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The solution structure reveals an a helix bent in the same direction as the more bent conformer of the published crystal structure of TTTT, while the side chain v1rotamers of VVVV2KE are

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Solution structure of a hydrophobic analogue of the winter flounder antifreeze protein

Edvards Liepinsh1, Gottfried Otting1, Margaret M Harding2, Leanne G Ward2, Joel P Mackay3

and A D J Haymet4

1

Karolinska Institute, Tomtebodava¨gen, Stockholm, Sweden;2School of Chemistry, University of Sydney, NSW, Australia;

3

Department of Biochemistry, University of Sydney, NSW, Australia;4Department of Chemistry and Institute for Molecular Design, University of Houston, TX, USA

The solution structure of a synthetic mutant type I antifreeze

protein (AFP I) was determined in aqueous solution at

pH7.0 using nuclear magnetic resonance (NMR)

spectro-scopy The mutations comprised the replacement of the four

Thr residues by Val and the introduction of two additional

Lys-Glu salt bridges The antifreeze activity of this mutant

peptide, VVVV2KE, has been previously shown to be

sim-ilar to that of the wild type protein, HPLC6 (defined here as

TTTT) The solution structure reveals an a helix bent in the

same direction as the more bent conformer of the published

crystal structure of TTTT, while the side chain v1rotamers of

VVVV2KE are similar to those of the straighter conformer

in the crystal of TTTT The Val side chains of VVVV2KE

assume the same orientations as the Thr side chains of TTTT, confirming the conservative nature of this mutation The combined data suggest that AFP I undergoes an equi-librium between straight and bent helices in solution, com-bined with independent equilibria between different side chain rotamers for some of the amino acid residues The present study presents the first complete sequence-specific resonance assignments and the first complete solution structure determination by NMR of any AFP I protein Keywords: antifreeze; a helices; proteins; winter flounder; NMR spectroscopy

During the last two decades, at least four classes of

structurally diverse antifreeze or thermal hysteresis proteins

(type I–IV AFPs) have been isolated from the serum of cold

water fish (for reviews see [1–6]) These compounds have in

common the ability to lower the freezing point of blood

serum, thus allowing fish to survive in subzero ocean

temperatures While some progress has been made in the

structural characterization of these proteins [7–10], the exact

mechanism by which they are able to inhibit ice growth is

not fully understood

Most studies have focused on the type I antifreeze

proteins [5], which are structurally the simplest members of

the AFPs Fourteen type I proteins have been identified

from the right-eye flounders and sculpins [5], and these

proteins are characterized by being low Mr, alanine rich,

a helical structures Within this class, HPLC6 (TTTT) [11], a

37-residue sequence containing three 11-residue repeats of

ThrX2AsxX7is by far the most extensively studied protein

and is the only type I AFP for which a solid state structure

has been reported Single X-ray diffraction [8,12] showed

that in the solid state this protein is completely a helical in

conformation with the exception of the last unit, which

adopts a 310-helix conformation The protein has also been studied by NMR spectroscopy [13] but due to the high number of alanine residues in the sequence, which led to significant spectral overlap, full resonance assignments were not possible These studies confirmed the global helical conformation of the peptide and allowed the rotamer conformations of a number of residues to be determined, but clear evidence for the presence of helix-stabilizing interactions arising from the capping motifs observed in the crystal structure was not obtained More recently, meas-urements of chemical shifts and rotational correlation times

of TTTT in supercooled water [14] showed no evidence for any structural change in the protein at temperatures below the freezing point

Structure–activity studies on TTTT, summarized previ-ously [5], have identified the importance of the Thr residues

at positions 2, 13, 24 and 37 (highlighted in bold in the sequence in Table 1), plus surrounding residues, for ice growth inhibition activity While the Thr residues were assumed to be involved in hydrogen-bonding interactions with ice for many years [15–18], more recent mutations [19–23] have identified the hydrophobicity provided by the c-methyl group of Thr, in addition to hydrogen bonding involving other residues, as a key factor related to the ability

to inhibit ice growth However, a plausible model that explains the selective interaction of TTTT with the [2 0 22 1] plane [15] has not emerged (for a full description of the different ice interfaces, see [5]) Recent computational studies on the nature of the ice/water interface have allowed the first real simulations of the interaction of TTTT with the fluid interface to be carried out [24] These studies support experimental data on mutants [19–23] that have shown that

