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Base pairs in the duplex exhibit slide 1.96 A˚ and intermediate values for X-displacement 3.23 A˚, as in ADNA, while their inclination to the helical axis is not prominent.. Importantly,

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Solution structure of 2¢,5¢ d(G4C4)

Relevance to topological restrictions and nature’s choice of phosphodiester links Bernard J Premraj1, Swaminathan Raja1, Neel S Bhavesh2, Ke Shi3, Ramakrishna V Hosur2,

Muttaiya Sundaralingam3and Narayanarao Yathindra1

1

Department of Crystallography and Biophysics, University of Madras, Guindy Campus, Chennai, India;2Department of Chemical Sciences, TIFR, Colaba, Mumbai, India;3Department of Chemistry, The Ohio State University, Columbus, OH, USA

The NMR structure of 2¢,5¢ d(GGGGCCCC) was

deter-mined to gain insights into the structural differences between

2¢,5¢- and 3¢,5¢-linked DNA duplexes that may be relevant

in elucidating nature’s choice of sugar-phosphate links to

encode genetic information The oligomer assumes a duplex

with extended nucleotide repeats formed out of mostly

N-type sugar puckers With the exception of the 5¢-terminal

guanine that assumes the syn glycosyl conformation, all

other bases prefer the anti glycosyl conformation Base pairs

in the duplex exhibit slide ()1.96 A˚) and intermediate values

for X-displacement ()3.23 A˚), as in ADNA, while their

inclination to the helical axis is not prominent Major and

minor grooves display features intermediate to A and

BDNA The duplex structure of iso d(GGGGCCCC) may

therefore be best characterized as a hybrid of A and BDNA

Importantly, the results confirm that even 3¢ deoxy 2¢,5¢

DNA supports duplex formation only in the presence of distinct slide (‡)1.6 A˚) and X-displacement (‡ )2.5 A˚) for base pairs, and hence does not favor an ideal BDNA topology characterized by their near-zero values Such restrictions on base pair movements in 2¢,5¢ DNA, which are clearly absent in 3¢,5¢ DNA, are expected to impose con-straints on its ability for deformability of the kind observed

in DNA during its compaction and interaction with proteins

It is therefore conceivable that selection pressure relating to the optimization of topological features might have been a factor in the rejection of 2¢,5¢ links in preference to 3¢,5¢ links Keywords: structure of 2¢,5¢ DNA; evolution of 3¢,5¢ vs 2¢,5¢ links in nucleic acids; AB hybrid structure; restrained base pair movements; topological restrictions in 2¢,5¢ DNA

Nature’s selection of 3¢,5¢ linkages (instead of 2¢,5¢ linkages)

in nucleic acids, to encode genetic information, is intriguing

The fact that 2¢,5¢ links are formed in abundance and serve

as a template in nonenzymatic reactions suggest that they

might have been the ancestors of the biotic 3¢,5¢ links, which

could have evolved from a pool of 3¢,5¢ and 2¢,5¢ links [1]

Nucleic acids with 2¢,5¢ links satisfy one of the critical

features required for the fidelity of replication, namely that

they associate to form Watson and Crick base-paired

duplex structures [2–5], although with weaker affinity than

3¢,5¢-linked DNA strands However, detailed knowledge

about stereochemistry, polymorphism and topological

properties of 2¢,5¢ DNA duplexes, which may provide

insights into the factors that determine nature’s choice of

sugar-phosphate links from a stereochemical perspective, is

sparse [6–9] In fact, there are only two reports of NMR

structure determination – one on a 2¢,5¢ DNA fragment [10]

and one on a 2¢,5¢ RNA fragment [11] – both of which

suggest an A-type duplex structure with some

stereochem-ical details that differ from genomic DNA and RNA

duplexes In this context, it is relevant to recognize the results from recent modeling studies on 2¢,5¢ nucleic acids, which suggest that 2¢,5¢ DNA cannot form a 10-fold BDNA-like duplex (like 3¢,5¢ DNA) without the mandatory slide (‡)1.6 A˚) and X-displacement (‡ )2.5 A˚) [9] With a view to probe further into the structural properties of 2¢,5¢ DNA, we report here a high-resolution NMR study of the 2¢,5¢ DNA fragment that possesses a guanine tract followed

by a cytosine tract, to discern also possible sequence effects The results show that iso d(GGGGCCCC) [d(G4C4)] assumes a duplex that conforms to neither a canonical BDNA nor an ADNA family, but a duplex characterized

by features of both A and BDNA Possible implications

of this on the topological restrictions of 2¢,5¢ DNA, and its rejection by nature, are discussed

