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Tiêu đề Human Cdc45 is a proliferation-associated antigen
Tác giả S. Pollok, C. Bauerschmidt, J. Sänger, H.-P. Nasheuer, F. Grosse
Trường học Leibniz Institute for Age Research, Fritz Lipmann Institute
Chuyên ngành Biochemistry
Thể loại Báo cáo khoa học
Năm xuất bản 2007
Thành phố Jena
Định dạng
Số trang 16
Dung lượng 1,13 MB

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Nội dung

Our findings show that Cdc45 protein is absent from long-term quiescent, terminally differentiated and senescent human cells, although it is present throughout the cell cycle of prolifera

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S Pollok1, C Bauerschmidt2, J Sa¨nger3, H.-P Nasheuer4and F Grosse1,5

1 Leibniz Institute for Age Research, Fritz Lipmann Institute, Jena, Germany

2 Radiation Oncology and Biology, University of Oxford, UK

3 Institute of Pathology, Bad Berka, Germany

4 National University of Ireland, Department of Biochemistry, Galway, Ireland

5 Center for Molecular Biomedicine, Friedrich Schiller University, Jena, Germany

In an adult human body only a small proportion of

cells actively progresses through the mitotic cell cycle

in self-renewing tissues [1] The majority of cells have

ceased proliferation during growth and development

and have arrested temporarily or permanently in

non-proliferative states Normal somatic cells require

stimu-lation by growth factors for continual proliferation

After mitogen withdrawal, cells exit the cycle prior to

progression through the restriction point in G1 and

enter into a quiescent state also called G0 [2] The G0

arrest is reversible and after addition of growth factors

cells re-enter the cell cycle [2] In addition, cells can be

induced to enter a differentiation pathway [1]

More-over, normal somatic cells have only a limited

poten-tial to divide After a finite number of cell divisions

they irreversibly enter a senescent state [3] In contrast

to quiescent cells, senescent cells fail to initiate DNA replication in response to mitogens [4]

Previous reports have shown that licensing factors are present in actively cycling cells but are downregu-lated during quiescence, differentiation and senescence [5–8] The licensing reaction depends on the sequential assembly of cell division cycle protein 6 (Cdc6), cdc10 target 1 (Cdt1) and minichromosome maintenance (Mcm)2–7 at origins of replication in late mitosis and early G1 to form the so-called prereplicative complex [9] At the G1⁄ S transition prereplicative complexes are converted into initiation complexes by the concerted action of cyclin-dependent kinases and Cdc7 kinase [10] Following activation of these kinases, replication factors such as Cdc45, GINS and Mcm10 are recruited

to the origins [11] Cdc45 has a critical role in the

Keywords

half life; molecule number; proliferation

marker; senescence; terminal differentiation

Correspondence

F Grosse, Leibniz Institute for Age

Research, Fritz Lipmann Institute e.V.,

Biochemistry, Jena, Germany

Fax: +49 3641-656288

Tel: +49 3641 656290

E-mail: fgrosse@fli-leibniz.de

(Received 9 March 2007, revised 21 May

2007, accepted 23 May 2007)

doi:10.1111/j.1742-4658.2007.05900.x

Cell division cycle protein 45 (Cdc45) plays a critical role in DNA replica-tion to ensure that chromosomal DNA is replicated only once per cell cycle We analysed the expression of human Cdc45 in proliferating and nonproliferating cells Our findings show that Cdc45 protein is absent from long-term quiescent, terminally differentiated and senescent human cells, although it is present throughout the cell cycle of proliferating cells More-over, Cdc45 is much less abundant than the minichromosome maintenance (Mcm) proteins in human cells, supporting the concept that origin binding

of Cdc45 is rate limiting for replication initiation We also show that the Cdc45 protein level is consistently higher in human cancer-derived cells compared with primary human cells Consequently, tumour tissue is pref-erentially stained using Cdc45-specific antibodies Thus, Cdc45 expression

is tightly associated with proliferating cell populations and Cdc45 seems to

be a promising candidate for a novel proliferation marker in cancer cell biology

Abbreviations

BrdU, 5-bromo-1-(2-deoxy-b- D -ribofuranosyl) uracil; Cdc, cell division cycle; Cdt1, cdc10 target 1; CENP-F, centromer protein F; b-Gal, senescence associated b-galactosidase; HEF, human embryonic fibroblasts; HRP, horseradish peroxidase; IP, immunoprecipitation; Mcm, minichromosome maintenance; Orc, origin recognition complex; PCNA, proliferating nuclear antigen; PMA, 4b-phorbol 12-myristate 13-acetate; RPA, replication protein A; TdR, thymidine.