Correspondence to M M Harding, School of Chemistry, F11,

Uni-versity of Sydney, N.S.W 2006, Australia Fax: + 61 29351 6650,

Tel.: + 61 29351 2745, E-mail: harding@chem.usyd.edu.au

Abbreviations: AFP I, type I antifreeze protein; NMR, nuclear

magnetic resonance; TTTT, HPLC6 polypeptide; NOE, nuclear

Overhauser effect; AU, analytical ultracentrifugation.

(Received 28 September 2001, revised 21 December 2001, accepted

7 January 2002)

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hydrogen bonds involving the hydroxyl groups of the four

Thr residues is not the primary reason for the interaction of

TTTT with the ice/water interfacial region

We have recently designed and synthesized analogues of

TTTT in which the relative size, hydrophobicity and

hydrogen bonding characteristics of the side chains at

positions 2, 13, 24 and 37 were systematically varied [21,22]

Four additional charged residues K7, E11, K29 and E33

(italicized in the VVVV2KE sequence shown in Table 1)

were incorporated into the sequence to improve solubility

and minimize aggregation The valine-substituted analogue

VVVV2KE showed similar behaviour to TTTT at low

concentrations [22] and showed conclusively that models for

the mechanism of ice growth inhibition that are dominated

by hydrogen bonding involving the Thr hydroxyls are

incorrect

This paper reports determination of the solution structure

of VVVV2KE The additional charged residues in this

sequence provided chemical shift dispersion in the

alanine-rich segments compared with TTTT and thus allowed the

first solution structure of a type I protein to be determined

Such experimental solution data are important in modelling

the interaction of these peptides with the ice/water interface,

in order to provide a mechanism for the selective interaction

of the peptide with the [2 0 22 1] ice plane, and hence to

allow the rational design of synthetic AFPs

M A T E R I A L S A N D M E T H O D S

Materials

VVVV2KE was obtained and purified as previously

described [20,22] Sample concentrations were determined

by amino-acid analysis NMR samples were prepared in

unbuffered 90% H2O/10% D2O at concentrations of

11 mM (pH4.9) and 2 mM (pH7.0) The 2-mM sample

was desalted by ultrafiltration

NMR spectroscopy, collection of conformational

restraints and structure calculation

NMR spectra were recorded on Bruker DMX-600 and

Varian Unity INOVA-800 NMR spectrometers The

NOESY spectrum used for collection of NOE distance

restraints was recorded at 10C on the 800-MHz NMR

spectrometer, using the 2-mM sample This spectrum was

recorded with a mixing time of 80 ms, using the 3-9-19

sequence for water suppression [25] In addition, NOESY,

ROESY, TOCSY and DQF-COSY spectra were recorded

using the 11-mM sample at temperatures between )8 C

and 15C to support the resonance assignment and check

for conformational differences The in-phase lineshape of

NOESY cross peaks was used to determine JHN,Hacoupling

constants [26] The COSY and TOCSY cross-peaks were

visually inspected to determine the relative magnitude of the

J couplings of CbH methylene groups The ROESY

spectrum at 15C (mixing time 50 ms) was used to identify spin-diffusion cross-peaks in the NOESY spectrum recor-ded with an 80-ms mixing time The programXEASYwas used for resonance assignments and peak integration [27] DYANA [28] and OPAL [29] were used for the structure calculations and energy minimization, respectively Stand-ard parameters were used for both programs The energy minimization was performed in a water shell of 6 A˚ Hydrogen bonds were identified by O Æ Æ Æ Hdistances