Materials and methods

DNA synthesis and NMR sample preparation The 2¢,5¢-linked 3¢ deoxy (GGGGCCCC) (iso DNA), was synthesized at 1 lmol scale on an in-house Applied Biosystem 391 automatic DNA synthesizer using solid-state phosphoramidite chemistry [12] The universal support (purchased from BioGene) was used as the solid support for the synthesis The standard concentration of phospho-ramidite was diluted with an equal volume of acetonitrile The products were cleaved off the column with 5 mL of 37% ammonium hydroxide containing 5% LiCl The

Correspondence to N Yathindra, Department of Crystallography and

Biophysics, University of Madras, Guindy Campus, Chennai-600 025,

India Fax: + 91 44 2230 0122,

2 Tel.: + 91 44 2235 1367,

E-mail: ny@vsnl.com

Abbreviations: d(G 4 C 4 ), d(GGGGCCCC); LALS, linked atom least

squares; RDC, residual dipolar couplings.

(Received 4 March 2004, revised 30 April 2004, accepted 21 May 2004)

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solution was incubated in a 55C water bath for 16 h and

then lyophilized The pellet from lyophilization was

dis-solved in 5% NaHCO3and purified by FPLC The collected

peak elution was lyophilized and the sample stored at

)20 C NMR samples (0.6 mM) of the 2¢,5¢ DNA fragment

were prepared in 20 mM potassium phosphate buffer

containing 0.5 mM EDTA and 100 mM KCl For

experi-ments in D2O, the samples were lyophilized and redissolved

in D2O UV melting studies show that the Tmof iso d(G4C4)

is 32 C under identical buffer conditions

NMR data acquisition

NMR experiments were carried out on a 600 MHz Varian

Unity-plus spectrometer 1D spectra in H2O were recorded

using the jump-and-return pulse sequence for H2O

sup-pression at different temperatures in the range of 2–45C

[13] 2D NOESY spectra in H2O were recorded at 2C with

mixing times of 80 ms and 300 ms Phase-sensitive NOESY

spectra in D2O [14] were recorded with mixing times of 70,

120, 150, 200, 250 and 300 ms; and TOCSY spectra [15]

were recorded with mixing times of 30 and 90 ms at 2C

The DQF-COSY spectrum [16,17] and 2D J-resolved

spectra [18] were recorded in D2O for 1H–1H coupling

constant estimation For the various experiments, the time

domain data consisted of 2048 complex points in t2 and

300–400 complex points in t1 dimension The relaxation

time delay was between 1 and 3 s for the different 2D

experiments

Experimental restraints

Data processing and analysis were carried out usingVNMR

andFELIXpackages [19] on a Silicon graphics work station

Based on the relative intensities and build-up, the cross

peaks in the NOESY spectra (obtained in D2O at various

mixing times), are classified as strong, medium-strong,

medium, and weak, and the interproton distances are

restrained, respectively, to the ranges 2–3 A˚, 2.5–3.5 A˚,

3–4.5 A˚, and 3.5–5.5 A˚ The narrow bounds are mostly

used for strong intranucleotide cross peaks, for which

distance ranges are small and known As the distance ranges

for the observable NOEs are not so large, the NOE distance

bounds used are considered to be realistic The interproton

distances involving the exchangeable protons in the H2O

NOESY spectra are restrained to the ranges 2–4 A˚ and 3.5–

5.5 A˚, corresponding to the strong and weak cross peaks,

respectively At this level of NOE intensity quantification,

spin diffusion is not expected to influence the distance

restraints to a significant extent Even so, the larger the

number of distance restraints, the better it is for internal

consistency, and the structures derived would be more

reliable A total of 162 NOE restraints were collected, of

which 115 were intranucleotide and 47 internucleotide NOEs

Base (H8/H6) sugar proton NOEs, especially to the H1¢, also enable deriving constraints on the glycosyl torsion angles The H8/H6–H1¢ distance is very short ( 2.3–2.5 A˚) for a syn conformation and relatively much longer ( 3.5– 4.0 A˚) for an anti conformation Thus, the H8/H6–H1¢ NOE will be very strong, even at short mixing times (such as 60–70 ms) if the glycosyl torsion angle is in the syn domain, whereas, under the same conditions, the peak will be nearly absent for an anti conformation We observe that G1 has a synconformation, while all others are in the anti domain (spectra presented in Results)

