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Báo cáo khoa học: Characterization of an N6 adenine methyltransferase from Helicobacter pylori strain 26695 which methylates adjacent adenines on the same strand pptx

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Using different fragments of pUC19 with varying numbers of GAGG sites fragments 3 to 6, or fragments not con-taining GAGG sites fragments 1 and 2, Table S1, as a substrates for the methy

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from Helicobacter pylori strain 26695 which methylates adjacent adenines on the same strand

Ritesh Kumar1, Asish K Mukhopadhyay2and Desirazu N Rao1

1 Department of Biochemistry, Indian Institute of Science, Bangalore, India

2 Division of Bacteriology, National Institute of Cholera and Enteric Disease, Kolkata, India

Introduction

DNA methylation is one of the most common forms

of DNA modification occurring in the prokaryotic

genome This modification does not affect the

Wat-son–Crick pairing, but creates a signature motif that

can be recognized by the proteins interacting with

DNA It has been shown that DNA methylation can

enhance or abrogate the affinity of transcription

fac-tors for DNA, thus affecting gene expression and

regu-lation These base modifications thus act as a second

line of genetic information [1]

Prokaryotic DNA methyltransferases (MTases) are

classified into two major groups – exocyclic amino

MTases and endocyclic MTases – based on the

position of the methyl group on the bases The exocy-clic amino MTases methylate adenine at the N6 position and cytosine at the N4 position, whereas endocyclic MTases methylate the cytosine at the C5 position [2,3] In prokaryotes most of the MTases are associated with a restriction enzyme and form a restriction-modification (R-M) system R-M systems are involved in the protection of bacteria from bacte-riophage invasion However, the identification of MTases without any associated restriction enzyme in many bacteria has compelled biologists to explore the functions of MTases beyond the distinction of self and nonself DNA Extensive work on solitary MTases,

Keywords

base flipping; DNA methyltransferase;

Helicobacter pylori; S-adenosyl- L -methionine;

site-directed mutagenesis

Correspondence

D N Rao, Department of Biochemistry,

Indian Institute of Science, Bangalore 560

012, India

Fax: +91 80 2360 814

Tel: +91 80 2293 2538

E-mail: dnrao@biochem.iisc.ernet.in

(Received 18 November 2009, revised 26

December 2009, accepted 25 January 2010)

doi:10.1111/j.1742-4658.2010.07593.x

Genomic sequences of Helicobacter pylori strains 26695, J99, HPAGI and G27 have revealed an abundance of restriction and modification genes hp0050, which encodes an N6adenine DNA methyltransferase, was cloned, overexpressed and purified to near homogeneity It recognizes the sequence 5¢-GRRG-3¢ (where R is A or G) and, most intriguingly, methylates both adenines when R is A (5¢-GAAG-3¢) Kinetic analysis suggests a nonpro-cessive (repeated-hit) mechanism of methylation in which HP0050 methyl-transferase methylates one adenine at a time in the sequence 5¢-GAAG-3¢ This is the first report of an N6 adenine DNA methyltransferase that methylates two adjacent residues on the same strand Interestingly, HP0050 homologs from two clinical strains of H pylori (PG227 and 128) methylate only 5¢-GAGG-3¢ compared with 5¢-GRRG-3¢ in strain 26695 HP0050 methyltransferase is highly conserved as it is present in more than 90% of

H pylori strains Inactivation of hp0050 in strain PG227 resulted in poor growth, suggesting its role in the biology of H pylori Collectively, these findings provide impetus for exploring the role(s) of this conserved DNA methyltransferase in the cellular processes of H pylori

Abbreviations

2AP, 2-aminopurine; AdoMet, S-adenosyl- L -methionine; Dam, DNA adenine methylase; DLS, dynamic light-scattering; IPTG, isopropyl thio-b- D -galactoside; KD, dissociation constant; LB, Luria–Bertani; MTase, methyltransferase; Rh, hydrodynamic radius; R-M, restriction-modification.

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such as DNA adenine methylase (Dam) and cell

cycle-regulated methylase (CcrM), have indeed shown the

role of DNA methylation in regulating cellular events

such as bacterial virulence, cell cycle regulation and

phase variation [4–6]

The Gram-negative bacterium Helicobacter pylori

persistently colonizes the human stomach and is

wide-spread throughout the world It is a major cause of

gastritis and peptic ulcer disease, and is an early risk

factor for gastric cancer H pylori is one of the most

genetically diverse species of bacteria, and

strain-spe-cific genetic diversity has been proposed to be involved

in the organism’s ability to cause different diseases

[7,8] Analysis of genome sequences of H pylori strains

26695 and J99 revealed the presence of 23 and 22 R-M

systems, respectively, far more than the number

detected in other bacterial genomes sequenced to date

[9–11] Two more H pylori strains – HPAG1 (isolated

from a patient with chronic atrophic gastritis) and

G27 – were sequenced and a similar number of

puta-tive R-M systems were identified [12,13] Comparison

of strains 26695 and J99 showed that the two genomes

are quite similar, with only 6–7% strain-specific genes

R-M systems are a major source of the strain

differ-ences [14] iceA-hpyIM, which encodes a cognate

restriction enzyme and an N6 adenine methylase has

been studied in various H pylori strains It was shown

that hpyIM expression is growth-phase regulated and

required for normal bacterial morphology Deletion of

hpyIM altered the expression of the stress-responsive

dnaK operon, suggesting that hpyIM may play a role

in H pylori physiology beyond its R-M function [15]