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initiation and elongation steps of DNA replication

[12–14] Chromatin association of Cdc45 requires

activity of both cyclin-dependent kinases and Cdc7

[15,16] Studies in baker’s yeast and Drosophila

revealed that Cdc45 is part of a high molecular mass

complex, which was shown to possess helicase activity

[17,18] leading to the concept that Cdc45 is an

auxili-ary factor for the putative Mcm2–7 helicase [19]

In contrast to human replication licensing factors

such as the Mcm proteins, very little is known about

the expression of human Cdc45 during exit from

cell proliferation to nonproliferating states Here, we

report on the analysis of human Cdc45 protein levels

during the mitotic cell cycle and in various

nonprolifer-ating states Our data highlight that Cdc45 is a

prolif-eration-associated antigen that becomes undetectable

in long-term quiescent, terminal differentiated and

sen-escent human cells Demonstration of good

immunore-activity of a Cdc45-specific antibody in formalin-fixed

paraffin-embedded tissues suggests that Cdc45 could

be used as a marker for cell proliferation From our

analysis we estimated that the number of Cdc45

mole-cules per human cell is 4.5· 104 Comparison with the

published molecule number for Mcm3 (1· 106) [20]

demonstrates the relative low abundance of Cdc45 in

human cells and is further evidence that Cdc45 may be

a rate-limiting factor for the initiation of DNA

replica-tion [21,22]

Results

Level of Cdc45 protein is constant during the cell

cycle in proliferating cells

The central functions of Cdc45 in human DNA

repli-cation raised the question of whether Cdc45 is

regula-ted differently in proliferating and nonproliferating

cells First, we analysed the expression and subcellular

distribution of human Cdc45 protein during the cell

cycle in proliferating HeLa S3 cells To this end, cells

were arrested at the G1⁄ S border by a double

thymi-dine (TdR) block and released to continue the cell

cycle Successful synchronization and cell-cycle

distri-bution was confirmed by flow cytometry (Fig 1A) To

monitor cell-cycle progression of the synchronized

cells, levels of cyclin A and cyclin B1 were detected in

western blots and shown to fluctuate depending on

progression through the cycle (Fig 1B) In parallel,

levels of origin recognition complex (Orc)2, Cdc45 and

b-actin (loading control) were determined to be rather

invariable in cycling HeLa S3 cells (Fig 1B)

To verify the cell-cycle distribution of synchronized

cells, which were maintained under optimal growth

conditions, immunofluorescence studies were per-formed with the following phase-specific markers: Ki-67 for G1phase (12 h after TdR block) and mitosis (9 h after TdR block), 5-bromo-1-(2-deoxy-b-d-ribo-furanosyl) uracil (BrdU) incorporation for the S phase (3 h after TdR block) and centromer protein F (CENP-F) for the G2 phase (9 h after TdR block) Human Cdc45 protein was exclusively present in the nucleus from G1 to G2, but was uniformly distributed throughout the cell interior after breakdown of the nuclear membrane in mitosis (Fig 1C) Consistent with our previous report [23], Cdc45 appeared in a spot-like pattern in the S phase, which partially colo-calized with BrdU signals In metaphase, anaphase and telophase, Cdc45 was found spread around the condensed chromosomes (Fig 1C) These prominent changes in the subcellular localization of Cdc45, together with an unchanged protein level during the cell cycle, were also obtained with T98G cells (data not shown) The data led us to conclude that human Cdc45 protein is present at comparable amounts throughout all phases of cycling cells

