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Dinucleoside polyphosphates stimulate the primer independentsynthesis of polyA catalyzed by yeast polyA polymerase Marı´a A.. Gu¨nther Sillero, Anabel de Diego, Hugo Osorio and Antonio S

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Dinucleoside polyphosphates stimulate the primer independent

synthesis of poly(A) catalyzed by yeast poly(A) polymerase

Marı´a A Gu¨nther Sillero, Anabel de Diego, Hugo Osorio and Antonio Sillero

Departamento de Bioquı´mica, Instituto de Investigaciones Biome´dicas Alberto Sols UAM/CSIC, Facultad de Medicina,

Madrid, Spain

Novel properties of the primer independent synthesis of

poly(A), catalyzed by the yeast poly(A) polymerase are

presented The commercial enzyme from yeast, in contrast to

the enzyme from Escherichia coli, is unable to adenylate the

3¢-OH end of nucleosides, nucleotides or dinucleoside

poly-phosphates (NpnN) In the presence of 0.05 mM ATP,

dinucleotides (at 0.01 mM) activated the enzyme velocity in

the following decreasing order: Gp4G, 100; Gp3G, 82; Ap6A,

61; Gp2G, 52; Ap4A, 51; Ap2A, 41; Gp5G, 36; Ap5A, 27;

Ap3A, 20, where 100 represents a 10-fold activation in

relation to a control without effector The velocity of the

enzyme towards its substrate ATP displayed sigmoidal

kin-etics with a Hill coefficient (nH) of 1.6 and a Km(S0.5) value of

0.308 ± 0.120 mM Dinucleoside polyphosphates did not

affect the maximum velocity (Vmax) of the reaction, but did alter its nHand Km(S0.5) values In the presence of 0.01 mM

Gp4G or Ap4A the nHand Km(S0.5) values were (1.0 and 0.063 ± 0.012 mM) and (0.8 and 0.170 ± 0.025 mM), respectively With these kinetic properties, a dinucleoside polyphosphate concentration as low as 1 lM may have a noticeable activating effect on the synthesis of poly(A) by the enzyme These findings together with previous publications from this laboratory point to a potential relationship between dinucleoside polyphosphates and enzymes catalyz-ing the synthesis and/or modification of DNA or RNA Keywords: Ap4A; Gp4G; dinucleoside polyphosphates; yeast poly(A) polymerase

We have recently shown that Escherichia coli poly(A)

polymerase adenylates the 3¢-OH end of nucleosides,

nucleotides and dinucleotides of the type nucleoside (5¢)

oligophospho (5¢) nucleosides (NpnN¢) [1] This novel

property of E coli poly(A) polymerase moved us to analyze

whether these compounds were also substrates of eukaryotic

yeast poly(A) polymerase The yeast enzyme is involved in

the processing of the 3¢-OH end of mRNA [2,3], forming a

complex with two cleaving factors and a polyadenylation

factor [4,5] The core yeast poly(A) polymerase appears to

have a molecular mass of around 63 kDa [3] Separated

form the complex, the core yeast enzyme catalyzes the

addition of poly(A) tails to a variety of RNAs or poly(A) of

different lengths [3] The experiments described below were

carried out with a commercial preparation obtained from an

E coli strain containing a clone of the yeast poly(A)

polymerase gene [6] In principle, it can be assumed that this

preparation corresponds to pure poly(A) polymerase with

no contaminating cleaving factors

While using this preparation, we observed that primer independent poly(A) synthesis was activated by dinucleo-side polyphosphates The findings reported here could open new views both on the catalytic properties of yeast poly(A) polymerase and on the intracellular role of dinucleoside polyphosphates, a family of compounds of increasing metabolic and regulatory interest [7–11]