< 2.4 A˚ and internuclear O Æ Æ Æ H-N angles < 35 Plots of the structure were prepared withMOLMOL[30]

Accession numbers The coordinates of the 20 energy-refinedDYANAconformers

of VVVV2KE and the resonance assignments were depos-ited in the Protein Data Bank with the accession code 1K16 The NMR chemical shifts were deposited at the Bio-MagResBank (BMRB) under the accession code 5157

Analytical ultracentrifugation (AU) Sedimentation experiments were performed on a Beckman XL-A analytical ultracentrifuge VVVV2KE was dissolved

in 50 mMKH2PO4(pH8.0) containing 50 mMKCl, to give initial loading concentrations of 1.0, 0.3 and 0.1 mM Sample aliquots (200-lL) were loaded into 12-mm double-sector cells, and data were collected at 0C in an An-60ti rotor (45 000 and 54 000 r.p.m.) Data were acquired as absorbance vs radius scans (at 240 and 360 nm) at 0.001-cm intervals and as the sum of 10 scans Data were collected at 3-h intervals and compared to determine when the samples had reached chemical and sedimentation equilibrium After subtraction of the 360-nm scans, the data from all speeds and loading concentrations were fitted simultaneously to a number of models using the program NONLIN [31]; the quality of each fit was determined by inspection of residual plots and v2values Visualization of the plots of apparent molecular mass vs concentration andW vs concentration was carried out using the programOMMENU[32]

R E S U L T S

Analytical ultracentrifugation Figure 1 shows the results of AU experiments on VVVV2KE at three concentrations, including the fitted curves obtained using an ideal single species model The combined residuals of the fit are presented in the bottom panel of Fig 1 The derived molecular mass for the peptide shows that in the concentration range less than 1 mM, and under the conditions used for these measurements, the major species present in all cases is the monomeric peptide The peptide also appears to be monomeric at 2 mM concentration (the concentration used for NMR structure determination), as no significant chemical shift changes were

Table 1 Sequence alignment of TTTT and VVVV2KE.

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observed in the concentration range 0.1–2 mM(measured at

5C and pH3.55)

NMR spectroscopy and structure calculation

Significant spectral overlap prevented the resolution of all

cross peaks In particular, the chemical shifts of residues

Glu11 and Ala14 were practically indistinguishable from

those of Glu22 and Ala25 (Table 2) Yet, the appearance of

the 800-MHz NOESY spectrum shows that, at least for the

amide protons, the degeneracy is not complete (Fig 2A)

Sequential connectivities between amide protons can be

traced from Ala3 to Ala36 without interruption (Fig 2A),

indicating a helical conformation The spectral overlap is

more severe for the resonances of the aliphatic protons

Nevertheless, many of the nuclear Overhauser effects

(NOEs) characteristic of a helical secondary structure could

be resolved (Fig 2B)

In the case of strongly overlapping cross peaks, as

observed for example for the homologous repeats Glu11–

Ala14 and Glu22–Ala25, upper distance limit restraints

were derived using the assumption that corresponding

NOEs from the different segments contributed equally to

the overlapping cross peak intensity Similarly, the same

dihedral angle restraints were used for homologous repeats,

when the corresponding COSY cross peaks overlapped, but

their assignment was otherwise unambiguous The use of

identical restraints for homologous, spectrally unresolved

peptide segments was motivated by the observation of

similar NOEs and coupling constants, when cross peaks

between homologous repeats could be resolved

NOEs with the terminal amino-acid residues were very

weak, presumably due to increased mobility Therefore, the

set of upper distance restraints of residues 2 and 37 was

supplemented by restraints obtained from the ROESY spectrum recorded at 15C and a much higher sample concentration Furthermore, a hydrogen bond between the carboxyl group of Asp1 and the amide proton of Ser4 was indicated by the observation of a large high-field shift of this

HNresonance when the pHwas lowered to pH2 (data not shown) [33,34] This hydrogen bond seems to be highly populated at neutral pH, where the HNresonance of Ser4 is the most low-field shifted amide (Fig 2)

