or

with (B) MltA as described in Experimental procedures At the

com-pletion of the incubation, the sample was passed over a Nucleosil 300

C 18 column to which was applied 0.1 m M sodium phosphate buffer

(pH 2), 5% acetonitrile for 5 min, 100% methanol for 5 min, and

again starting buffer The radioactivity of the eluate was monitored.

The peak eluted between 20.2 and 22.2 min corresponds to intact

glycan strands In a control assay in which MltA was replaced with

E coli MltA, the same elution profile as seen in (B) was observed (data

not shown).

Trang 8

against meningococcal infection Sequence comparison

predicted that GNA33 encodes a lipoprotein homologous

to the lytic transglycosylase MltA from E coli To

definitively identify and characterize GNA33, we cloned

and expressed the ORF of GNA33 in E coli with and

without an LPSS Although the level of expression of the

truncated form was 20-fold higher than of the lipoprotein

form, incorporation of an LPSS in MltA increased

specific activity by 22-fold Incorporation of3[H]palmitate,

cleavage of the leader peptide, and localization of the

protein to the membrane fraction all suggest that

recom-binant MltA is correctly processed as a lipoprotein in

E coli Moreover, purification of enzymatically active

protein and lysis of host cells during expression confirmed

the fidelity of the heterologous expression system When

MltA was expressed with its own LPSS, the level of

expression was low The level of expression was increased

significantly by fusing codons 21–441 of MltA to an LPSS

from an unrelated Meningococcus B lipoprotein,

GNA1946 This LPSS in combination with MltA is

obviously efficiently processed by the

lipoprotein-process-ing machinery of E coli

We demonstrated that recombinant MltA is capable of

lysing murein sacculi, confirming that the protein is a

muramidase The lipoprotein produced two major

reac-tion products, 1,6-anhydrodisaccharide tripeptide and tetrapeptide, confirming that the protein is indeed a lytic transglycosylase Of the four exo-specific lytic transglycos-ylases in E coli studied to date, only MltA is capable of utilizing unsubstituted murein glycan strands as substrate [18] The ability of meningococcal MltA to also utilize the unsubstituted substrate shows a functional similarity between the two homologues Furthermore, in many of the biochemical parameters assessed, such as pH opti-mum, Km and requirement for bivalent cations, the

N meningitidis and E.coli enzymes are similar [9,18] These results confirm the sequence-based prediction that GNA33 is a homologue of E coli lytic transglycosylase MltA For these reasons, we assigned the name MltA to GNA33

In this study, we used affinity chromatography to demonstrate an association between meningococcal MltA and PBP2 The ability to interact with a PBP is a characteristic common to MltA from N meningitidis and

E coli and is the first description of such an association beyond that reported for E coli E coli MltA is thought

to form part of an enzyme complex composed of murein synthases and muramidases This association is believed

to facilitate the co-ordinated action of different enzymes involved in enlargement and septation of the murein sacculus [10] Reconstitution experiments with E coli

Fig 6 PBP assay of proteins fractionated by affinity chromatography

on MltA-sepharose Aliquots of fractions obtained from the elution of

the meningococcal membrane extract from either a MltA–Sepharose

or control column were assayed for the presence of PBPs with

125

I-labelled ampicillin as detailed in Experimental Procedures The

labelled fractions were subjected to SDS/PAGE on a 10% separating

gel and visualized by autoradiography after 100 h exposure SM is

membrane extract before addition to the column C indicates eluates

obtained from the control column, and T represents eluates from the

MltA–Sepharose column Shown are the first two fractions from the

wash with buffer I (150 m M NaCl) and each of the elution steps in

300 m M NaCl, 600 m M NaCl and 1 M NaCl The position of

molec-ular-mass markers is indicated.

Fig 7 Western blot of proteins fractionated by affinity chromatography

on MltA–Sepharose Aliquots of fractions obtained after elution of the meningococcal membrane extract from the MltA–Sepharose column were analysed by immunoblotting with anti-PBP2 sera Immunore-active bands were detected by enhanced chemiluminesence as described in Experimental procedures Lane 1, purified gonococcal PBP2; lane 2, membrane extract from meningococcus before addition

to the column; lane 3, fraction obtained after elution with 300 m M

NaCl The positions of molecular-mass markers are shown.

Trang 9

MltA and PBP1B demonstrated the necessity for the

structural protein MipA, and it has been proposed that

this enzyme serves as a scaffold for assembly of the

multienzyme complex [14] We performed an extended

homology search of the Meningococcus B genome but

failed to identify a homologue of MipA A similar

situation exists for Haemophilus influenzae, which contains

a homologue of MltA but not MipA [14] A BLAST

search showed that N meningitidis PBP2 and E coli

PBP3 have 39% identity and 59% homology over a

541-amino-acid overlap and revealed that meningococcal

PBP2 is more homologous to E coli PBP3 than PBP2

In fact, Meningococcus does not have a homologue of

E coli PBP2, which is involved in maintaining the

characteristic rod shape of the bacterium Interestingly,

it is the presence of either PBP2 or PBP3 in the enzyme

complex of E coli that confers a specific function to the

complex [14] In E coli, PBP2 is known to be responsible

for cell elongation, whereas PBP3 is involved in septum

formation [27,28] It will be interesting to determine if

such an enzyme complex exists in Meningococcus, the

nature and composition of the protein components, and

in particular the function of the association between

MltA and PBP2

We initially reported that antibodies raised against

GNA33 are bactericidal, a property known to correlate

with protective effects in humans [1] It was subsequently

discovered that antibodies elicited by vaccination with

GNA33 are bactericidal because MltA is an effective

mimetic antigen of the PorA epitope P1.2 [3] In its own

right, MltA may be a useful vaccine for the prevention of

disease caused by P1.2 strains Furthermore, it has been

suggested that substituting strain specific PorA loops into

MltA or its subdomains may generate immunogenic

mimetics of other serotype PorA epitopes [3] The ease of

expression and purification demonstrated in this work

further suggests the great potential that MltA offers as a

recombinant vaccine candidate against meningococcal

infection A direct role for lytic transglycosylases in

meningococcal disease is suggested by an investigation of

genes required for bacteraemic disease In an infant rat

model of N meningitidis infection, Sun and co-workers

[29] used insertional mutagenesis to identify genes

essen-tial for pathogenesis, one of which was the gene encoding

MltB A further role for lytic transglycosylases in disease

may be associated with their reaction products The

1,6-anhydrodisaccharide-containing metabolites, such as

those shown here to be produced by meningococcal

MltA, have been shown to have diverse biological

activities For instance, the cytopathology of respiratory

epithelium that is characteristic of Bordetella pertussis

infection is caused by 1,6-anhydromuramic

acid-contain-ing products [30] The same compounds are also capable

of inducing sleep and arthritis [31,32] Perhaps most

importantly is the potential of 1,6-anhydromuramyl

peptides to induce meningeal inflammation [33] Hence

lytic transglycosylases such as MltA may be directly

involved in the pathogenesis associated with

meningoc-cocal infection The potential that lytic transglycosylases

offer as targets for disease intervention combined with

their importance in growth, septation, recycling of

peptidoglycan, and pore formation makes them worthy

of further investigation

A C K N O W L E D G E M E N T S

We would like to thank Vega Masignani and Maria Scarselli for sequence comparisons and database searches, and Mariagrazia Pizza for many helpful discussions We are also grateful to Giorgio Corsi for preparing the figures and to Catherine Mallia for formatting and submitting the manuscript.

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