The 2D J-resolved spectra provides precise values of the J(H1¢–H2¢) coupling constants (Table 1) The observed coupling constants are very small, indicating that the sugar geometry belongs largely to the N domain (in the N domain this coupling constant is near 0–2 Hz, whereas it varies between 9 and 10 Hz in the S domain) A common practice is to consider the sugar geometry as an equilib-rium mixture of N and S types, and the coupling constants as weighted averages However, there are also reports in the literature [18] where the sugar ring is believed to be rigid, and is primarily of a single type, at least in the interior of the duplex In the present case, we observe that the terminal residues, for example, C8 and G2, where one would have expected greater dynamism, exhibit very small values ( 1.5Hz) for J(H1¢–H2¢) If one considers an equilibrium model, for a 10% contribution of the S domain, the contribution to the coupling constant would be around 1 Hz Moreover, it is clear from the steepness of the curve displaying the dependence of coupling constants on pseudorotation phase angle P (Fig 1), that the P range in the N domain is not going

to be very different regardless of whether the S contribu-tion is explicitly considered Thus, from the small values

of the coupling constants for the terminal residues, it is evident that the sugar geometries are dominantly in the N domain only This will be also true for the internal residues Now, in the N domain, especially in the P range 30–80, the dependence of H1¢–H2¢ coupling on P is very steep and this significantly narrows the range of permis-sible P-values for a given coupling constant value [18,20] Taking these factors into consideration, sugar puckers were restrained to the P ranges indicated in Table 1 and these were then converted to respective dihedral angle ranges in the sugar rings

The hydrogen bond restraints were given as two distances per hydrogen bond (a total of 36 restraints) for the central hexamer (see below) Based on the observation that the peak count for the duplex is the same as expected from a single strand in the various spectral data (indicating that the duplex is highly symmetric and the two strands are

Table 1 J(H1¢–H2¢) coupling and the corresponding ranges of phase angle of pseudorotation (P°).

Range of phase angle

of pseudorotation (P)

49–58 35–47 55–64 49–58 57–66 37–48 68–77 33–45

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equivalent), NCS restraints were imposed to obtain

sym-metry between the two strands forming the duplex

Structure calculation

Structure calculation of the iso d(GGGGCCCC) was

carried out using X-PLOR 3.8.5 [21] The topology and

parameter files were appropriately modified to handle 2¢,5¢

linkages to obtain optimum geometry at the 2¢,5¢

phospho-diester linkage Ideal A- and B-type duplex models for iso

DNA (possessing helical parameters identical to those of the

canonical ADNA and BDNA), obtained previously [9]

using the linked atom least squares (LALS) refinement

approach [22], were used as the starting models for structure

calculation This is justified considering that the NMR

spectra in water clearly establish Watson and Crick base

pair formation between antiparallel strands The model iso

ADNA duplex is characterized by the same value of slide,

X-displacement and the helical parameters, as ADNA On

the other hand, the iso BDNA model, while possessing the

same helical parameters as BDNA, is distinguished by a

nonzero slide (‡)1.7 A˚) and X-displacement (‡ )2.5 A˚), in

sharp contrast to the ideal BDNA that is characterized by

zero values for them Nonzero slide and X-displacement are

found to be mandatory to generate a 10-fold 2¢,5¢ duplex,

even with 3¢ deoxy sugars [9] Thus, the iso BDNA and iso

ADNA models are very different from each other, and

choosing these two as initial models removes any starting

model bias in the results of calculation Such a strategy also

saves computational efforts compared to starting the

calculation from a completely extended structure In the

latter case, much effort is expended for the formation of

the base pair itself

Syn conformation was imposed for the 5¢ end guanine

(see below) The initial model was subjected to restrained

energy minimization using the conjugate gradient algorithm

and was guided by the experimental NOE distance restraints

as well as dihedral restraints A conformational search was

performed on the octamer duplex using the simulated

annealing protocol [23], followed by structure refinement

using the gentle refine protocol ofX-PLOR3.8.5 A distance-dependent dielectric constant was used throughout the structure calculation to mimic the presence of high dielectric solvent, typically for simulating water (when explicit water is not used) The starting structure was heated to 1000 K, and sets of 100 structures that are significantly different from one another were extracted during high-temperature dynamics Each of the structures was subjected to 18 ps of high-temperature dynamics followed by slow cooling to