Solution structure of VVVV2KE The solution structure of VVVV2KE, represented by the ensemble of 20 energy-minimized DYANA conformers, consists of a bent a helix spanning the entire length of the peptide The most pronounced bend seems to occur near Lys18 While all residues were engaged in proper a helical backbone hydrogen bonds in the conformer closest to the average structure and in the conformer with the smallest residual violations, the hydrogen bond between Lys18 and Ala14 was broken in eight of the 20 NMR conformers In four of these, the carbonyl oxygen of Ala14 was hydrogen bonded to the amide proton of Ala17 instead A straight helix around Lys18 was obtained in test calculations, and a short distance restraint was artificially introduced between Ala14 Haand Lys19 HN, at the expense of an increased number of distance-restraint violations in the resulting conformers As the corresponding i/i + 4 NOE was, however, absent (Fig 2B), it was not used in the final calculations

Temperature coefficients measured for the amide-proton chemical shifts between 5 and )5 C did not show any irregularities for these lysine residues Twofold to threefold larger values than average were, however, observed for the

HNchemical shifts of Ala15 and Ala26 (0.011 p.p.m perC between 5 and)5 C) and Asn16 and Asn27 (0.015 p.p.m perC) which might reflect conformational irregularities at these locations of the a helix While local flexibility would necessarily affect the amplitude and precise direction of the helical bend calculated from NOE data, a bend of the helix seems to be a genuine feature of VVVV2KE The hydrogen bond between the side chain of Asp1 and the backbone amide of Ser4 results in the presence of an N-cap (Fig 3B) When this hydrogen bond was removed from the list of restraints, it was found only in a minority of the conformers The presence of this hydrogen bond was, however, strongly supported by the chemical shift changes observed in the pH titration and it was consequently included as a restraint The chemical shift of Ser4 HNshowed the largest temperature coefficient of all amide protons (0.017 p.p.m per C between 5 and)5 C), suggesting that this hydrogen bond

is particularly short or is readily broken at higher temper-atures In contrast, the experimental evidence for the presence of a well-defined C-cap, as in the crystal structure

of TTTT [8], was less clear Any NOEs involving the terminal residue Arg37 were weak, probably due to increased mobility, and the temperature coefficients of the chemical shifts of the C-terminal NH2group of Arg37 were too large to suggest any involvement in a stable hydrogen bond Yet, the temperature coefficients of the two NH2 protons were significantly different and smaller for the high-field shifted proton, which in the crystal structure of TTTT hydrogen bonds to the carbonyl oxygen of Thr35 [8]

Fig 1 Analytical ultracentifugation data for VVVV2KE at

concentra-tions of 1 m M (diamonds), 0.3 m M (squares) and 0.1 m M (circles) Top

panel shows fits of data to an ideal-single species model and bottom

panel shows residuals derived from this fit.

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Although no restraints were used for this NH2group in the

structure calculations of VVVV2KE, and Arg37 was largely

disordered (Fig 3B), most of the conformers formed the

corresponding hydrogen bond between Arg37 NH2 and

Val35 O

The amino-acid side-chains of VVVV2KE assumed the

same v1rotamer position in all 20 conformers, while different

rotamers were found beyond the b carbons Only the side

chain of Ser4 populated all three staggered v1rotamers

Comparison between the structures of VVVV2KE

and TTTT

The crystal structure of TTTT contains two conformers in

the unit cell that differ widely in their helical bend (Fig 4)