Cdc45 protein is diminished in quiescent human cells

Stoeber et al [6] demonstrated that human Mcm2, Mcm3 and Mcm5 proteins were completely down-regulated when WI-38 cells stopped proliferation and entered into quiescence Furthermore, Cdc6, Mcm2, Mcm3, Mcm5 and Mcm7 proteins were not detectable

in quiescent mouse NIH 3T3 cells [6] Also, another initiation factor, human Cdt1 protein, was not expressed in quiescent human foreskin fibroblasts [24] Arata et al reported that Cdc45 protein was below detectable levels in quiescent mouse NIH cells [25] These findings led us to investigate whether the human replication factor Cdc45 is also downregulated when human cells exited from the cell cycle and entered into the G0 phase Therefore, T98G glioblastoma cells and human embryonic fibroblasts (HEF) were growth-arrested by serum starvation in combination with contact inhibition for up to 20 days and cells were collected at the indicated times for later analyses After 7 days of serum starvation the majority of T98G and HEF cells reached quiescence, as monitored

by the absence of cyclin A and upregulation of the p27KIP1 protein (Fig 2A,C) Expression of the Ki-67 protein is associated with proliferating cells and is undetectable in quiescent cells [26,27] We found that Cdc45 protein became undetectable in long-term quies-cent cells (Fig 2A,C) Cdc6, Mcm2 and Mcm7 were previously shown to be downregulated in G0 and

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served as controls for proteins that are absent in

nonproliferating cells (Fig 2A,C) [6] Logarithmically

growing T98G cells expressed Ki-67 and also Cdc45,

whereas quiescent cells, which were markedly smaller

in size, expressed neither Ki-67 nor Cdc45 (Fig 2D)

Contrary to these findings, proliferating nuclear

anti-gen (PCNA), the DNA polymerase d subunits p125

and p50 and the replication protein A subunits p70

and p32 were present in G0 cells even after 20 days

serum starvation, although the protein levels of some

were reduced slightly (Fig 2B) These findings suggest

that the latter proteins might fulfil essential functions

in quiescent cells such as DNA repair Furthermore,

Cdc45 protein was not detectable in an extract from

primary unstimulated lymphocytes isolated from fresh

blood of a healthy volunteer (see below), in accordance

with the reported resting G0 state of primary periph-eral blood T lymphocytes [28]

Regulation of Cdc45 in terminally differentiated cells

To explore the regulation of human Cdc45 in nonpro-liferating cells in more detail, the differentiation of human cells was used as a second system Human Cdc6 protein was completely downregulated during

in vitro differentiation of K562 cells to cells with a megakaryocytic phenotype [29] Furthermore, the amount of human Mcm3 protein was significantly reduced after induction of HL60 differentiation into monocytes⁄ macrophages [7] Mcm protein expression was absent in adult neurons and cardiac myocytes [6]

A

C

B

Fig 1 Expression of human Cdc45 protein in proliferating cells (A) Flow cytometry analysis of HeLa S3 cells after release from a double TdR block Asynchronously growing cells (log) served as a control for the classification of cell-cycle phases (B) Immunoblot analysis was performed from whole-cell lysates of asynchronously proliferating cells (log) and cells in a time course after release from a double TdR block Cdc45, Orc2, cyclin A and cyclin B1 were detected with specific primary antibodies, HRP-coupled secondary antibodies, followed by the standard enhanced chemoluminescence technique b-Actin served as a control for equal loading (C) Immunofluorescence analysis of the subcellular dis-tribution of Cdc45 throughout the cell-cycle phases The yellow bar in the phase contrast ⁄ DAPI stain indicates 10 lm (·100) The upper panel shows phase contrast and DAPI staining, the middle panel displays Cdc45 in green and the lower panel shows in red either Ki-67 (G 1 phase:

12 h after TdR block, and mitosis: 9 h after TdR block), BrdU (S phase: 3 h after TdR block) or CENP-F (G 2 phase: 9 h after TdR block).