100 K, at steps of 50 K During each cooling step the structures were subjected to 500 fs of molecular dynamics Finally, the structures were energy minimized using the conjugate gradient algorithm This was followed by a refinement using the gentle refine protocol, where each of the structures was subjected to 20 ps of molecular dynamics

at 300 K Average coordinates over the last 10 ps of molecular dynamics simulation were computed and then refined by conjugate gradient minimization The NOE distance restraints, hydrogen bond restraints (given as two distances per hydrogen bond), and dihedral restraints on the sugar conformation were applied throughout the entire calculation with force constants of 50 kcalÆmol)1ÆA˚ )2,

100 kcalÆmol)1ÆA˚)2 and 300 kcalÆmol)1ÆA˚)2, respectively NCS restraints with a force constant of 300 kcalÆmol)1ÆA˚)2 were imposed to obtain symmetry between the two strands

of the duplex

Results

1D and 2D proton spectra The 1D1H NMR spectrum (Fig 2A) of the octamer iso d(GGGGCCCC) displays three peaks corresponding to the imino protons at 13.25 (G4), 12.80 (G2) and 12.70 (G3) p.p.m., expected from Watson and Crick base pairs in

an antiparallel duplex Sequence-specific assignments for the exchangeable and nonexchangeable protons were made from the NOESY and TOCSY spectra following the procedures developed for 3¢,5¢ duplexes [24] The observa-tion of NOE changes from G imino to C amino protons of nonterminal base pairs in the NOESY water spectra (Fig 2B) further substantiates the formation of Watson and Crick base pairing between G and C The uninterrupted self and sequential connectivity from H8/H6 to H1¢ (Fig 3A), as well as H8/H6 to H2¢ (Fig 3B) in the NOESY spectra suggest a right-handed helical structure These sequential connectivities are consistent throughout the various regions of the spectra From the temperature dependence of the G imino resonances in 1D spectra in

H2O (data not shown), the melting temperature of the duplex was seen to be 30 C

Tables 2 and 3

3 show the chemical shift values for all the assigned sugar and base protons The stereospecific assign-ments involving the 3¢ and 3¢¢ protons were based on the 2¢)3¢ and 2¢)3¢¢ NOE intensities in the 70 ms NOESY spectrum As the H2¢–H3¢ proton separation is shorter than the H2¢–H3¢¢ separation, irrespective of the sugar confor-mation, the H2¢–H3¢ NOE intensity should be stronger at shorter mixing times The relative intensities of the cross-peaks of the interproton base to sugar NOEs in the NOESY spectrum (Fig 3C), at mixing times varying from 70 to

300 ms, indicate that the 5¢-terminal guanine exists in the

Fig 1 Plots showing the dependence of the 3-bond coupling constants

(J) on the phase angle of pseudorotation (P).

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synconformation, while other bases favor the anti confor-mation This is a recurring feature found in 2¢,5¢-linked dimers [25–27] and oligomers [10,11] In the crystal struc-tures of 2¢,5¢-linked dinucleoside monophosphates, the syn conformation is stabilized by an intramolecular hydrogen

Fig 2 NMR spectra and the NOESY spectrum (A) 1D H 2 O

exchangeable NMR spectra of iso d(GGGGCCCC) in 100 m M KCl,

pH 7.0, and at 2 C, showing the imino and amino proton signals (B)

Selected region of the NOESY spectrum (mixing time 300 ms) in H 2 O

solution showing NOE correlations from G imino to C amino protons.

CNH 2(i) and CNH 2(e) refer to the internal (H-bonded) and external

(free) amino protons of the cytosine base.

Fig 3 (H8/H6)–H1¢ cross-peak region of a 300 ms 2D NOESY spectrum of iso d(GGGGCCCC) in D 2 O solution at 2 °C, showing the uninterrupted sequential connectivities from (A) (H8/H6) to H1¢ protons (B) (H8/H6) to H2¢ protons (C) Stacked plot of the H8/H6 to H1¢ region showing a high intensity for the H8–H1¢ cross-peak of G1, suggesting syn glycosyl conformation for the terminal G1 residue.