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

Materials Poly(A) polymerase from yeast was from Amersham Pharmacia Biotech (Code 74225Z, lot numbers: 109217; 109899; 110278; 111182 One unit of enzyme is the amount that incorporates 1 nmol of ATP (as AMP) into

an acid insoluble form in 1 min at 37C These preparations contained 761 UÆmL)1 (1522 UÆmg)1 pro-tein) When required, the enzyme was diluted in 0.25% bovine serum albumin (BSA) Shrimp alkaline phospha-tase (EC 3.1.3.1) was from Roche Molecular Biochemicals and phosphodiesterase (from Crotalus durissus, EC 3.1.4.1) was from Boehringer Mannheim [a-32P]ATP (3000 CiÆmmol)1) was from Dupont NEN TLC silica-gel fluorescent plates were from Merck X-ray films were from Konica Corporation Radioactively labeled nucleo-tides were quantified by the use of an InstantImager (Packard Instrument Co.) HPLC was carried out in a Hewlett Packard chromatograph (model 1090), with a diode array detector, commanded by an HPLC Chem-Station The Hypersil ODS column (2.1· 100 mm) was from Hewlett Packard

Correspondence to A Sillero, Departamento de Bioquı´mica,

Facultad de Medicina UAM, C/Arzobispo Morcillo 4, 28029

Madrid, Spain Fax: + 34 91 5854587, Tel.: + 34 91 3975413,

E-mail: antonio.sillero@uam.es

Abbreviations: Gp n G, guanosine(5¢)oligophospho(5¢)guanosine;

Np n N, nucleoside (5) oligophospho (5¢) nucleosides.

Enzymes: alkaline phosphatase (EC 3.1.3.1); phosphodiesterase from

Crotalus durissus (EC 3.1.4.1); poly(A) polymerase from Escherichia

coli and from yeast (EC 2.7.7.19).

(Received 9 July 2002, revised 9 September 2002,

accepted 11 September 2002)

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reaction mixtures were treated with 20 UÆmL)1 shrimp

alkaline phosphatase for 1 h at 37C, and after

inacti-vation of the phosphatase, by heating at 90C for

5 min, treated further with 20 lgÆmL)1phosphodiesterase

for 1 h at 37C

TLC

The reaction mixtures (usually 0.01–0.02 mL) contained

(0.02 mM) [a-32P]ATP (20 lCiÆmL)1) Aliquots (0.0015 mL)

of the reaction were taken, spotted on silica gel plates, and

developed in dioxane/ammonium hydroxide/water 6 : 1 : 6

(v/v/v) Nucleotide spots were localized with a 253-nm

wavelength light and the radioactivity measured by

auto-radiography and/or with an InstantImager

HPLC

Aliquots (0.01 mL) of the reaction mixtures (usually in a

volume of 0.035 mL) were transferred into 0.1 mL of water

and kept at 95C for 1.5 min After chilling, the mixtures

were filtered (using a Millipore HA, 0.45 lm nitrocellulose

membrane) and a 0.05-mL aliquot injected into a Hypersil

ODS column Elution was performed at a flow rate of

0.5 mLÆmin)1with a 20-min linear gradient (5–30 mM) of

sodium phosphate (pH 7.5), in 20 mM

tetrabutylam-monium bromide/20%methanol (v/v) (buffer A) followed

by a 10-min linear gradient (30–100 mM) of sodium

phosphate (pH 7.5) in buffer A

R E S U L T S

Comparison of poly(A) polymerase fromE coli

and yeast

As stated in the Introduction, E coli poly(A) polymerase,

in the presence of micromolar concentrations of ATP,

adenylates the 3¢-OH residues of most of the nucleosides,

nucleotides and dinucleotides tested and, under our

experimental conditions, is unable to catalyze the synthesis

of a poly(A) chain in the absence of a primer [1] In order

to explore whether the yeast enzyme also exhibited the

same properties we assayed, in parallel, the activity of

both enzymes on guanosine, GDP and diguanosine

tetraphosphate (Gp4G), in the presence of 0.02 mM

[a-32P]ATP While confirming the adenylylation of these

compounds and the absence of synthesis of poly(A) by the

E colipoly(A) polymerase, we did not observed

adenyly-lation of guanosine, GDP or Gp4G by the yeast enzyme

In the absence or presence of these compounds, labeled

ATP was transformed mainly into a radioactive spot

absence or presence of Gp2G, Gp3G, Gp4G and the reaction products analyzed by HPLC after 30, 60 and