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To test whether Cdc45 is regulated during terminal

differentiation both HL60 and K562 cells were treated

with 4b-phorbol 12-myristate 13-acetate (PMA) After

24 h of PMA incubation HL60 cells showed several

monocyte⁄ macrophage-like characteristics, such as an

intense clustered adherence of almost all cells on the

plastic surface, accompanied by the formation of

prom-inent pseudopodia (Fig 3B) Terminal differentiation

to the monocyte⁄ macrophage phenotype was also

veri-fied by a Nitro Blue tetrazolium reduction assay

Monocytes⁄ macrophages are able to generate reactive

oxygen species and this burst activity can be visualized

by the existence of blue–black diformazan granules

within the cell Only 12 h after PMA incubation 35%

of HL60 cells were Nitro Blue tetrazolium-positive

(Fig 3C,F) indicating the macrophage status [30] Fur-thermore, the arrest of PMA-treated HL60 cells was monitored by the detection of p21CIP1 and p27KIP1 in western blots (Fig 3A) Exponentially growing HL60 cells expressed no detectable p21CIP1 and only small amounts of p27KIP1 Induction of p21CIP1 and p27KIP1 was detected at defined periods after PMA treatment [31] indicating that the cells stopped cycling after induction of differentiation (Fig 3A) Changes in morphology of cycle-arrested cells were accompanied

by a rapid decrease in immunological detectable Cdc45 within 36 h after PMA application; 12 h later the level of Cdc45 protein was almost completely abol-ished (Fig 3A) Similarly, immunofluorescence studies with HL60 cells revealed that Cdc45 protein became

Fig 2 Regulation of human Cdc45 protein following exit into the G 0 phase (A,C) Immunoblot analysis of Mcm2, -4, -7, Cdc6, Cdc45, cyclin

A and p27 KIP1 in whole-cell lysates of asynchronously proliferating (log) and serum-starved T98G cells (A) and human embryonic fibroblasts (HEF) (C) (B) Immunoblot analysis of DNA polymerase d p125 and p50 subunits, PCNA and replication protein A p70 and p32 subunits in whole-cell lysates of serum-starved T98G cells (D) Immunofluorescence analysis of Cdc45 in logarithmic (log) or 10 days serum-starved T98G cells (G 0 ) The upper panel shows phase contrast and Ki-67 in red, the lower panel shows Cdc45 in green (·20).

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undetectable after 48 h of PMA incubation (data not

shown) In addition, a significant downregulation of

human Cdc45 protein was also detected after

incuba-tion of HL60 cells with all trans retinoic acid, which

causes terminal differentiation along the granulocyte

phenotype (supplementary Fig S1A) Moreover, in the

same cell line, the Cdc45 protein became undetectable

60 h after incubation with 1a-25-dihydroxy-vitamin

D3, which induces differentiation of HL60 cells into

monocytes (supplementary Fig S1B) In contrast to the

considerable downregulation of Cdc45 after induction

of differentiation, the licensing factors Cdc6, Mcm2,

Mcm4 and Mcm7 were still present in those

differenti-ated cells (Fig 3A, supplementary Fig S1)

Ninety-six hours after incubation with PMA, the multipotential, haematopoietic malignant K562 cells displayed morphological changes characteristic of mega-karyocytic differentiation Numerous cells were larger and adhered on plastic surfaces compared with parental suspension cells (Fig 3E) In these cells, Cdc6 became undetectable 24 h after PMA incubation (Fig 3D), in agreement with published results [29] PMA-induced differentiation along the megakaryocytic phenotype was accompanied by downregulation of cyclin E [29] and cyclin A, indicating cell-cycle arrest (Fig 3D) Forty-eight hours after PMA application Cdc45 pro-tein was no longer detectable, whereas Mcm2 and Mcm7 protein levels were still visible but significantly

Fig 3 Regulation of human Cdc45 protein during terminal differentiation (A,D) Immunoblot analysis of whole-cell lysates of HL60 (A) and K562 (D) cells treated with PMA for up to 96 h to induce terminal differentiation b-Tubulin served as an internal control (B,E) Changes of cell morphology and attachment properties after PMA incubation of HL60 cells (B, ·100) and K562 cells (E, ·10) (C) Number of Nitro Blue tetrazolium-positive HL60 cells in PMA time course (F) Detection of Nitro Blue tetrazolium-positive HL60 cells after 12 h of PMA incubation (Left) magnification ·20, (right) magnification ·100.