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bond between the purine N3 and O5¢H of the sugar residue,

besides sugar O4¢–base (syn) base interaction [9,25–27]

The (H1¢–H2¢) coupling constants derived from 2D

J-resolved spectra clearly indicate that all of the 3¢ deoxy

sugars belong to the N type, except for C7 which has a

slightly higher coupling constant (5.1 Hz)

Structural features of 2¢,5¢ d(GGGGCCCC)

The 3D structure of 2¢,5¢ d(GGGGCCCC) was obtained by

simulated annealing molecular dynamics usingX-PLOR3.8.5

[21] Experimental restraints and structure convergence

parameters are listed in Table 4 The convergent structures

are clustered into families: BFI (Fig 4A) with 39 structures,

and BFII (Fig 4B) with 20 structures when the starting

model was ideally iso BDNA; and AFI (Fig 4C) with 85

structures and AFII (Fig 4D) with 15 structures when the

starting model was iso ADNA Structures represented

by BFI and AFI families (FI) differ considerably in their

overall topologies from the structures represented by BFII

and AFII families (FII) The root mean square

devi-ation (rmsd) between FI and FII is greater than 3 A˚, while

it is less than 1 A˚ for structures within FI or FII The

structures were selected using standard criteria on the basis

of proper covalent geometry, the least number of distance

and dihedral violations, symmetry and low energy

The duplex model AFI (Fig 5A), closely resembles BFI

(Fig 5B) The rmsd between the average structure of AFI

(Fig 5A) and BFI (Fig 5B) is 0.8 A˚ Thus, in spite of the

large rmsd (> 4 A˚) in the starting structures, the final

structures fall into similar families, indicating that the

structures are not biased by the choice of the initial model

This also indicates that the experimental restraints are

sufficient and consistent to define good convergent struc-tures In view of this, it is believed that there is no need for any further refinements using residual dipolar couplings (RDCs), as often performed in longer DNA stretches [28–30] Likewise, we also did not feel the need for any relaxation matrix refinement, which takes into account spin diffusion explicitly, which may be required if the NOE data set is very small At the same time, relaxation matrix refinement puts a greater demand on the accuracy of NOE quantification

In the final structures, the terminal GC pairs are not well defined owing to insufficient NOEs Hence, structural features manifested in the central hexamer of iso d(G4C4), corresponding to the GGGCCC duplex in the family AFI, which has the highest population of converged structures and also has very good convergence, are considered for detailed discussion

Calculated values of X-displacement and slide for the base pairs in AFI are given in Table 5 Average values of X-displacement and slide of GC base pairs at the GG step (Fig 5A) are)3.25 A˚ and )1.62 A˚ (Table 5), respectively

On the other hand, slide for the GC pair at the GC step that links the G stretch with the C stretch is rather high ()3.32 A˚)

The nature of the base stacking interaction in the iso d(GGGGCCCC) duplex, as seen in AFI, is shown in Fig 6A Stacking at the G2G3 and G3G4 steps involves overlap of the six-membered ring of one guanine with the imidazole ring of the adjacent guanine, while there is only

Table 3 Chemical shifts (p.p.m) for iso d(GGGGCCCC) 2

exchange-able protons.

Base H 1 H 22 /H 42 (e) H 21 /H 41 (i)

Table 2 Chemical shifts (p.p.m) for iso d(GGGGCCCC) 2

non-exchangeable protons.

Residue H6/H8 H1¢ H2¢ H3¢ H3¢¢ H4¢ H5¢/H5¢¢ H5

G1 7.97 5.98 5.18 2.53 2.37 4.58 3.88,3.69 –

G2 7.78 5.83 4.7 2.45 2.31 4.61 4.18,4.08 –

G3 7.62 5.96 4.91 2.56 2.48 4.78 4.51,4.14 –

G4 7.58 5.99 4.61 2.48 2.38 4.77 – –

C5 7.5 6.08 4.62 2.44 – 4.76 4.39,4.07 5.10

C6 7.88 5.94 4.5 2.31 – 4.71 4.10 5.48

C7 7.73 6.03 4.66 2.49 2.31 4.04 4.27 5.52

C8 7.84 5.66 4.26 1.84 1.82 4.56 4.39,4.0 5.61

Table 4 NMR restraints for iso d(GGGGCCCC) 2 NOE distance restraints (per strand)

Non-exchangeable NOE restraints 140 Exchangeable NOE restraints 22 Total restraints 162

Sugar dihedral restraints (per strand) 40 Hydrogen bond restraints 36 BFI (model obtained when iso BDNA is used as the starting duplex) Number of convergent structures 39

rmsd from the average structure 0.5 A˚ )1.0 A˚ NOE violation > 0.2 A˚ 1

Dihedral angle violation > 5 Nil BFII (model obtained when iso BDNA is used as the starting duplex) Number of convergent structures 20

rmsd from the average structure 0.3 A˚ )1.0 A˚ NOE violation > 0.2 A˚ 1

Dihedral angle violation > 5 Nil AFI (model obtained when ADNA is used as the starting duplex) Number of convergent structures 85