[8] In the following, we refer to the more bent conformer as

the b-conformer, and the less bent conformer as the

s-conformer Interestingly, the b- and s-conformers are bent in opposite directions The overall bend observed in the NMR structure of VVVV2KE is in the same direction as in the b-conformer, placing residues 2, 13, 24 and 37, that are putatively involved in ice-binding, on the concave surface The two conformers of TTTT also differ by the side chain

v1rotamers of several residues, namely Asp1, Leu12, Lys18, Leu23 and Thr35 Both conformers display the backbone hydrogen bonds expected for an a helix spanning all residues, and include elaborate terminal cap structures As with the NMR structure of VVVV2KE, the N-terminal cap structure of TTTT includes a hydrogen bond between the side chain carboxyl group of Asp1 and the backbone amide

of Ser4 The C-terminal cap structure, however, makes use

of the Arg37 side chain to form a hydrogen bond to the backbone carbonyl oxygen of Ala33 [12] No evidence of this could be obtained in solution Interestingly, the

Table 2 1 H-NMR chemical shifts of VVVV2KE at 10 °C, pH 7.0 The chemical shifts were referenced to the water signal at 4.994 p.p.m The estimated error is ± 0.01 p.p.m The chemical shift values of stereospecifically assigned protons are in italics, where the first number is the shift of the proton with the lower branch number, e.g the b 1 proton.

Residue

Chemical shift

NH 2 7.24, 7.27

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chemical shift difference between the1H-NMR resonances

of the C-terminal NH2group increased by about 0.1 p.p.m

as the temperature was lowered to)2 C (data not shown),

suggesting that a hydrogen bond between Arg37 NH2and

the carbonyl oxygen of residue 35 may be significantly

populated at low temperatures, in agreement with the

crystal structure of TTTT [8] In contrast to the crystal

structure of TTTT, where Arg37 HNis hydrogen bonded to

Ala34 O, this amide proton consistently formed a hydrogen

bond with Glu33 O in the NMR structure of VVVV2KE

This difference, however, is hardly significant, as Arg37 HN

and Glu33 O are also close in the crystal structure of TTTT

The side chain v1angles observed in the NMR structure

of VVVV2KE are very similar to those observed in the X-ray conformers of TTTT (Table 3) In particular, the side-chain orientations of the valine residues in VVVV2KE are equivalent to those of the Thr residues in TTTT; i.e the ThrfiVal mutation effectively resulted in the replacement

of the OHby a CH3group without affecting the position of the other CH3group Five residues have different rotamer positions in the two TTTT conformers Except for Asp1, the rotamers of these residues in VVVV2KE are similar to those

of the s-conformer of TTTT (Table 4) There is thus no simple correlation between helix bend and side-chain conformation

D I S C U S S I O N

The molecular mechanism whereby TTTT and other type I proteins are able to inhibit ice growth via accumulation at the specific [2 0 22 1] plane remains a continued subject of discussion in the literature [5,6,24,35–37] The first molecu-lar dynamics simulation of a complete ice/TTTT/water system, that does not restrict ice lattice positions, and includes long-range electrostatic interactions, has been reported very recently [24] This study has allowed a comparison of the hydrogen bonding between the protein in water and the protein in the ice/water interfacial region

A

B

Fig 2 Selected spectral regions from the NOESY spectrum of

VVVV2KE in 90% H 2 O/10% D 2 O at 10 °C, pH 7.0 The spectrum

was recorded at a 1 H-NMR frequency of 800 MHz, using a mixing

time of 80 ms Cross peaks are labelled with the residue numbers of the

amino acids involved The first/second number refers to the residue in

the d 1 /d 2 frequency dimension, respectively (A) Cross peaks between

backbone amide protons (B) Cross peaks between a-protons in the d 1

dimension and amide protons in the d 2 dimension i/i + 3 and i/i + 4

NOEs are identified, where i is the residue number in the amino acid

sequence A circle marks the predicted location of the NOE cross peak

between Ala14 Haand Lys18 HN, which could not be detected even at

much lower plot levels.

