DNA Damage-Processing Pathways Involved in the Eukaryotic
Cellular Response to Anticancer DNA Cross-Linking Drugs
Vladimir Beljanski, Luigi G. Marzilli, and Paul W. Doetsch
Departments of Chemistry (V.B., L.G.M.) and Biochemistry (P.W.D.) and Division of Cancer Biology and Department of
Radiation Oncology (P.W.D.), Emory University, Atlanta, Georgia; and Department of Chemistry, Louisiana State University,
Baton Rouge, Louisiana (L.G.M.)
Received November 12, 2003; accepted March 5, 2004 This article is available online at http://molpharm.aspetjournals.org
ABSTRACT
We used a panel of isogenic Saccharomyces cerevisiae strains
compromised in several different DNA damage-processing
pathways to assess in vivo processing of DNA adducts induced
by four cross-linking anticancer drugs. By examining cytotox-
icity profiles, cell cycle arrest patterns, and determining recom-
bination and mutation frequencies, we found that cisplatin-,
nitrogen mustard-, mitomycin-, and carmustine-induced DNA
adducts in S. cerevisiae are processed by components of the
nucleotide excision repair (NER), recombination repair (RR),
and translesion synthesis (TLS) pathways, with substantially
different contributions of each pathway for the drugs studied
here. In contrast to previous studies that used single pathway-
compromised strains to identify genes that mediate sensitivity
to DNA cross-linking drugs, we used strains that were compro-
mised in multiple pathways. By doing so, we were able to
establish several functions that were previously unknown and
interconnections between different DNA damage-processing
pathways. To our surprise, we found that for cisplatin-induced
cytotoxicity, TLS and RR contribute to survival to a significant
extent. In the case of nitrogen mustard DNA adduct processing,
equal involvement of two major pathways was established: one
that requires functional RR and NER components and one that
requires functional TLS and NER components. These data re-
veal the complexity of DNA cross-link processing that, in many
cases, requires interactions of components from several differ-
ent DNA damage-processing systems. We demonstrate the
usefulness of yeast strains with multiple simultaneous defects
in DNA damage-processing pathways for studying the modes
of action of anticancer drugs.
Compounds that form chemical bonds with DNA molecules
represent several important classes of anticancer drugs. A
large number of such compounds have been synthesized and
tested for anticancer activity, and many of them are in clin-
ical use. These drugs include nitrogen mustards, the aziri-
dines, the alkane sulfonates, the nitrosoureas, and platinum
compounds (Pratt, 1994; Lawley and Phillips, 1996; Tannock
and Goldenberg, 1998). All of these drugs interact with a
variety of biomolecules in cells, but the most important as-
pect responsible for their cytotoxicity seems to be inhibition
of cell division or stimulation of apoptosis caused by the
formation of DNA adducts (Tannock and Goldenberg, 1998).
Important examples of such drugs include cisplatin, nitrogen
mustard, mitomycin, and carmustine (Fig. 1) (Dronkert and
Kanaar, 2001).
Once DNA adducts are formed, to carry out normal DNA
transactions, such as replication and transcription, cells must
be able to remove or to tolerate the presence of such DNA
damage. Generally, base excision repair (BER) removes base
damage that causes relatively minor distortions in DNA (Memi-
soglu and Samson, 2000). Nucleotide excision repair (NER) is a
major pathway by which cells remove bulky, DNA helix-distort-
ing adducts (Friedberg et al., 1995). Mismatch repair (MMR)
corrects errors (insertions, deletions, and/or base substitutions)
created during DNA replication (Harfe and Jinks-Robertson,
2000). Homologous recombination repair (RR) and translesion
synthesis (TLS) also provide routes by which cells can continue
replication despite the presence of replication fork-blocking ad-
ducts (Doetsch et al., 2001). RR and TLS are often regarded as
DNA damage-tolerance pathways because they allow cells to
complete replication and mitosis at the expense of increasing
mutation and recombination frequencies. These pathways are
summarized in Fig. 2.
Resistance of cancer cells to chemotherapeutic drugs is a
major problem encountered in the treatment of tumors (Tan-
nock and Goldenberg, 1998). The basis for resistance has
been studied extensively and can be drug-specific, or nonspe-
cific as in the case of alkylating and platinum drugs (Pratt,
This research was supported by National Institutes of Health Grants
CA073041 and ES11163 (to P.W.D.) and GM29222 (to L.G.M.).
ABBREVIATIONS: BER, base excision repair; NER, nucleotide excision repair; MMR, mismatch repair; RR, recombination repair; TLS, translesion
synthesis; YEPD, medium composed of 1% yeast extract, 2% Bacto-peptone, 2% dextrose, 2% agar, and 0.005% adenine sulfate.
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