rmsd from the average structure 0.1 A˚ )0.6 A˚ NOE violation > 0.2 A˚ 1

Dihedral angle violation > 5 Nil AFII (model obtained when ADNA is used as the starting duplex) Number of convergent structures 15

rmsd from the average structure 0.1 A˚ )0.5 A˚ NOE violation > 0.2 A˚ 1

Dihedral angle violation > 5 Nil

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minimal stacking between cytosines Likewise, stacking at

the GC step, which links the G stretch with the C stretch, is

minimal owing to a larger slide ()3.32 A˚) Superposition of

the base pairs of the (GGGCCC)2 fragment of the iso

d(G4C4) duplex with the ideal iso BDNA (Fig 7),

demon-strates a strong resemblance in the stacking patterns

An estimate of the dimensions of major and minor

grooves is obtained by generating a 12mer duplex using the

central hexamer of the average structure (AFI) as the repeat

using the programFREEHELIX[31] The groove topologies of

AFI show significantly different features from the ideal

duplex models The major groove is wide (17 A˚), while its

minor groove is narrow (10.3 A˚)

The 3¢ deoxy sugars in iso d(G4C4) favor N-type pucker,

corresponding to the C4¢ exo conformational domain (P ¼

38–64), except in the residue C7, which favors C4¢ exo/O4¢

endo pucker, corresponding to P¼ 54–90 (Table 1) in

AFI In any case, none of the sugars shows a tendency for

S-type sugar conformation

Base pairs in AFI are slightly overwound, and the duplex

has 9 bp per turn, with an average helical twist of 38.4 and

a rise of 3.76 A˚ (Table 5) The average helical twist at the

GG and CC steps is 41, while it is 28 at the GC step Slight underwinding at this step is accompanied by a higher slide of)3.32 A˚ Base pairs are nearly perpendicular to the helix axis (inclination angle 3) The two central base pairs

of the duplex are practically planar and they do not exhibit significant propeller twist (Table 6), while the base pairs flanking them possess a larger value of)22 Phosphodi-ester conformations at all the GG steps, as well as at the GC step, conform to the (g–,g–) domain, while they correspond

to the (t,g–) at the CC steps (Table 7)

Discussion

It is now well established that nucleic acids, even with 2¢,5¢ linkages, associate to form Watson and Crick paired duplexes [2–5,10,11,32–37] They also selectively associate with DNA and RNA with a varying degree of stability Interestingly, it has been shown recently that 2¢,5¢ RNA fragments form even hairpins with a stability comparable to RNA hairpins [38] In an effort to obtain a comprehensive understanding of the stereochemistry that govern the structures of 2¢,5¢ nucleic acids, we recently reported the

Fig 5 Stereo plot of the average structure of iso d (G 4 C 4 ) (A) AFI and (B) BFI.

Fig 4 Stereo plot of the families of converged structures of iso

d(GGGGCCCC) 2 (A) BFI (39 structures), (B) BFII (20 structures),

(C) AFI (85 structures), and (D) AFII (15 structures).

Table 5 Base-step parameters in the average structure (AFI) of the iso d(GGGGCCCC) duplex.

Base step Slide (A˚) X-disp (A˚) Twist () Rise (A˚) G2-G3 )1.53 )3.36 42.3 3.68 G3-G4 )1.71 )3.13 39.67 3.61 G4-C5 )3.32 )3.19 28.02 4.23 C5-C6 )1.71 )3.13 39.63 3.61 C6-C7 )1.53 )3.23 42.37 3.68 Average )1.96 )3.20 38.39 3.76

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NMR structure of a 2¢,5¢ RNA fragment [11] that exhibited

interesting features which supported our predictions from

modeling studies [8,9] We report here the results of

high-resolution NMR structure of a 2¢,5¢-linked DNA fragment

d(GGGGCCCC)

The structural model, AFI, that emerged from NOE

and other NMR data, exhibit slide ()1.96 A˚) and

intermediate X-displacement ()3.32 A˚) for the base pairs,

a feature normally seen only in ADNA duplexes

However, the magnitude of X-displacement observed here

is lower () 4.7 A˚) than that found in ADNA

Interest-ingly, the slide ()3.32 A˚) at the lone GC step, linking the

G stretch with the C stretch, is found to be nearly twice

that found at the GG steps ()1.62 A˚), indicating possible

sequence effects A comparison of the stacking pattern

observed at the GG steps of the present structure with those in ideal ADNA, iso ADNA and iso BDNA duplexes (Fig 6B) brings out a strong similarity It is interesting that the similarity in stacking persists, notwith-standing different values for X displacement that charac-terizes these duplexes (Table 5) However, it should be noted that all of them possess nearly the same slide ()1.7 A˚) Thus, the base stacking pattern in iso d(G4C4) is like that in ADNA, except at the GC step where a large slide causes adjacent bases to move away, resulting in minimal overlap between them