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downregulated, and Mcm4 levels did not change at all

in the differentiated megakaryocytic-like cells compared

with undifferentiated K562 cells (Fig 3D) Collectively,

in the tested differentiation systems there seem to exist a

(slightly) unequal regulation of the various DNA

repli-cation factors, whereas the time dependence of Cdc45

expression was remarkably similar

Level of Cdc45 protein is abolished in human

cells entering senescence in vitro

After a finite number of cell divisions normal somatic

cells irreversibly arrest in G1 with a senescent

pheno-type Stoeber et al [6] showed that human Mcm2,

Mcm3, Mcm5 and Cdc6 proteins were downregulated

in senescent WI-38 fibroblasts, whereas Orc2 protein

levels remained largely unaffected [6] However, to

date, nothing has been reported about the regulation

of Cdc45 protein in cells entering replicative

senes-cence

Senescent MRC-5 and WI-38 fibroblasts were

obtained by continuously culturing them up to passage

26 or 28 Intracellularly, senescence was exerted and

maintained through the function of the cyclin-kinase

inhibitors p21CIP1 and p16INK4A [32] In agreement

with the literature [33], the protein level of p21CIP1

accumulated when the cells were growth arrested and

then decreased when the cells achieved senescence

(Fig 4A,B), whereas the p16INK4Aprotein level peaked

when the fibroblasts had reached senescence (Fig 4A)

To verify the presence of senescent cells, the activity

of senescence-associated b-galactosidase (b-Gal) was

determined (Fig 4C) [34] Approximately 65% of

MRC-5 and WI-38 cells in passage 26 were

b-Gal-pos-itive (Fig 4A,B; percentages above the passage

num-ber) In WI-38 cells of passage 28 this was increased to

83% (Fig 4B) Immunoblot analysis of total extracts

revealed that Cdc45 protein was no longer detectable

in late passage and in senescent fibroblasts, where it

followed a similar expression course as Mcm7, which

was determined in parallel (Fig 4A,B)

In cells induced to proliferate Cdc45 protein is

expressed just prior to the S phase

The apparent absence of Cdc45 from nonproliferating

cells raised the question of the time point of de novo

Cdc45 protein expression in a reversible system, such

as in cells released from G0 to start proliferation To

this end, T98G cells were made quiescent by a

com-bination of serum starvation and contact inhibition

Cell-cycle re-entry was induced by the addition of

10% fetal bovine serum and the subsequent splitting

of culture cells to enhance proliferation The trans-ition from G0 to proliferation was monitored by flow cytometry (Fig 5A; percentage of cell population in

G0, G1, S, G2⁄ M) and BrdU incorporation into cells (Fig 5B) In addition, the expression of cyclin D1, cyclin A, cyclin B1 and p27KIP1 was determined by western blotting (Fig 5C) p27KIP1 was reported to

be elevated in quiescent cells [35] and to become degraded by the ubiquitin–proteasome pathway after stimulation of cells with growth factors [36] A signi-ficant decrease in the p27KIP1 protein level was seen

6 h after serum addition (Fig 5C) Cyclin expression started in a defined order beginning with cyclin D1

A

B

C

Fig 4 Regulation of human Cdc45 protein during exit into senes-cence (A,B) Immunoblot analysis of whole-cell lysates of MRC-5 (A) and WI-38 (B) fibroblasts with the indicated passage numbers b-Actin served as a control for equal loading The percentage of senescence-associated b-Gal-positive cells (b-Gal) is depicted above the passage number (C) Detection of senescence-associated b-Gal activity in WI-38 cells of passage 18 and 28 cells (·20).