The Type II MTase, M.HpyAIV, which recognizes the

5¢-GANTC-3¢ site, has been shown to affect the

expression of the katA gene encoding the H pylori

catalase [16]

H pylori 26695 has three DNA MTases that lack

cognate restriction enzymes Vitkute et al [17] and Lin

et al [18] showed that HP0050, an orphan N6 adenine

MTase from H pylori 26695 recognizes 5¢-GAGG-3¢

and methylates adenine; these findings were based on

the results of a restriction endonuclease assay The

ORF hp0050 has been reported to be part of an R-M

system that contains two MTases and an inactive

restriction endonuclease This R-M system was later

assigned as HpyAVI, with hp0050 designated as

M1.HpyAVI, hp0051 as M2.HpyAVI and hp0052 as

HpyAVIP (putative) The hp0050 homolog of H pylori

strain HPAGI (HPAG1_0046) is a chronic atrophic

gastritis-associated gene [12]

Strain-specific DNA-modification genes are thought

to influence strain-specific phenotypic traits, host

speci-ficity, adaptability to changing micro-environmental

conditions or virulence [14] The identification and study of both species-specific and strain-specific MTases of H pylori could enhance our understanding

of the pathogenic mechanisms of this organism Our findings indicate that hp0050 from strain 26695 has evolved a relaxed specificity as a result of mutations, compared with other strains These observations fur-ther highlight the capability of this organism to undergo random mutations and evolve proteins with new functions

Results and Discussion HP0050 is an N6 adenine MTase from H pylori and belongs to the b subgroup of MTases, based on the linear arrangement of the S-adenosyl-l-methionine (AdoMet)-binding domain (FXGXG), the target rec-ognition domain and the catalytic domain (DPPY) HP0050 MTase is present in all the three sequenced strains of H pylori HP0050 MTase is present in all the three strains of H pylori (26695, J99 and HPAGI) for which genome has been sequenced The HP0050 proteins from H pylori J99 and HPAG1 have 91.7% and 90% identities respectively, to the HP0050 protein from H pylori 26695 [19] In H pylori 26695, hp0050 exists as an overlapping ORF with another MTase, hp0051 These MTases are remnant MTases of a defunct R-M system Both these ORFs have a high similarity with the MnlI DNA MTase that belongs to the Type IIS R-M system [20] However, in H pylori the functional MnlI restriction enzyme is absent [21]

Cloning, overexpression and purification of HP0050 protein

A 699 bp fragment (Fig S1A), representing the hp0050 gene from H pylori 26695, was PCR amplified using primers 1 and 2 (Table 1) and cloned between the BamHI and XhoI sites of the expression vector pET28a (data not shown) A polypeptide of the expected

Table 1 Primers used for cloning and mutagenesis The restriction enzyme site is indicated in bold letters SN, serial number.

SN Primer sequence (5¢- to 3¢)

Restriction site created(+) ⁄ lost(-)

5 TAGATCCTTCCATGGGGAGCGGCACCACCGGCT NcoI (+)

6 AACCGAAATGTTTAAAGGAGGGTCCGTGATGAT Psi I (-)

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molecular mass (32 kDa) was expressed at high levels

upon induction with 0.5 mm isopropyl

thio-b-d-galac-toside (IPTG) (Fig S1B) HP0050 was expressed as an

N-terminal His-tagged protein and was purified As

the purified HP0050 protein has an N-terminal

His-tag, western blot analysis was carried out with anti-His

IgG and a single band corresponding to HP0050

pro-tein was detected (Fig S1C) The His-tag was removed

using the Thrombin cleancleaveTM kit, according to

the manufacturer’s instructions (see the Experimental

procedures) The protein was purified to > 95%

homogeneity, as judged by SDS⁄ PAGE followed by

silver staining (Fig S1D)