120 min incubation In the absence of dinucleotides, the amount of ATP decreased slowly along the incubation time, with no concomitant increase of any ATP derivative (Fig 1A) In the presence of diguanosine polyphosphates (Gp2G, Gp3G or Gp4G), ATP consumption was strongly stimulated, but again, formation of potential products of the reaction was not observed The results obtained after

30 min incubation are represented in Fig 1B The apparent loss of ATP was assumed to be due to the formation of a product, probably poly(A), that could be retained by the column

To test this assumption, the enzyme was incubated with 0.2 mMATP, under the same experimental conditions as

in Fig 1, for 60 min at 37C A control without enzyme was also carried out The complete reaction mixture was then divided into equal parts and one of them treated with phosphodiesterase The three samples involved were analyzed by HPLC The amount of ATP in the control, indicates the ATP present at the start of the reaction (Fig 2A); the ATP that was consumed after incubation with the polymerase (Fig 2B), was totally recovered as AMP (Fig 2C), when the reaction mixture was treated with phosphodiesterase before analysis by HPLC From these results (Figs 1 and 2), it can be concluded that poly(A) was synthesized from ATP, in the absence of primer, and that Gp2G, Gp3G, and Gp4G stimulated that synthesis

Stimulation of poly(A) synthesis as a function of diguanosine diphosphate (Gp2G) concentration The concentration of dinucleoside polyphosphate needed

to stimulate the synthesis of poly(A) was analyzed using

Gp2G as effector Yeast poly(A) polymerase was incu-bated with 0.02 mM [a-32P]ATP, in the absence and presence of three different concentrations of Gp2G (0.001, 0.010, or 0.050 mM) After 5, 10 and 20 min incubation, aliquots of the reaction mixture were analyzed by TLC The results corresponding to the 5-min incubation are shown in Fig 3 No appreciable synthesis of poly(A) (spot at the origin) was observed in the absence of Gp2G, whereas in its presence the ATP spot decreased, increasing concomitantly the radioactivity

at the origin In the presence of 0.01 or 0.050 mMGp2G, almost no ATP was left in the assay after 5 min incubation These results show that a concentration as low as 0.001 mM Gp2G stimulates, under these condi-tions, the synthesis of poly(A) catalyzed by yeast poly(A) polymerase around sixfold

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Relative activity of GpnGs as effectors of the synthesis

of poly(A)

Based on the above results, the effect of several diguanosine

polyphosphates on the synthesis of poly(A) was

comparat-ively studied The enzyme was incubated for 10 min with

0.05 mM [a-32P]ATP, and in the absence or presence of

Gp2G, Gp3G, Gp4G, Gp5G (0.01 mMeach) Aliquots of

the reaction mixture were applied to a TLC plate Under

these conditions, the maximum ATP consumed was less

than 50% (Fig 4A) Formation of poly(A) (spots at the

origin) was clearly seen in the samples containing

dinucleo-tides, but scarcely visible in the control reaction (with

enzyme and without GpnG) carried out in duplicate (lanes

C) The reaction mixtures were treated further with alkaline

phosphatase and (after inactivation of the phosphatase)

with phosphodiesterase and analyzed by TLC as above

(Fig 4B) The results round off those presented in Figs 4A

i.e AMP, representing the amount of ATP incorporated

into poly(A), appears preferentially in the reaction mixtures

containing the effectors (Fig 4B) From the radioactivity

present in the AMP spot, the relative capacity of

diguan-osine polyphosphates to stimulate the synthesis of poly(A),

considering a media of four experiments, was: Gp4G, 100;

Gp3G, 82; Gp2G, 52; Gp5G, 36, where 100 represents a

10-fold activation in relation to a control without effector

Effect of diadenosine polyphosphates on poly(A)

polymerase

Previous experiments had shown that diadenosine

poly-phosphates also stimulated the synthesis of poly(A)

catalyzed by yeast poly(A) polymerase The relative

activity of diadenosine polyphosphates as effectors of

the poly(A) synthesis was assayed as in Fig 4, using 0.05 mM [a-32P]ATP as substrate, in the absence or presence of 0.01 mM ApnAs The relative efficiency of diadenosine polyphosphates to stimulate the synthesis of poly(A), considering a media of four experiments, was:

Ap6A, 61; Ap4A, 51; Ap2A, 41; Ap5A, 27; Ap3A, 20 (results not shown) These values were calculated relative

to the maximal activation (100) considered for Gp4G (see above)

Dinucleoside polyphosphates diminish the Km(S0.5) value for ATP in the primer independent synthesis of poly(A)

In order to understand why dinucleoside polyphosphates activated the primer independent synthesis of poly(A), the effect of 0.01 mM Gp4G or Ap4A on the synthesis of poly(A) was analyzed at different ATP concentrations (0, 0.025, 0.05, 0.1 and 0.2 mM) Samples were taken after

10 min incubation (a time at which the velocity of the reactions were linear, as tested in previous assays) spotted

on TLC plates and the rate of synthesis of poly(A) as a function of ATP concentration determined as in Fig 4 Moreover, in these conditions less than 30% of the ATP was consumed in the case of the reaction mixtures containing effectors and the lowest concentration of substrate The Michaelis-Menten (Fig 5A), Lineweaver-Burk (Fig 5B) and Hill (Fig 5C) plots of the results showed that the enzyme presented a sigmoidal kinetics that tended to hyperbolic in the presence of Gp4G or

Ap4A From these plots, maximum velocity (Vmax) and

Km(S0.5) values were determined In the absence of effector, the enzyme presented a Hill coefficient of around 1.6 that decreased to around 1.0 and 0.8 in the presence

of 0.01 mM GpG or ApA, respectively The K (S )

Fig 1 Effect of diguanosine polyphosphates

(Gp 2 G, Gp 3 G, Gp 4 G) on the consumption of

ATP catalyzed by yeast poly(A) polymerase.

The reaction mixtures (0.035 mL) contained:

20 m M Tris/HCl, pH 7.0, 50 m M KCl, 0.7 m M

MnCl 2 , 0.2 m M EDTA, 100 lgÆmL)1

acetyl-ated BSA, 10% glycerol, 0.5 m M MgCl 2 ,

0.2 m M ATP and 0.44 units of the enzyme

(part A) Reaction mixtures supplemented

with 0.04 m M Gp 2 G, 0.1 m M Gp 3 G or Gp 4 G

are shown in part (B) of the figure After 30, 60

and 120 min incubation at 37 C, aliquots

were taken and analyzed by HPLC as

indica-ted in Materials and methods.

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values for ATP were 0.308 ± 0.120 mM (n¼ 5),

0.063 ± 0.012 mM (n¼ 3) and 0.170 ± 0.025 mM

(n¼ 3) in the absence or presence of Gp4G or Ap4A,

respectively The Vmax value determined for the primer

independent synthesis of poly(A) was about the same in

the absence or presence of dinucleotides, i.e around

500 UÆmL)1 [equivalent to a rate (kcat) of AMP

incor-poration of 1 s)1] a value close to that determined in the

presence of poly(A) as a primer, as stated by the

manufacturer

D I S C U S S I O N

Some experimental aspects can be considered firstly, in

relation to the methods currently used by others to assay

poly(A) polymerases As noted previously [1], the labeled RNA-(A)nproducts synthesized by polymerases are usually determined by acid precipitation or phenol extraction and ethanol precipitation The amount of radioactivity deter-mined in those precipitates is the parameter used to determine the poly(A) polymerase activity [12–18] Potential reaction products that do not precipitate with these procedures may pass unnoticed

Adenylation of nucleosides, nucleotides and dinucleotides

by E coli poly(A) polymerase [1] was detected using TLC and HPLC methods, the same two methods used in this work to study the yeast enzyme The TLC procedure involves spotting aliquots of the complete reaction mixture onto a plate and analysis of all the potential reaction products synthesized during incubation In the HPLC procedure, the reaction mixture is heated and filtered (see Materials and methods) All the poly(A) products synthes-ized from ATP passed through this filter, but were retained

by the precolumn or column The enzyme activity could be followed either, by measuring the decrease of the ATP content in the reaction mixture or by treating the reaction mixture first with alkaline phosphatase (to hydrolyze residual adenosine 5¢-phosphates to adenosine) and then with phosphodiesterase to hydrolyze the synthesized poly(A) to AMP According to our results, the amount of

