[CANCER RESEARCH 58. 767-778. February 15, 1998]
Defective Expression of the DNA Mismatch Repair Protein, MLH1, Alters G2-M
Cell Cycle Checkpoint Arrest following Ionizing Radiation1
Thomas W. Davis, Carmell Wilson-Van Patten, Mark Meyers, Keith A. Kunugi, Scott Cuthill,2 Catherine Reznikoff,
Christopher Garces, C. Richard Roland, Timothy J. Kinsella, Richard Fishel, and David A. Boothman3
Department of Human Oncology. University of Wisconsin-Madison, Madison, Wisconsin 53792 ¡T.W. D., C. W-V. P., M. M.. K. A. K.. S. C. C. K., C. G.. T. J. K.. D. A. B.¡;
Department of Medicine and the Cancer Center, University of California-San Diego. La Jolla, California 92093 ¡C.R. B./; and DNA Repair and Molecular Carcinogenesis
Program, Kimmel Cancer Institute, Thomas Jefferson University, Philadelphia, Pennsvlvania 19107 ¡R.F.]
ABSTRACT
A role for the Mut L homologue-1 (MLH1) protein, a necessary com
ponent of DNA mismatch repair (MMR), in G2-M cell cycle checkpoint
arrest after 6-thioguanine (6-TG) exposure was suggested previously. A
potential role for MLH1 in G, arrest and/or G,-S transition after damage
was, however, not discounted. We report that MLHl-deficient human
colon carcinoma (IK'II16) cells showed decreased survival and a con
comitant deficiency in G2-M cell cycle checkpoint arrest after ionizing
radiation (IR) compared with genetically matched, MMR-corrected hu
man colon carcinoma (IK"11 Id 3-6) cells. Similar responses were noted
between murine MLH1 knockout compared to wild-type primary embry
onic fibroblasts. MMR-deficient HCT116 cells or embryonic fibroblasts
from Ml,111 knockout mice also demonstrated classic DNA damage tol
erance responses after 6-TG exposure. Interestingly, an enhanced p53
protein induction response was observed in HCT116 3-6 (MLHI ' ) com
pared with HCT116 (MI.Hl ) cells after IR or 6-TG. Retroviral vector-
mediated expression of the E6 protein did not, however, affect the en
hanced G2-M cell cycle arrest observed in IK" 1 116 3—6compared with
MLHl-deficient IK II16 cells. A role for MLH1 in G2-M cell cycle
checkpoint control, without alteration in G,, after IR was also suggested
by similar S-phase progression between irradiated MLHl-deficient and
MLHl-proficient human or murine cells. Introduction of a nocodazole-
induced G2-M block, which corrected the MLHl-mediated G2-M arrest
deficiency in IK I 116 cells, clearly demonstrated that IK Til ft and
IK II16 3-6 cells did not differ in G, arrest or G,-S cell cycle transition
after IR. Thus, our data indicate that MLH1 does not play a major role in
G, cell cycle transition or arrest. We also show that human MLH1 and
MSH2 steady-state protein levels did not vary with damage or cell cycle
changes caused by IR or 6-TG. MLHl-mediated G2-M cell cycle delay
(caused by either MMR proofreading of DNA lesions or by a direct
function of the MLH1 protein in cell cycle arrest) may be important for
DNA damage detection and repair prior to chromosome segregation to
eliminate carcinogenic lesions (possibly brought on by misrepair) in
daughter cells.
INTRODUCTION
Hereditary nonpolyposis colorectal cancer is a familial colon cancer
syndrome that accounts for 1-5% of all colorectal tumors (1). This
syndrome is caused by inherited mutations in several MMR4 genes,
Received 7/23/97; accepted 12/16/97.
The coses of publication of this article were defrayed in part by the payment of page
charges. This article must therefore be hereby marked advertisement in accordance with
18 U.S.C. Section 1734 solely to indicate this fact.
1This work was supported by Grant DE-FO02-93ER61707-06 from the U. S. Depart
ment of Energy, Health Effects Research Division (to D. A. B.), and by NIH Grant
90-DKHD-10 (to T. W. D.). A preliminary version of this work was presented, in part, at
the 1996 American Association for Cancer Research Annual Meeting, April 20-24,
Washington, DC.