Peptide finger mapping of HP0050

A peptide finger map of the HP0050 protein was

obtained by digesting purified HP0050 protein with

trypsin and subjecting it to MALDI analysis The

finger map thus obtained was then matched with

the expected finger map It was found that eight

pep-tide ions matched with the expected ions, as shown by

the asterisk in Fig S2A, suggesting the authenticity of

the purified protein

Oligomeric status of HP0050 protein

HP0050 protein elutes as a monomer, and the molecular

mass was determined to be 28 kDa by analytical

gel-fil-tration chromatography (Fig S2B) Dynamic

light-scat-tering (DLS) measurements on HP0050 MTase were

performed on a DynaPro DLS instrument using 20 lL

of 1.5 mgÆmL)1 of protein with a data-acquisition time

of 10 s Scattering intensities at various time intervals

(ls) with the initial (t = 0 s) intensity were compared

and a combined correlation function was constructed

(inset, Fig S2C) As seen in Fig S2C, DLS data, when

fitted to the Stokes–Einstein equation, gave a

hydrody-namic radius (Rh) of 2.2 nm The frictional ratio was

calculated as 0.89, suggesting that HP0050 is more or

less spherical in structure An ideal spherical protein

would give a value of 1.0 Higher values indicate an

anisotropic structure

Kinetics of methylation reaction

To establish the relationship between the initial

veloc-ity of the reaction and the enzyme concentration, the

rate of DNA methylation catalysed by HP0050 was

determined pUC19 DNA was used as a substrate

Different concentrations of HP0050 protein (10–

100 nm) were added to the reaction mixture containing

DNA (80 nm) and AdoMet (2.0 lm) and incubated at

37C When the initial velocities were plotted against increasing enzyme concentrations, a linear relationship was obtained (Fig 1A) This indicated that the initial velocity of the reaction was directly proportional to the enzyme concentration Next, the initial velocities were determined at various concentrations of the sub-strates, [3H]AdoMet and pUC19 DNA For the deter-mination of Km (DNA), a series of similar reactions containing HP0050 MTase (100 nm), [3H]AdoMet (2.0 lm) and increasing concentration of pUC19 DNA (10–80 nm) were performed and a conventional hyper-bolic dependence was obtained Nonlinear regression analysis of initial velocity versus DNA concentration established the Km (DNA)as 19.9 ± 3 nm (Fig 1B)

To determine Km (AdoMet), a series of reactions containing HP0050 MTase (100 nm), DNA (50 nm) and increasing concentration of [3H]AdoMet (0.3–

12 lm) were performed Increasing the concentration

of AdoMet led to a progressive stimulation in the reaction rate Whereas the initial portion of the concentration-dependence curve corresponded approx-imately to a conventional hyperbolic dependence, saturation was not achieved (Fig 1C) Similar obser-vations have been reported for T4 Dam and EcoDam [22,23]

Determination of site of methylation The recognition sequence of HP0050 MTase was previ-ously reported by Vitkute et al [17], based on restric-tion enzyme digesrestric-tion, to be 5¢-GAGG-3¢, where A is methylated by HP0050 MTase in the target site Using different fragments of pUC19 with varying numbers of GAGG sites (fragments 3 to 6), or fragments not con-taining GAGG sites (fragments 1 and 2, Table S1), as

a substrates for the methylation reaction by HP0050 MTase, it was observed that besides fragments with GAGG sites, fragment 2 (without GAGG site) was also methylated It should be noted that fragment 2 has one GAAG site, which could be a recognition site for HP0050 MTase

There are 20 GAAG and 13 GAGG sites per mole-cule of pUC19 To further confirm this observation we used 26 mer duplex substrates (Table 2) with GAGG (duplex 1), GGAG (duplex 2), GAAG (duplex 3), GTGG (duplex 4), GAGA (duplex 5) or GmAmAG (duplex 8) site to determine the specificity of HP0050 MTase It was found that HP0050 MTase recognized and methylated GAGG, GGAG and GAAG, but did not methylate GTGG, GmAmAG or GAGA (Fig 2)

As HP0050 was able to recognize and methylate both GAGG and GGAG, it was of interest to determine which A was the target for the MTase in the

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oligonu-cleotide with the GAAG sequence To address this, two 26-mer duplex substrates – one with 5¢- GAmAG-3¢ (duplex 6) and the other with 5¢-GmAAG-GAmAG-3¢ (duplex 7) (where mA is the methyl-adenine) site – were used individually as a substrate in the methylation assay It was found that HP0050 MTase was able to methylate duplex 6 and duplex 7, suggesting that both adenine residues were targets for HP0050 MTase (Fig 2), and

Table 2 Duplex DNA used in this study The underlined region of the oligonucleotide represents the HP0050 MTase recognition sequence, and restriction enzyme sites are shown in bold 2, 2-amino purine; Bt, biotin; mA, methyl adenine.

Duplex Sequence (5¢- to 3¢)