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3 h after serum stimulation in early G1, cyclin A

after 18 h of serum stimulation at the G1⁄ S

trans-ition, and cyclin B1  9 h later during the S phase

(Fig 5C) Flow cytometry analysis and BrdU

incor-poration, together with cyclin A accumulation,

indica-ted that cells starindica-ted replication at 18–21 h after

serum stimulation (Fig 5) As described, Cdc45

pro-tein was not expressed in G0 T98G cells (Figs 2,5C

time point 0 h), but became detectable at 15 h after

serum re-addition in late G1 phase, which was  3 h

after Cdc6 expression but 3 h before the p180 sub-unit of DNA polymerase a showed up (Fig 5C) These results indicate that human Cdc45 protein is synthesized de novo after G0 release prior to the S-phase entry in consistence with its requirement for the initiation of DNA replication Remarkably, the observed time course of expression of Cdc6, Cdc45 and DNA polymerase a seems to mirror the time course of loading of these replication factors to the origins of replication

A

B

C

Fig 5 Expression of human Cdc45 protein after serum stimulation T98G cells were arrested by serum starvation in the G 0 phase and sti-mulated with 10% fetal bovine serum to re-enter the cell cycle Samples were taken at the indicated time points after serum stimulation and from asynchronously proliferating cells (log) (A) In order to assess cell-cycle progression, flow-cytometry analysis was performed (B) To determine the percentage of replicating cells, the cells were pulse labelled with BrdU (C) SDS ⁄ PAGE and western blotting were performed with whole-cell lysates from 2 · 10 5 cells for each time point after serum stimulation p27 KIP1 , cyclin D1, cyclin A and cyclin B1 were ana-lysed to determine entry into and passage through cell cycle.

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Half-life of Cdc45 protein and number of Cdc45

molecules in proliferating human cells

In human cells, the half-life of Cdc6 is very short,

whereas that of Mcm3 is significantly higher [7,37]

Here, we determined the half-life of human Cdc45

protein in logarithmically growing HeLa S3 cells by

performing [35S]-pulse-chase labelling of proteins

Approximately equal amounts of protein were taken

from cell extracts after the indicated chase periods with

unlabelled cysteine These samples were

immunoprecip-itated and analysed by SDS gel electrophoresis,

west-ern blotting and autoradiography (Fig 6) Westwest-ern

blotting demonstrated that the precipitates contained

approximately equal amounts of the human Cdc45

protein Autoradiography of these samples showed a

significant reduction in the radiolabelled Cdc45 protein

to  40% after a chase period of 12 h (Fig 6A)

Therefore, endogenous Cdc45 can be described as a

stable protein with a half-life of 10 h in proliferating

HeLa S3 cells (Fig 6B)

The number of molecules of replication proteins in

HeLa cells varies from 1· 106 for Mcm3 [20] to

3· 104for both Cdt1 and geminin [24] Here we deter-mined the number of Cdc45 molecules in HeLa S3 and T98G cells by loading known amounts of recombinant His6–Cdc45 onto an SDS gel alongside total cell lysates from 2· 105 asynchronously growing cells Quantification of the western blot signals revealed that

 1 ng of Cdc45 protein was present in 2 · 105 HeLa S3 as well as in T98G cells (Fig 7B) Because the molecular mass of Cdc45 is 65.5 kDa it can be cal-culated that 4.5 · 104 molecules were present in each cell of these two human cell lines It should be kept in mind that the Cdc45 protein was detectable in all sta-ges of the cell cycle of proliferating cells (Fig 1B,C)

Cdc45 is overexpressed in cancer-derived cell lines and can serve as a biomarker for tumour cells using immunohistology

After showing a positive correlation between Cdc45 expression and cell proliferation, we examined the expression levels of the protein in different cancer-derived cell lines in comparison with primary cells Cell extracts were prepared from the primary cells WI-38, MRC-5 and HEF in low passage numbers, as well as

A

B

Fig 6 Estimation of Cdc45 protein half-life Metabolic labelling of

logarithmically growing HeLa S3 cells was performed to measure

the half-life of human Cdc45 protein (A) [ 35 S]-pulse-chase labelling

and IP with Cdc45-specific antibody was performed as described in

Experimental procedures Briefly, HeLa S3 cells were labelled with

[ 35 S]-methionine and -cysteine and were collected after the

indica-ted chase periods Then whole-cell extracts were prepared and

1 mg extract for each time point was subjected to IP The

precipi-tates were separated on a 10% SDS polyacrylamide gel and

trans-ferred onto a poly(vinylidene difluoride) membrane Cdc45 signals

were determined by immunoblotting and by autoradiography as

indicated (B) The autoradiographic Cdc45 bands were quantified

with the program PHORETIX 1 D ADVANCED , and depicted in a graph.