Fig 2 ATP consumption catalyzed by yeast poly(A) polymerase The

reaction mixtures (0.035 mL) contained: 20 m M Tris/HCl, pH 7.0,

50 m M KCl, 0.7 m M MnCl 2 , 0.2 m M EDTA, 100 lg/mL acetylated

BSA, 10% glycerol, 0.5 m M MgCl 2 , 0.2 m M ATP and in the absence

(A) or presence of 0.76 units of the enzyme (B and C) After 60

incubation at 37 C (B) an aliquot of the reaction mixture was then

treated further with phosphodiesterase (C) The analysis was

per-formed by HPLC as indicated in Materials and methods The areas of

the peaks corresponding to ATP (A and B) and AMP (C) were, in

arbitrary units, 1243, 175 and 1265, respectively.

Fig 3 Effect of different concentrations of Gp 2 G on the synthesis of poly(A) catalyzed by yeast poly(A) polymerase The reaction mixture (0.01 mL) contained: 0.02 m M ATP, 0.2 lCi [a-32P]ATP, Gp 2 G (as indicated), 0.38 units of the enzyme and other conditions as described

in Materials and methods After 5 min incubation at 37 C, aliquots were taken and analyzed by TLC Lane (– E): control without enzyme.

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AMP so obtained was equimolar to the ATP consumed

during the enzyme reaction

The difference between the enzyme from E coli and yeast

concerning their substrate specificity towards nucleosides,

nucleotides and dinucleotides is also worth noting The

yeast poly(A) polymerase, contrary to the E coli enzyme, is

apparently unable to adenylate the 3¢-OH end of those

compounds However, the primer independent activity of

the yeast enzyme is strongly activated by dinucleoside

polyphosphates Commercial yeast poly(A) polymerase

presented, in the absence of primer, a sigmoidal kinetics

towards its substrate ATP, with a Hill coefficient (nH) of

around 1.6 The presence of GpG or ApA changed the

kinetic from sigmoidal to hyperbolic, decreasing the Km (S0.5) value from 0.308 ± 0.120 mMto 0.063 ± 0.012 mM and 0.170 ± 0.025 mMin the presence of GpG or ApA,

Fig 4 Effect of diguanosine polyphosphates (Gp 2 G, Gp 3 G, Gp 4 G,

Gp 5 G) on the synthesis of poly(A) catalyzed by yeast poly(A)

poly-merase The reaction mixture (0.02 mL) contained: 0.05 m M ATP,

0.4 lCi [a- 32 P]ATP, 0.01 m M Gp n G, 0.19 units of the enzyme and

other conditions as described in Materials and methods After 10 min

incubation at 30 C, aliquots were taken, and spotted on a TLC plate

(Part A) The rest of the reaction mixture was treated with shrimp

alkaline phosphatase and phosphodiesterase as described in Materials

and Methods and analyzed as above (Part B) Lane (– E): control

without enzyme; lanes (C): complete reaction with no added

dinu-cleotide; other lanes (1–4) with added Gp n G (0.01 m M ) as indicated. Fig 5 Influence of ATP concentration on the primer independent

syn-thesis of poly(A) catalyzed by yeast poly(A) polymerase Effect of Ap 4 A

or Gp 4 G The reaction mixture (0.02 mL) contained: variable concentrations of [a- 32 P]ATP (0.025–0.2 m M ) specific activity:

320 lCiÆlmol)1, 0.2 m M MgCl 2 , 0.1 units of the enzyme, 0.01 m M

Ap 4 A or Gp 4 G where indicated and other conditions as described in Materials and methods After 10 min incubation at 30 C, the reaction was stopped by heating 2 min at 90 C, treated with alkaline phos-phatase and phosphodiesterase and analyzed by TLC (v, is expressed

as lmol of AMP incorporated min)1ÆmL)1).