ATGTTACATGGCTCCTAGATAACTAG

ATGTTACATGGCCTCTAGATAACTAG

ATGTTACATGGCTTCTAGATAACTAG

ATGTTACATGGCACCTAGATAACTAG

ATGTTACATGGCTCTTAGATAACTAG

ATGTTACATGGCTTCTAGATAACTAG

ATGTTACATGGCTTCTAGATAACTAG

ATGTTACATGGCTTCTAGATAACTAG

ATGTTACATGGCTCCTAGATAACTAG

ATGTTACATGAGCTTCGATAGATAACTAG

ATGTTACATAGTACTTCATGAGATAACTAG

ATGTTACATAGCGCTTCGCGAGATAACTAG

GAAGCTGATCGAGTC ATGTTACATGAGCTCGATCTATAGATAAACCTT CGACTAGCTCAG

ATGATGTTGT TATGACATGGCTCCGACGCTAGATCCAGACGAC TCCTACTACAACA

ATGTTACATGGCTTCTAGATAACTAG

GAGGATGATGTTGT TATGACATGGCTCCGACGCTAGATCCAGACGAC TCCTACTACAACA

ACGCTCCTACCAGACAGCTTCGACTACAA

ATGTTACATGGCTTCGAGATAACTAG

A

B

C

600

400

200

0

500

400

300

200

100

0

2500

2000

1500

1000

500

0

HP0050 (n M )

pUC19 DNA (n M )

AdoMET (µ M )

Fig 1 Kinetics of methylation (A) Initial ,velocity versus the

con-centration of HP0050 MTase Increasing concon-centrations of HP0050

MTase (10–100 n M ) were incubated with 80 n M pUC19 and 2.0 l M

AdoMet in standard reaction buffer at 37 C for 15 min, then the

reaction was stopped and analyzed as described in the

Experimen-tal procedures (B) Determination of Km (DNA) Methylation assays

were carried out in reactions containing 2.0 l M [3H]AdoMet and

increasing concentrations of pUC19 DNA (10–80 n M ) in standard

reaction buffer at 37 C for 15 min HP0050 MTase (100 n M ) was

added to start the reaction The data points were analysed using

nonlinear regression analysis (C) Initial velocity versus the

concen-tration of AdoMet Methylation assays were carried out in

reactions containing 50 n M pUC19 DNA and increasing

concentra-tions of [ 3 H] AdoMet (0.3–12 l M ) in standard reaction buffer at

37 C for 15 min HP0050 MTase (100 n M ) was added to start the

reaction.

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this was carried out at different protein concentrations

(data not shown)

Experiments were then performed to estimate the

kinetic constants for these DNA substrates by

nonlin-ear regression analysis The duplex with GAGG was

the substrate most preferred, with a Kmof 5.2 lm, and

DNA with a GAAG site was a preferred substrate over

DNA with GGAG, GAmAG or GmAAG sites, with a

Km of 13 lm compared with Km values of 17 lm,

27 lm or 29 lm, respectively (Table 3) In addition, the

kcat⁄ Km(specificity constant) was calculated for

differ-ent DNA substrates and it was found that the

specific-ity constant for duplex 1 was 10 times higher than the

specificity constant for duplex 2, suggesting that duplex

1 was a better substrate than duplex 2 (Table 3) The

specificity constant for duplex 3 was 2.1-fold higher

than the specificity constant for duplex 2, and the Km

values were very similar, which again suggests that both

the adenines are methylated by HP0050 MTase

Furthermore, to confirm the observation that both

adenines in GAAG are methylated by HP0050 MTase,

duplex 10 (Table 2) was used as a substrate Duplex 10

contains an HP0050 MTase recognition sequence (GAAG) with overlapping AluI (AGCT) and TaqI (TCGA) restriction sites Upon methylation with HP0050 MTase if both adenine bases were modified, the DNA would be resistant to both AluI and TaqI digestion It is clear from Fig 3A that the methylated duplex is resistant to restriction with AluI and TaqI, confirming that HP0050 MTase indeed methylates both the adenines in 5¢-GAAG-3¢ Furthermore, duplex 11 (Table 2) was used, which contains an HP0050 MTase site (GAAG) with an overlapping ScaI site (AG-TACT), as a substrate in the methylation assays Upon methylation, if the second adenine was methylated in GAAG, the DNA would be resistant to ScaI digestion

It was found that upon methylation with HP0050 MTase the duplex DNA was resistant to ScaI digestion (Fig S3A) It is possible that HP0050 MTase binds strongly to the duplex and thus inhibits the cleavage

To rule out this possibility we used duplex 12, which contains an HP0050 MTase site (GAAG) with an over-lapping AfeI site (AGCGCT), as a substrate in the methylation assays AfeI is not sensitive to the methyla-tion status of adenine in its cognate sequence It was found that, upon methylation, the duplex DNA was sensitive to digestion with AfeI (Fig 3B) In addition, duplex 13 was used, which contains two AluI sites – one overlapping with the HP0050 MTase site (GAAG) and other 15 bp away from it When duplex 13 was methylated by HP0050 MTase and then digested with AluI, two fragments were obtained It was observed that, upon methylation, the AluI site overlapping with the HP0050 MTase cognate sequence became resistant

to AluI digestion However, three fragments of same size were obtained when unmethylated duplex 13 was digested with AluI (Fig S3B) To eliminate the possibil-ity that AluI is blocked by modification immediately outside its recognition site, duplex 18 was used Duplex

18 has a GAAG site with an overlapping AluI site and

in which the first A was methylated (GmAAG) Duplex

18 was completely digested with AluI, suggesting that the modification immediately outside the recognition site of AluI has no effect on its activity (Fig S3C)

1600

1200

800

400

0

Oligonucleotide (µ M )

GGAG GmAAG GAmAG GTGG GAGA GmAmAG

Fig 2 Specificity of HP0050 MTase (A) Methylation activity of

HP0050 MTase as a function of increasing concentrations of

differ-ent 26-mer duplex DNA species Methylation assays were carried

out in reactions containing 2.0 l M [ 3 H]AdoMet and increasing

con-centrations of 26-mer duplex DNA (2.5–15 l M ), with one GAGG site

or with a modified GAGG site, in standard reaction buffer at 37 C.