20

29

37

11

1

37 29 20 11

1

Fig 3 Stereo views of the solution structure of VVVV2KE (A) Super-position of the 20 conformers representing the NMR structure of VVVV2KE (left panel) and single conformer closest to the average structure (right panel) The line drawings include all heavy atoms a-Carbon positions are identified by spheres, and the location of approximately every tenth residue is labeled by its number in the amino acid sequence (B) Stereo views of the N-cap (left panel) and C-cap (right panel) in the NMR structure of VVVV2KE The backbone atoms of the first five and last six residues, respectively, were super-imposed for minimum r.m.s.d Only bonds with backbone atoms and backbone carbonyl atoms are displayed, except for the side chain of Asp1 The N- and C-terminal ends are identified and hydrogen bonds drawn with dotted lines The N-cap hydrogen bond between the carboxyl group of Asp1 and the backbone amide of Ser4 is identified in bold.

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In parallel, recent experimental data on mutants that

incorporate systematic changes in both hydrophobicity

and hydrogen bonding characteristics have assisted in

defining the characteristics of the residues that are crucial

for activity and has led to new proposals for the ice-binding

face of the protein [22,36,37] Further molecular dynamics

studies are required to explain these new experimental

results with mutants and to explain why TTTT recognizes

and accumulates at the {2 0 22 1} planes of ice 1h the usual

form of hexagonal ice at 1 atm

The starting point for almost all simulations to date

[16,18,24,35,38,39] has been the X-ray coordinates of TTTT

[12] The protein is assumed to adopt a very similar

geometry in solution, and NMR studies on TTTT are

consistent with an a helical geometry [13] Simulations of

VVVV2KE with the ice/water interface should provide

significant insight into the mechanism of ice-growth inhibi-tion, as this is the first example of an active mutant that lacks hydrogen bonding side chains at positions 2, 12, 24 and 35 While CD data are consistent with an a helical structure [22], and substitution of ThrfiVal would not be predicted to significantly alter the helical conformation, it is important to confirm that the side chain conformations are unaltered and that the absence of hydrogen bonding residues at the C- and N-terminus does not affect the capping network and overall conformation of the peptide The structure determination of the VVVV2KE mutant of AFP I in solution was made possible by the increased chemical shift dispersion afforded by the two additional Lys/Glu salt bridges in this sequence compared to the wild type peptide (TTTT) There was still substantial resonance overlap, but it mostly affected the peptide repeats for which very similar conformations were suggested by the similarity

in chemical shifts With this assumption, the entire structure could be determined from experimental restraints

As the NMR structure of VVVV2KE is based on short-range restraints, the overall bend of the helix crucially depends on the calibration used for translating the NOE cross peaks into upper distance restraints Therefore, the bend could in principle be an artifact of the automatic calibration routine used in the DYANA calculations The largely different cross-peak intensities observed for different i,i + 3 and i,i + 4 NOEs (Fig 2B) suggest, however, that the a helix is indeed not as uniform and ideal as might be expected for an isolated helix Furthermore, the HNchemical shifts and their temperature coefficients suggest that the VVVV2KE structure is bent in the same direction as the more strongly bent b-conformer in the TTTT crystal structure [8] Superficially the bend seems to be strongest near Lys18 in both VVVV2KE and TTTT As VVVV2KE contains two additional Lys-Glu salt bridges, bends near the additional lysines would also be expected Indeed, the backbone hydrogen bond between Lys29 and Ala25 is formed in only half of the 20 NMR conformers of VVVV2KE, but the resulting bend does not affect the overall structure as much as that near Lys18, because Lys29

is close to the C-terminal end of the peptide The same is true for Lys7 near the N-terminal end, although this residue forms correct backbone hydrogen bonds to Ala3 in all but four of the NMR conformers

While the overall bend in the b-conformer of TTTT is accompanied by changes in the v1angles of several residues, the side-chain conformations in the NMR structure of VVVV2KE are more similar to those of the s-conformer These data can be reconciled by a model where helix bending is facile, proceeding independently of side chain conformations AFP I peptides in solution would thus be involved in an equilibrium between straight and bent helices and, independently, equilibria between different side chain conformations Notably, the conformational spread among the NMR conformers is merely a measure of the precision with which the restraints define the structure, i.e the conformers are not meant to sample the entire conforma-tional space accessible to the peptide Instead, the NMR structure attempts to reflect the most highly populated conformations, although the use of NOE distance restraints entails a bias towards conformers with shorter internuclear distances This bias is also likely to exaggerate the overall helix bend in the NMR structure of VVVV2KE