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About the presence of these compounds in the nucleus,

Ap4A is a dinucleotide specifically described to be present

in that organelle [24,25], but due to the pore size of the

nuclear envelope it can be considered that the

(di)nucleo-tide content in the nucleus may be similar to that in whole

cells [26] An additional, and still unsolved problem, is the

question of how much of the (di)nucleotide content in

nuclei is free or ligated to nuclear structures [27] or

present in the environment in which the poly(A)

poly-merase is located This may have an influence on the

enzyme as it seems to be a relationship between the

enzyme activity and the concentration of both ATP and

dinucleotides: poly(A) polymerase displays a sigmoidal

kinetics that becomes hyperbolic in the presence of

dinucleotides, a behavior that greatly enhances the enzyme

activity particularly at low ATP concentrations; for

instance at 0.02 mM ATP, concentrations as low as

1 lM of some dinucleotides may increase poly(A)

synthe-sis more than sixfold.; the influence that this activation

could have on the processing of the 3¢-OH end of mRNA

could also be considered

The sigmoidal kinetics displayed by the enzyme favors the

view that poly(A) polymerase may contain an allosteric area

for a dinucleotide or (a dinucleotide-like structure) with the

following apparent preferences: comparing dinucleotides

with the same number of inner phosphates, guanine

dinucleotides are more active than adenine dinucleotides

and, adenine dinucleotides with even number of inner

phosphates tend to be more efficient than those with odd

number of phosphates

We are aware that poly(A) polymerase has been

described as a multienzyme complex that may have in vivo

different, or additional, properties to those reported here In

any event, yeast poly(A) polymerase, as supplied by the

manufacturer, is strongly activated by lmolar

concentra-tions of dinucleotides, preferentially at low ATP

concen-trations The physiological significance of these findings

deserves further exploration

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

This investigation was supported by grants from Direccio´n General de

Investigacio´n Cientı´fica y Te´cnica (PM98/0129; BMC2002-00866) and

Comunidad de Madrid (08/0021.1/2001) H.O was supported by a

Fellowship from Fundac¸a˜o para a Cieˆncia e a Tecnologia (SFRH/BD/

1477/2000).

R E F E R E N C E S

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11 McLennan, A.G., Barnes, L.D., Blackburn, G.M., Brenner, Ch, Guranowski, A., Miller, A.D., Rovira, J.M., Rotlla´n, P., Soria, B., Tanner, J.A & Sillero, A (2001) Recent developments in the study

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19 Garrison, P.N & Barnes, L.D (1992) Determination of dinu-cleoside polyphosphates In Ap 4 A and Other Dinucleoside Poly-phosphates (Mclennan, A.G., eds), pp 29–61 CRC Press, Boca Raton, FL, USA

20 Warner, A.H (1992) Diguanosine and related nonadenylated polyphosphates In Ap 4 A and Other Dinucleoside Polyphosphates (Mclennan, A.G., eds), pp 275–303 CRC Press, Boca Raton, FL, USA.

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21 Sillero, M.A.G., de Diego, A., Cerda´n, S., Criel, G & Sillero, A.

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22 Jankowski, J., Hagemann, J., Tepel, M., van Der Giet, M.,

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Zidek, W & Schlu¨ter, H (2001) Dinucleotides as

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dipho-sphates Ap 2 A, Ap 2 G, and Gp 2 G in releasable granules of platelets.

J Biol Chem 276, 8904–8909.

23 Schlu¨ter, H., Grob, I., Bachmann J., Kaufmann, R., van der Giet,

M., Tepel, M., Nofer, J.R., Assmann, G., Karas, M., Jankowski,

J & Zidek, W (1998) Adenosine (5¢) oligophospho-(5¢)

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24 Weinmann-Dorch, C & Grummt, F (1986) Diadenosine tetra-phosphate (Ap 4 A) is compartmentalized in nuclei of mammalian cells Exp Cell Res 165, 550–554.

25 Andersson, M & Lewan, L (1989) Diadenosine tetraphosphate (Ap 4 A): its presence and functions in biological systems Int J Biochem 21, 707–714.

26 Traut, T.W (1994) Physiological concentrations of purines and pyrimidines Mol Cell Biochem 140, 1–22.

27 Sols, A & Marco, R (1970) Concentrations of metabolites and binding sites Implications in metabolic regulation Curr Top Cell Regul 2, 227–273.

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