HP0050 MTase (100 n M ) was added to start the reaction (d,

GAGG; , GAAG; , GGAG; , GmAAG; r, GAmAG; s, GTGG; h,

GAGA; D, GmAmAG) mA, methyl adenine.

Table 3 Kinetic parameters for HP0050 N 6 adenine methyltransferase.

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To further confirm the methylation of adjacent

ade-nines in GAAG, we used duplex 17, which contains a

FokI site (GGATG) and GAAG, which is 7 bp away

from the FokI site Duplex 17 was used as a substrate

and the methylation reaction was carried out in the

presence of [3H] AdoMet The methylated duplex was

purified and then digested by FokI, which resulted in

two fragments, each containing one adenine from

GAAG These fragments were separated by

electro-phoresis on a 20% polyacrylamide gel and then

checked for the incorporation of radiolabel It was

found that both fragments were labelled, confirming

that HP0050 MTase indeed methylates both the

ade-nines in 5¢-GAAG -3¢ (Fig 4) It is worth mentioning

here that the Type IIS MnlI R-M system, comprising

N6 adenine and C5 cytosine MTase and a restriction

endonuclease, recognizes the nonpalindromic

nucleo-tide sequence 5¢-CCTC(N)7 ⁄ 6-3¢ While the C5 MTase modifies the first cytosine base within the 5¢-CCTC-3¢ sequence, the N6 adenine MTase methylates the bottom strand of the MnlI target, resulting in 5¢-G mAGG Interestingly, these two MTases share the greatest degree of similarity with HP0050 MTase and HP0051 MTase from H pylori 26695 [20] In the case of the FokI MTase, two domains are responsible for methylating two adenine residues – one in the upper strand and one in the lower strand [24].Yet another variation is seen in the case of MmeI, where it has been reported that MmeI modifies the adenine in the top strand of the recognition sequence 5¢-TCC RAC-3¢ and uses modification only on one of the two DNA strands for host protection [25] Interestingly, M.Alw261, M.Eco31l and M.Esp3l methylate both strands of their recognition sites, yielding C5 methyl

AluI TaqI

*

29 mer

12 mer/13 mer

Unmethylated duplex 12

Methylated duplex 12 M

50 bp

30 bp

A

B

Fig 3 Comparison of restriction digestion patterns of methylated and unmethylated duplex DNA (A) Restriction digestion of 29-mer duplex

10 M, molecular mass marker, AluI and TaqI denote digestion of duplex 10 with these respective enzymes Schematic representation of the 29-mer duplex 10 is shown with HP0050 MTase and overlapping AluI and TaqI sites (B) Restriction digestion of the 30-mer duplex 12 AfeI denotes digestion of duplex 12 Schematic representation of the 30-mer duplex 12 is shown with HP0050 MTase and an overlapping AfeI site The underlined region of the oligonucleotide represents the HP0050 MTase recognition sequence UD, undigested duplex.

* Corresponds to a 50-bp band in the marker.

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cytosine and N6 methyl adenine on opposite strands

[26] To the best of our knowledge, M.CviPII is the

only other DNA MTase that modifies adjacent

resi-dues in the cognate sequence In addition to modifyng

the first cytosine in CCD (D = A, G or T) sequences,

M.CviPII also modifies both the cytosines in CCAA

and CCCG sites [27]

Processivity of DNA methylation

HP0050 MTase methylates adjacent adenines in

GAAG The methylation can take place either in a

sin-gle binding event or in two separate binding events

To address this, 100 nm HP0050 MTase was

pre-incu-bated with 5 lm AdoMet for 10 min at 37C to

pro-mote the formation of the protein–AdoMet complex

This complex was then made catalytically competent

by adding 2 lm duplex 15 and incubated for an

addi-tional 5 min on ice to allow the formation of a ternary

complex Following the second incubation, the

reac-tion mixture was split in two and 40 lm duplex 3 was

added in one set as a trap and the other set was

allowed to proceed without the DNA trap Both the

reaction mixes were incubated at 25C, and reaction

aliquots withdrawn at 2 min intervals were checked for

methylation The reaction mixes were incubated at

25C in order to decrease the turnover rate so that

the first turnover could be monitored

If HP0050 MTase methylates in a nonprocessive

manner, it would dissociate from the substrate

mole-cule after each round of methylation and would

re-associate in the next round of catalysis If, however,

the MTase works in a processive manner, then it would

dissociate from the substrate molecule after methylating both the adenines in GAAG (duplex 15) A biotin– avidin microplate assay was used to separate biotiny-lated substrate from nonbiotinybiotiny-lated duplex DNA and

to monitor the methylation of biotinylated substrate The addition of a molar excess of duplex 3 to duplex