A

B

Fig 7 Calculation of the number of Cdc45 molecules per HeLa S3 and T98G cell (A) Human Cdc45 was expressed as His 6 -tagged protein in High five TM insect cells, purified on Co-Talon TM MS ana-lysis revealed that the band marked with an asterisk was recombin-ant Cdc45, the band above Cdc45 was heat shock protein 70 and the bands below were cytokeratin 1 and 9 Four microlitres of the eluted fraction was loaded onto a SDS gel together with declining amounts of BSA After staining with PageBlue TM protein-staining solution (Fermentas) the bands were quantified with the program PHORETIX 1 D ADVANCED (B) Whole cell extracts of 2 · 10 5 asynchro-nously proliferating HeLa S3 and T98G cells were run alongside with declining amounts of recombinant human His 6 -Cdc45 The gel was immunoblotted and probed with the anti-Cdc45 serum and an HRP-coupled secondary antibody using the enhanced chemolumi-nescence technique The positions of endogenous and recombinant His6-tagged Cdc45 are marked The protein bands were quantified with the program PHORETIX 1 D ADVANCED

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from human cell lines that represented carcinoma-,

sarcoma-, leukaemia- and lymphoma-derived cells (for

details see description in Fig 8) Western blot analysis

revealed that cancer-derived cell lines had consistently

higher Cdc45 levels than the tested primary lines

(Fig 8A,B) Interestingly, Cdc45 was exclusively

detec-ted as a double band in HL60 cells (Figs 3A,8B),

whereas Cdc45 appeared as a single band in other

leukaemia-derived cell lines The investigation of the

nature of the Cdc45 double band is still in progress

Although Cdc45 was found in actively cycling cells

it became undetectable in nonproliferating cells

(Figs 1–4 and Fig 8B, lane 1) These observations led

us to investigate whether the mAb C45-3G10 raised

against human Cdc45 [23,38] can be used for

histologi-cal sections The antibody was tested on formalin-fixed

paraffin-embedded normal human skin sections as well

as on invasive-lobular mamma carcinoma and small

cell bronchial carcinoma sections using standard

immunohistochemical procedures (Fig 9) Expression

of Ki-67 and PCNA, both approved markers for

pro-liferating cells [39], were stained on parallel sections of

the same preparation (Fig 9A,B)

The Cdc45-specific antibody C45-3G10 worked well

for immunohistochemical staining on formalin-fixed

paraffin-embedded tissues (Fig 9) In normal human

skin sections there were fewer Cdc45-positive than PCNA- or Ki-67-positive cells Cdc45

immunoreactivi-ty was mostly nuclear although a weak cytoplasmic staining was also seen (Fig 9A) In a series of inva-sive-lobular mamma carcinoma sections the antibodies against Cdc45 and PCNA intensely stained in a very similar manner tumour-associated cells (Fig 9B) Some proliferating fibroblasts or activated lymphocytes adja-cent to the malignant cells also showed Cdc45 staining The Ki-67 signal was associated only with a small frac-tion of the malignant cell populafrac-tion (Fig 9B) The lower percentage of Ki-67-stained cells in comparison with Cdc45 or PCNA might have been caused by the fact that the specimen consisted of a relatively slow growing cell population with a high number of cells in the G1 phase Ki-67 is a short-lived protein [40] pre-dominantly expressed during the S, G2 and M phases [27], whereas Cdc45 is present in comparable amounts throughout the cell cycle (Fig 1)