Fig 4 Stereo views of the crystal structure conformers of TTTT The

two different conformers found in the unit cell of the crystal structure

(PDB accession code 1WFA [8]) are displayed in a line drawing

rep-resentation as in Fig 3A, using a similar orientation and residue

labeling While neither conformer presents a perfectly straight helix,

the conformer in the right panel is more strongly bent than the

con-former in the left panel Throughout the present text, the left and right

conformers are referred to as s- and b-conformer, respectively.

Table 3 Structural statistics for the NMR conformers of VVVV2KE.

Number of nonredundant NOE

upper-distance limits

414

Intra-protein AMBER energy (kcalÆmol)1) )1651 ± 42

Sum of residual NOE-restraint violations (A˚) 4.6 ± 0.2

Maximum dihedral-angle restraint violations () 1.6 ± 0.3

Rmsd to the mean for N, C a

Rmsd to the mean for all heavy atoms (A˚)b 0.88 ± 0.16

Ramachandran plot appearance c

Generously allowed and disallowed regions (%) 0.0

a 33 3 J(H N,Ha ), 24 3 J( Ha,Hb ) b For all residues c From PROCHECK - NMR

[42].

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Earlier NMR studies of TTTT in aqueous solution

showed that the side chains of many of those residues, which

are presumably involved in ice-binding, can populate

multiple v1rotamers in solution, although the most highly

populated rotamers coincided with those found in the

crystal structure [13] A similar situation probably holds for

VVVV2KE, where different side chain rotamers may be

populated to some degree despite the unique rotamers for

most amino-acid side chains (Table 4) Except for some

evidence for increased hydrogen bonding by the C-terminal

NH2group at lower temperatures (see above), there was no

clear indication for more rigid or better-defined backbone or

side-chain conformations at subzero temperatures

com-pared to 10C In principle, the questions of helix bend and

conformational variation could be addressed more

accu-rately by measuring the residual dipolar couplings A

significant set of residual dipolar coupling data would,

however, require isotopically enriched peptide to overcome

problems of signal overlap and to measure the signs of the

dipolar couplings [40]

C O N C L U S I O N S

The solution structure of VVVV2KE provides an improved

basis for simulations of possible ice-binding modes

Furthermore, the availability of sequence-specific resonance

assignments paves the way for a site-specific study of water–

peptide interactions at subzero temperatures by the use of

intermolecular water-peptide NOEs [41] Such a study,

which can be performed in solution, seems particularly

interesting in view of the fact that the interaction of water

with the putative ice-binding surface of TTTT in the single

crystal is severely hindered by intermolecular contacts

between different peptide molecules in the crystal lattice [8]

Note added in proof: the amide chemical shift changes

and helix bend in VVVV2KE are supported by a recent

publication [Cicrpicki, T & Otlewski, J (2001) Amide proton temperature coefficients as hydrogen bond indica-tors in proteins J Biomol NMR 21, 249–261], which has shown that the temperature coefficients of the amide chemical shifts are particularly large on the concave face

of curved helices

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

This research was supported in part by an Australian Research Council Grant (A D J H and M M H.), University of Sydney Sesqui Research and Development Grant (M M H), Welch Grant (A D J H.) and the Swedish Research Council (E L and G O.).

R E F E R E N C E S

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Table 4 Side chain rotamers in the NMR structure of VVVV2KE and

the X-ray structure of TTTT Only those residues are listed that are

none-alanine in both sequences The v 1 -angles listed are those of the

nearest staggered rotamer All angles are given in degrees.

)60

a

Where different side chain rotamers were observed in the two

crystal structure conformers, the first value pertains to the straight

conformer and the second to the bent conformer b Thr in TTTT.

c

Predominant rotamer All three rotamers are populated.

Trang 8

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