15 at different time-points of the modification reaction

of the GAAG substrate resulted in a decrease in the rate of methylation of duplex 15 (Fig 5A) This result clearly suggests that HP0050 methylates adjacent adenines in a nonprocessive manner

To determine if HP0050 MTase methylates the duplex with two recognition sites in a nonprocessive manner, we used duplex 16 containing two GAGG sites (duplex 14 with a 5¢ biotin tag) as a substrate and duplex 14 as competitor DNA The biotin–avidin mi-croplate assay was used to separate biotinylated sub-strate from nonbiotinylated duplex DNA and to monitor the methylation of biotinylated substrate It was observed that, in the presence of a 20-fold excess

of nonbiotinylated duplex DNA, the extent of the methylation reaction did not increase, but in the absence of nonbiotinylated competitor, methylation was observed (Fig 5B) This suggests a distributive mechanism of methylation In this assay, EcoDam was used as a positive control for the processive mecha-nism of methylation (data not shown)

Yet another approach was used to show the proces-sivity of HP0050 A 294 bp dsDNA containing a GAAG site with overlapping AluI and TaqI sites (simi-lar to duplex 10) was used for the methylation assay The master mix (400 lL) containing 1 lm HP0050 MTase was incubated with 5 lm [3H] AdoMet and

Duplex 17

FokI

29 bp

1

19 10

2200 ± 150

Fragment c.p.m.

Duplex 17

Fragment 1 (19 bp) 950 ± 100

Fragment 2 (10 bp) 850 ± 100

20% PAGE

Fig 4 Analysis of the methylation pattern

of HP0050 MTase Duplex 17 was

methylat-ed by HP0050 MTase using [ 3 H]AdoMet After cleavage with FokI, the DNA was electrophoresed through a 20% polyacryl-amide gel and specific restriction fragments (Fragments 1 and 2) were isolated The labelled methyl group contents of the fragments are shown in counts per minute (c.p.m.).

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3 lm of 294 bp dsDNA at 25C (to decrease the

turn-over) Two aliquots (of 25 lL each) were withdrawn at

3-min intervals up to 15 min and the reactions were

stopped by snap-freezing in liquid nitrogen One

ali-quot from each time-point was analyzed for protection

from AluI digestion and the other for protection from

TaqI digestion (Fig 6) If HP0050 methylates adjacent

adenines in a processive manner there should not be

any difference in the resistance to AluI digestion and

to TaqI digestion However, if HP0050 methylates

adjacent adenines in a nonprocessive manner then the

substrate DNA should show early resistance to TaqI

digestion compared with AluI digestion

It is evident from Fig 6 that after 3 min the

sub-strate starts showing resistance to TaqI digestion but

shows AluI resistance only at the 6-min time-point

These results suggest that HP0050 methylates adjacent

residues in a nonprocessive manner In general, DNA

MTases accompanied with a restriction enzyme, such

as M.EcoRI exhibit a nonprocessive mechanism of

action, whereas solitary MTases, such as T4 Dam and

EcoDam, methylate DNA in a processive manner [3]

Purification and characterization of

AdoMet-binding motif (F195S) and catalytic

motif (Y32L) HP0050 mutant proteins

All N6adenine MTases have conserved characteristic

motifs such as the AdoMet-binding motif (FXGXG)

and the catalytic motif (DPPY) Several research groups have performed mutational studies on amino acids in these motifs, which, in turn, have revealed the significance of these motifs in catalysis [1,3] For instance, Pues et al [28] have shown in the case of M.TaqI that replacement of Y108 with alanine or glycine resulted in mutant MTases with reduced enzy-matic activities, which highlights the importance of tyrosine in the methylation activity It was shown that the replacement of F39 with alanine in the AdoMet-binding motif of M.EcoRV abrogated AdoMet AdoMet-binding [29] Site-directed mutagenesis was performed to replace F195 and Y32 of HP0050 MTase by serine and lysine, respectively Both the AdoMet-binding motif (F195S) and the catalytic motif (Y32L) HP0050 mutant proteins were purified to near homogeneity and analyzed on an SDS-polyacrylamide gel for altera-tions in their electrophoretic mobilities Both mutant proteins fractionated like the wild-type HP0050 protein and no apparent changes were detected To determine the size and subunit structure of the HP0050 mutant proteins in solution, gel-filtration chromatography was performed and it was found that the mutant proteins eluted as monomers with a molecular mass of 28 kDa (data not shown) Analysis of the wild-type, F195S and Y32L mutants did not reveal significant differ-ences in the CD spectra (data not shown), indicating that the amino acid exchanges did not affect the over-all structure of the mutant proteins