Another unusual feature is the predominance of N-type pucker in nearly all the 3¢ deoxy sugars in 2¢,5¢ d(G4C4) This is in sharp contrast to the S-type puckers preferred

by 2¢ deoxy sugars in DNA duplexes This has been

Fig 6 Base stacking at different steps in the AFI duplex of iso (G 4 C 4 ) and the GG steps of iso BDNA: iso ADNA and ADNA Note the identical base stacking at the GG steps of AFI and ideal duplexes Figures were drawn using 3 DNA v1.5 [47].

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anticipated in view of certain stereochemical arguments

[8,9] Exclusive preference for the N-type sugar puckers

has, in fact, been indicated by the early NMR studies on

2¢,5¢-AAA [39] and crystal structures of 3¢

deoxynucleo-sides [25–27] Such preference for N-type pucker has also

been confirmed by recent1H NMR analysis on a number

of 3¢ deoxynucleosides and stereo-electronic arguments

[40,41] Unconstrained molecular dynamics simulations of

a 2¢,5¢ DNA duplex, lasting a few nanoseconds, have also

demonstrated the retention of N-type pucker for the sugar

[42] It should be recognized at this juncture that the

consequence of N-type sugar pucker is to render the

preferred nucleotide conformation to be extended in 2¢,5¢

DNA and compact in 3¢,5¢ DNA [8,9] It is well known

that the extended nucleotide repeats lead to an extended

BDNA, and the compact nucleotide repeat leads to a

compact ADNA type of duplexes (Fig 8) The 2¢,5¢ DNA

fragment d(G4C4) is thus composed of extended

nucleo-tide repeats that are normally part of BDNA but with a

distinct X-displacement, slide and base stacking like in ADNA Thus, the duplex model AFI of 2¢,5¢ d(G4C4), possesses composite features of both A and BDNA In view of these, it is perhaps appropriate to regard the structure of iso d(G4C4) as a hybrid structure of A and B forms

It is gratifying that the more populated AFI family of iso d(G4C4) resembles the ideal iso BDNA-like duplex [9], which is also characterized by similar values of slide, intermediate displacement, base stacking pattern and extended nucleotide repeat formed out of N-type sugar puckers (Table 5) Furthermore, the overall groove topol-ogies of iso d(G4C4) resemble BDNA, with the widths of the major groove and the minor groove having values of 17 A˚ and 10.3 A˚, respectively (Table 8)

It has been demonstrated from modeling investigations that 2¢,5¢ isomers, even with 3¢ deoxyriboses, cannot form duplexes without base pair displacements [9] Results of CD and FTIR investigations on iso DNA fragments comprising

a variety of base sequences also seem to converge to suggest that they favor A-type rather than B-type duplexes (S Raja

& N Yathindra, unpublished observation) Furthermore, it has been found [43] that iso d(CGCGCG) does not associate

to form left-handed ZDNA This has been attributed to the inaccessibility [42] to form the well-known water-mediated hydrogen bond stabilization interaction between the amino group of the syn guanine and the anion oxygen of the phosphate group [44] These clearly point to the constraint

on the range of duplex helical structures possible for nucleic acids with 2¢,5¢ linkages

The lateral slide of the sugar-phosphate chain from the periphery (as in 3¢,5¢ links) towards the helix interior in

Fig 7 Superposition of the G 3 C 3 fragment of

AFI with ideal iso BDNA Root mean square

deviation with respect to base pairs is 0.6 A˚.

Table 6 Propeller twist (°) of base pairs in the average structure (AFI)

of the iso d(GGGGCCCC) duplex.

Base pair Propeller twist ()

Table 7 Conformation angles (°) in the average structure (AFI) of the iso d(GGGGCCCC) 2 duplex.