Discussion

Previous reports have shown that the amounts of human Mcm2, -3, -5, -7 and Orc2 remain constant during the cell cycle [6,41], whereas levels of Cdc6 and Cdt1 fluctuate [37,42] Here, we showed that in HeLa S3 (Fig 1B) and T98G cells (data not shown) levels of human Cdc45 protein remained constant dur-ing the cell cycle This confirms a previous report, in which, according to western blot analysis of HeLa cells, the protein level of Cdc45 remained unchanged during the cell cycle, whereas the amount of Cdc45 mRNA peaked at G1⁄ S [43] Although Cdc45 protein levels remained constant in proliferating cells (Fig 1B),

we detected significant changes in subcellular localiza-tion over the cell cycle (Fig 1C) In HeLa S3 (Fig 1C) and T98G glioblastoma cells (data not shown), Cdc45 protein was found exclusively in the nucleus during G1

to G2, but was distributed throughout the whole cell following breakdown of the nuclear membrane in mitosis In S-phase cells, the Cdc45 signal changed from a dispersed distribution to local accumulations, which colocalized with BrdU signals (Fig 1C), as reported for HeLa S3 cells [23]

When the cells exited the proliferative cycle and entered a nonproliferative state the licensing factors Cdt1, Cdc6 and Mcms were downregulated [6,8,24, 44,45] This contrasts to a persistence of the Orc2 protein in nonproliferating cells [6,7,46], which points to other functions of Orc proteins in addition to DNA replication, for example, transcriptional silencing Here,

we show that Cdc45 was downregulated completely when human cells ceased proliferation and entered into

A

B

Fig 8 Cdc45 is highly expressed in human cancer-derived cell

lines Immunoblot analysis of the Cdc45 protein level in whole-cell

lysates of various human cell lines The level of b-tubulin served to

monitor equal loading (A) Lanes 1–8: MRC-5 (human embryonic

lung fibroblasts), WI-38 (human embryonic lung fibroblasts),

HeLa S3 (cervix carcinoma), HEp2 (cervix carcinoma), MCF-7

(breast carcinoma), BT-20 (breast carcinoma), Saos-2

(osteosarco-ma) and T98G (glioblasto(osteosarco-ma), respectively (B) Lanes 1–8: PBL

(pri-mary unstimulated blood lymphocytes isolated from fresh blood

of a healthy volunteer), HEF (human embryonic lung fibroblasts),

WI-38 (human embryonic lung fibroblasts), CEM (acute

lymphoblas-tic leukaemia), Jurkat (acute T-cell leukaemia), HL60 (acute

pro-myelocytic leukaemia), K562 (chronic myelogenous leukaemia), and

U-937 (histiocytic leukaemia), respectively.

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quiescence, terminal differentiation or senescence

(Figs 2–4, supplementary Fig S1) Furthermore, both

in mouse cells [25] and human cells leaving the G0phase,

Cdc45 reappeared shortly before a new S phase started

(Fig 5) Downregulation of the essential replication

fac-tor Cdc45 seems to reflect an additional control

mechan-ism over the breakdown of licensing factors to ensure

the inactivity of replication origins in cells that had left

the mitotic cycle Previous reports clearly exhibited that

E2F-regulated promoters were transcriptional silenced

in quiescent as well as in senescent cells [47,48] E2F-binding sites were identified in the promoter regions of mammalian MCM genes [41], the CDC6 gene [49] and the gene for DNA polymerase a [50] Because

an ‘E2F-binding site’-like element was found on human Cdc45 cDNA [25] and Cdc45 protein was completely absent from nonproliferating cells (Figs 2–4), it is reasonable to assume that expression is regulated via the pRb-E2F pathway However, the observed consecutive expression of Cdc6, Cdc45 and polymerase a (Fig 5C)

Fig 9 Immunohistochemical detection of human Cdc45, PCNA and Ki-67 The proteins Cdc45, Ki-67 and PCNA were detected in formalin-fixed paraffin-embedded serial sections and visualized by the avidin–biotin complex technique (for details see Experimental procedures) (A) Cdc45, PCNA and Ki-67 were detected as indicated in serial sections of normal human skin The scale bar represents 50 lm (·40 objective and ·2.5 projective) (B) Cdc45, PCNA and Ki-67 were detected in serial sections of invasive-lobular mamma carcinoma The scale bar repre-sents 200 lm (·10 objective and ·2.5 projective).

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