HP0050+AdoMet

HP0050-AdoMet Binary complex

at 37°C

Ternary complex at 4°C

+ competitor – competitor

0 2 4 6 8

Time (min)

Without competitor

Without competitor Competitor added at 0 min

Competitor added at 0 min Competitor added at 4 min

Competitor added at 4 min Competitor added at 8 min

Competitor added at 8 min

10 12 14 16 0 2 4 6 8

Time (min)

10 12 14 16

100

200 300

400

200 0

Fig 5 Nonprocessive methylation catalyzed by HP0050 MTase HP0050 MTase (100 n M ) was incubated with 5 l M [3H]AdoMet at 37 C for

10 min to facilitate formation of the HP0050–AdoMet binary complex and then the 2 l M duplex 15 or duplex 16 was added The mixture was incubated on ice for 5 min to allow the formation of a ternary complex Then, the mixture was divided into two sets and 40 l M duplex

3 or duplex 14 was added to one set at different time-points ( , 0 min; , 4 min; and , 8 min) and the other set was allowed to proceed without a DNA trap (d), as described in the Experimental procedures The reaction was monitored at 2-min time intervals by processing

25 lL of the reaction mixture in duplicate (A) Duplex 15; (B) duplex 16.

Trang 9

The methylation activity of both the mutant

proteins was analysed as a function of increasing

enzyme concentration It was found that both the

mutant proteins were catalytically inactive compared

with wild-type HP0050 MTase (Fig 7A) The loss of

activity could be a result of the inability of these

mutant proteins to bind to one or both substrates To

investigate the AdoMet binding of the F195S mutant,

fluorescence emission spectra and fluorescence

intensi-ties were measured in the presence of different

concen-trations of AdoMet The F195S mutant protein

showed significantly less quenching in the presence of

AdoMet (up to 80 lm) compared with wild-type

HP0050 MTase The Ka value for AdoMet was

calcu-lated (using a modified Stern-Volmer plot) as 7 lm for

the wild-type protein and (using a Stern–Volmer plot)

as 64 lm for the F195S mutant (Fig S4), which is

nine times higher than that obtained for the wild-type

MTase This result showed that the F195S mutant was

not able to bind to the AdoMet as effectively as the

wild-type protein, therefore resulting in the loss of

activity When the Y32L mutant protein was analysed for its AdoMet-binding property, it was found to binds to AdoMet as efficiently as wild-type HP0050 MTase (Fig S4) but was catalytically inactive (Fig 7A)

DNA distortion induced by wild-type HP0050 MTase upon binding to 2-aminopurine-containing duplexes

Most DNA MTases flip the target base within the cog-nate sequence [30] The fluorescence of 2-aminopurine (2AP) is often used as a signal for base flipping because it shows enhanced fluorescence when its envi-ronment is perturbed However, it is now well estab-lished that the enhancement of 2AP fluorescence is a more general measure of DNA distortion [31] To study the change in DNA conformation in the enzyme–DNA complex, we used the 2AP fluorescence-based assay Irradiation of oligonucleotide (upper strand, duplex 9) containing 2AP at a target base instead of at an adenine base, at 320 nm produced a strong fluorescence emission spectrum with a kmax at

375 nm (Fig 7B) Annealing of this oligonucleotide with the complementary strand resulted in a decrease

of approximately threefold in fluorescence intensity at

375 nm When HP0050 MTase (100 nm) was incubated with 200 nm double-stranded 2AP DNA (duplex 9, Table 2), a fivefold increase in 2AP fluorescence was observed The increased fluorescence observed upon enzyme binding was more substantial than the fluores-cence of the single-stranded 2AP oligonucleotide This suggests that the increased fluorescence was not just caused by an enzyme-induced local unwinding of the helix resulting in a region of single-stranded DNA sur-rounding the 2AP, but possibly a result of DNA dis-tortion caused by binding of the protein The addition

of 1 lm sinefungin (an AdoMet analog) resulted in further enhancement of fluorescence Interestingly, the addition of sinefungin shifted the fluorescence emission spectrum 10 nm towards a longer wavelength This could be because of a change in the environment of the adenine base upon the addition of sinefungin By contrast, the Y32L mutant of the HP0050 MTase failed to show any increase in fluorescence, suggesting that, unlike the wild-type MTase, the mutant protein was not able to interact with DNA, and this could be the reason for being catalytically inactive When the F195S mutant was incubated with double-stranded 2AP DNA (duplex 9, Table 2), an increase in 2AP fluorescence was observed, but the addition of 1 lm sinefungin did not lead to further enhancement of fluorescence This is in agreement with the observation

TaqI

294 bp

150/146 bp

1.6% Agarose gel

AluI

0

10

20

30

40

50

Taql

Alul

Time (min)

Fig 6 Nonprocessive methylation of adjacent adenines in

5¢-GAAG-3¢ by HP0050 MTase HP0050 MTase (1 l M ) was incubated

with 5 l M [3H]AdoMet and 3 l M of 294-bp dsDNA at 25 Two

aliquots (each 25 lL) were withdrawn at 3-min intervals up to

15 min and the reactions were stopped by snap-freezing in liquid

nitrogen One of these aliquots was analyzed for protection from

digestion with AluI ( ) and the other was analyzed for protection

from digestion with TaqI (d).