2 Present address: Roche Discovery Welwyn. Broadwater Road, Welwyn Garden City,
Hertfordshire AL7 3AY, United Kingdom.
3 To whom requests for reprints should be addressed, at Department of Human
Oncology, University of Wisconsin-Madison, K4/626 Clinical Sciences Center, 600
Highland Avenue. Madison, WI 53792. Phone: (608)262-4970; Fax: (608)263-8613;
E-mail: boothman@humonc.wisc.edu.
4 The abbreviations used were: MMR, mismatch repair; 6-TG, 6-lhioguanine; MNNG,
/V-methyl-/V"-nitrosoguanidine; DSB. DNA double-strand break; MLHI, mutL homo
logue-1; MSH2, human mutS homologue; PMS2, postmeiotic segregation homologue-2;
IR, ionizing radiation; SER, survival enhancement ratio (i.e., the dose of IR required to kill
including MSH2, MLHI, and PMS25 (2-6). Mutations within these
genes have also been observed in sporadic cancers of various origins
(7-10). The MMR system is important for maintaining genomic
fidelity through the recognition and repair of incorrectly paired nu-
cleotides, which can arise in DNA by physical damage to existing
nucleotides, DNA polymerase incorporation errors, or heteroduplex
formation during genetic recombinational events (11-14). Expression
of the MLHI gene, mapped to chromosome 3p21, is essential for
competent MMR and maintenance of microsatellite stability (15, 16).
Because MLH1 has no known enzymatic activity or functional motifs,
it has been hypothesized to play a role as a "molecular matchmaker"
for other DNA repair proteins (17). Transgenic mice lacking MLHI
expression develop normally but present with lymphomas at an early
age and are sterile, presumably due to faulty meiotic chromosome
segregation (18, 19). To date, the only data on functional activity in
mammalian cells suggest that the MLH 1 protein may regulate G2-M
cell cycle checkpoint arrest following 6-TG or MNNG exposure,
which results in DNA base damage and mispaired lesions (20).
Previously, Hawn et al. (20) and Hawn et al. (21) generated and
characterized a genetically matched human colon carcinoma model
system, HCT116 (MLH1~) and HCT116 3-6 (MLHT). HCT116
cells were deficient in DNA MMR (22) due to the lack of MLH 1
transcript expression (4, 5). HCT116 3-6 (MLH1+) cells were gen
erated by introducing (via microcell fusion) a single copy of normal
human chromosome 3 into HCT116 cells (21). These corrected cells
demonstrated expression of the MLHI transcript (by single-strand
conformation polymorphism-PCR), reconstituted MMR, increased
stability in the maintenance of lengths of microsatellite sequences, and
an increased sensitivity to MNNG or 6-TG (20, 21). HCT116 cells
were apparently defective in the G2-M cell cycle arrest checkpoint
when compared with the MMR-competent, HCT116 3-6 cells after
6-TG exposure (20). These previous data did not, however, eliminate
a role for the MLHI protein in G, arrest or transition from G, into S
phase.
In general, the mechanisms of damage-induced G2-M cell cycle
checkpoint arrest in mammalian cells are poorly understood. A num
ber of regulatory proteins have been implicated in the G2-M cell cycle
checkpoint, including cyclin Bl, lyn kinase, cdc2, cdc25, and topoi-
somerase II-a (23-30). We, therefore, sought to determine whether
the MLHI protein, and MMR in general, played a role in G2-M cell
cycle checkpoint responses following other forms of DNA damage,
such as IR. The role of MMR in processing damage caused by IR,
compared with agents that directly cause base mispairing (e.g., 6-TG),
is not known. IR treatment generates a myriad of DNA lesions,
including the formation of modified nucleotides, abasic sites, DNA-
protein cross-links, SSBs, and DSBs (31, 32). The most lethal of these
lesions are thought to be DSBs (33). DNA mismatches may arise
directly from IR treatment or may result from later DNA repair
50% of one cell line divided by the dose required to kill 50% of another); SSB, DNA
single-strand break.
' Throughout this report we use MLHI, MSH2, and PMS2 designations for both hunan
(HMLHI. HMSH2, and hPMS2) and murine (Mlhl. Msh2. and Pms2) genes.
767
Research.
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