Residue

a (P-O5¢)

b (O5¢-C5)

c (C4¢-C5¢)

n (C2¢-O2¢)

f (P-O2¢)

v

(C1¢-N) P

Trang 9

2¢,5¢ nucleic acids causes the base pairs to slide, resulting in

the intrinsic requirement of slide, and hence

X-displace-ment, that manifest in all 2¢,5¢ nucleic acid duplexes This

limits the access to a lower range of values of both slide

(<)1.5 A˚) and X-displacement (< )2.5 A˚) in 2¢,5¢ nucleic

acids In contrast, nucleic acids with 3¢,5¢ links have a wider

range of access for both slide (0–2.5 A˚) and X-displacement

(0–4.7 A˚) that includes ranges forbidden for the 2¢,5¢ isomer This enables 3¢,5¢-linked nucleic acids to assume a variety of duplexes with distinct topological features and also afford other capabilities, such as bending, kinking and curvature, which form the basis for nucleic acid compaction and specificity of interaction with proteins It is therefore anticipated that the restricting factors in 2¢,5¢ nucleic acids,

Fig 8 Shape and dimension (adjacent P–P separations) of the repeating nucleotide units in 2¢,5¢- and 3¢,5¢-linked nucleic acids An equatorial (e) link renders the adjacent phosphates to be proximal, leading to a compact nucleotide (P–P  5.9 A˚), while an axial (a) link renders them to be distal, leading to an extended nucleotide (P–P  7.0 A˚).

Table 8 Comparison of structural features of the iso d(GGGGCCCC) 2 duplex (AFI) with the ideal A and B types of duplexes formed by 3¢,5¢ and 2¢,5¢ links.

Features/parameters BDNA ADNA iso BDNA iso ADNA AFI

Sugar pucker S type N type N type S type N type

C2¢endo C3¢endo C3¢endo C2¢endo C4¢exo

Trang 10

which are mentioned above, probably impose additional

constraints limiting these capabilities Also, it has been

shown from modeling consideration that the lateral slide

of the sugar-phosphate chain leads to overwinding of the

2¢,5¢-linked single-stranded helix to enhance the adjacent

base–base or sugar–base stabilizing interactions [9,42,45]

Tighter winding of the 2¢,5¢ single-stranded DNA helix,

compared with 3¢,5¢ DNA, probably offers restrictions to

the folding abilities of even single-stranded 2¢,5¢ DNA

Hence, it may be argued that topological restrictions

inherent to the 2¢,5¢-linked helical duplexes might have also

contributed towards their rejection It is worth mentioning

that the inherent low thermal stability of 2¢,5¢ links might

have been another factor involved in nature’s selection of

the 3¢,5¢ links Thus, optimization of the topology of duplex

helix, besides the optimization of base pair stability [46],

must have been important in the chemical etiology of

nucleic acid structures

Conclusions

Systematic investigations of 2¢,5¢ nucleic acids have provided

new perspectives on the stereochemical details pertaining to

their ability, or lack of it, to form duplex structures akin to

their naturally occurring 3¢,5¢ isomers In parallel to our

finding [8,9] of the critical features that distinguish the

shapes and dimensions of the repeating nucleotides of 3¢,5¢

and 2¢,5¢ isomers, we have provided structural details of an

isoRNA [11] and an iso DNA duplex fragment (present

work) from NMR studies Together, these should provide a

structural basis for understanding much of the experimental

data from solution studies concerning the associations of

2¢,5¢ nucleic acids and also with DNA and RNA

Compar-ison of the structure deduced for iso d(GGGGCCCC), from

the current study, and that of iso d(CGGCGCCG) [10]

suggest that even 2¢,5¢ DNAs are prone to sequence effects,

as evidenced by some differences seen in structures of the

two sequences The former sequence assumes a hybrid

structure of A and BDNA duplexes, while the latter assumes

an ADNA-like duplex with mixed C2¢ endo and C3¢ endo

sugar puckers for the central hexamer The fact that both

these sequences, studied by NMR, point to a non-BDNA

duplex structure, suggest a constrained nature of base pair

movements in 2¢,5¢ nucleic acids vis-a`-vis their 3¢,5¢ isomers

This is in complete conformity with the modeling studies

[8,9] which indicate that slide and X-displacement of base

pairs lower than )1.7 A˚ and )2.5 A˚, respectively, are

inaccessible owing to the inherent chemistry of the

2¢,5¢-linked sugar-phosphate backbone It seems, then, that a

need for greater topological flexibility of DNA helices might

have had a bearing on the selection of 3¢,5¢ links over 2¢,5¢

links during the course of evolution

Acknowledgements

NMR and computational facilities, provided by the National Facility

for High Resolution NMR at the Tata Institute of Fundamental

Research, Mumbai, are gratefully acknowledged N.Y and B.J.P.

thank DST and CSIR for a research grant and senior fellowship,

respectively S.R thanks CSIR for a Senior Research Fellowship UGC

and DST are thanked for the financial support to the Department

under DSA (UGC) and FIST (DST) programs.

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