Trang 10

that the F195S protein does not bind AdoMet Using

the 2AP fluorescence-based assay, enhancements in

flu-orescence upon enzyme binding to canonical sequences

have been reported with other MTases, such as

EcoDam [32] and T4Dam [33]

Distribution of hp0050 in clinical H pylori isolates

The strains of H pylori (26695, J99 and HPAG1) for

which the genome sequence is available were isolated

from patients with superficial gastritis, duodenal ulcer

and chronic atrophic gastritis, respectively In the

pres-ent study a number of clinical isolates of H pylori

were screened for the presence of hp0050 hp0050 was

found to be present in 97.14% of strains obtained

from patients [n = 73 (Kolkata strains)] compared

with 90.63% of strains from healthy volunteers

[n = 32 (Santhali strains)] (data not shown) Primers 3

and 4 (Table 1) were used to amplify hp0050

homo-logs The functionality of HP0050 MTase in the strains

was checked by digestion with MnlI If a strain has a

functional MTase then the genomic DNA will be

resis-tant to digestion with MnlI It was found that all

strains which were positive for the presence of hp0050

by PCR were resistant to digestion with MnlI (data

not shown) Kolkata strains are H.pylori isolates from

patients suffering from ulcer, gastritis or cancer,

whereas Santhali strains are isolates from healthy

vol-unteers [34] The hp0050 gene from two clinical isolates

(strain PG227 isolated from a patient suffering from

duodenal ulcers and strain 128 isolated from a patient

with antral gastritis) was cloned into the BamHI and

XhoI sites of pET28a, overexpressed and the proteins purified as mentioned in the Experimental procedures Both were found to be as active as wild-type HP0050 MTase (from H pylori 26695), and, in the presence of

1 lm sinefungin, which is a competitive inhibitor of all MTases, methylation activity was inhibited by 70%, similarly to the wild-type MTase (data not shown) The hp0050 gene from H pylori strains PG227 and

128 was sequenced and found to be 89% similar to its homolog from strain 26695 (Fig 8A)

Interestingly, when HP0050 MTase homologs were checked for their specificity, it was found that HP0050 MTase from strains PG227 and 128 methylate GAGG but do not methylate GAAG or GGAG (Fig 8B)

A dot-blot assay was performed to further confirm this observation using duplexes 1, 2 and 3 (Table 2) (Fig 8C–D) These observations suggest that because

of mutations, hp0050 from strain 26695 has evolved relaxed specificity HP0050 MTase from strain 26695 is able to methylate GAAG and GGAG, whereas its homologs from strains PG227 and 128 lack this speci-ficity as they methylate only GAGG Because HP0050

is an orphan MTase and lacks a cognate restriction enzyme, it can afford to undergo mutations that result

in changed specificity

Isolation and characterization of the Dhp0050 derivative of H pylori

Transcriptional regulation by methylation patterns has been described for a number of prokaryotes, where promoter methylation alters the interaction of

Duplex 9 + wild type HP0050 MTase + Sf

a

Enzyme (n M )

Wild type

a

c Duplex 9 + F195S + Sf

d

F195S Y32L

Duplex 9 + wild type HP0050 MTase

d

Duplex 9 + Y32L

e

ss 2AP DNA

f g

Duplex 9

B A

Y32L F195S

550 440

330 220 110 0

Wavelength (nm)

600

400

200

0

Fig 7 Characterization of HP0050 MTase Y32L and F195S mutants (A) Initial velocity versus enzyme concentration Increasing concentra-tions of wild-type or mutant HP0050 MTase (10–80 n M ) were incubated with 80 n M pUC19 and 2.0 l M AdoMet in the presence of 10 m M

Tris ⁄ HCl, pH 8.0, containing 5 m M b-mercaptoethanol, at 37 C for 15 min The reactions were stopped and analyzed as described in the Experimental procedures ( ) wild type, (•) Y32L, ( ) F195S (B) Steady-state fluorescence emission spectra of 2AP-substituted DNA with HP0050 MTase Spectra were recorded after incubating 100 n M enzyme and 200 n M duplex 9 for 15 min on ice in 10 m M Tris ⁄ HCl, pH 8.0, containing 5 m M b-mercaptoethanol The total volume of the reaction mixture was 400 lL Curve a, HP0050 MTase with duplex 9 in the presence of 1 l M sinefungin; curve b, F195S mutant with duplex 9; curve c, F195S mutant with duplex 9 in the presence of 1 l M sinefungin; curve d, HP0050 MTase with duplex 9; curve e, Y32L mutant with duplex 9; curve f, 2AP ssDNA; curve g, duplex 9; curve h, HP0050 MTase with sinefungin.

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